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1-naphthyl phosphate + H2O
1-naphthol + phosphate
1-naphthyl phosphate + H2O
?
-
-
-
?
3,6-fluorescein diphosphate + H2O
? + phosphate
-
-
-
?
3-nitrobenzyl phosphate + H2O
3-nitrobenzyl alcohol + phosphate
-
-
-
-
?
3-o-methyl fluorescein phosphate + H2O
3-o-methyl fluorescein + phosphate
3-O-methylfluorescein phosphate + H2O
3-O-methylfluorescein + phosphate
-
-
-
-
?
4-methylumbelliferyl phosphate + H2O
4-methylumbelliferone + phosphate
-
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
4-nitrophenyl phosphate + H2O
p-nitrophenol + phosphate
-
-
-
-
?
4-nitrophenylphosphate + H2O
4-nitrophenol + phosphate
-
-
-
-
?
6,8-difluoro-4-methylumbelliferyl phosphate + H2O
6,8-difluoro-4-methylumbelliferol + phosphate
6,8-difluoro-4-methylumbelliferyl phosphate + H2O
6,8-difluoro-4-methylumbelliferone + phosphate
AAAAApYEEVH + H2O
AAAAAYEEVH + phosphate
-
substrate of RPTPalpha
-
-
?
AAAAApYRHRR + H2O
AAAAAYRHRR + phosphate
-
substrate of RPTPalpha
-
-
?
Ac-AAAApYAAAA-NH2 + H2O
Ac-AAAAYAAAA-NH2 + phosphate
-
-
-
-
?
Ac-AAAEpYAAAA-NH2 + H2O
Ac-AAAEYAAAA-NH2 + phosphate
-
-
-
-
?
Ac-AAAQpYAAAA-NH2 + H2O
Ac-AAAQYAAAA-NH2 + phosphate
-
-
-
-
?
Ac-DGEEpYDDPF-NH2 + H2O
Ac-DGEEYDDPF-NH2 + phosphate
-
SKAP-HOM Tyr75 peptide
-
-
?
Ac-ENDEpYTARE-NH2 + H2O
Ac-ENDEYTARE-NH2 + phosphate
-
Lck Tyr394 peptide
-
-
?
Ac-TEPQpYQPGE-NH2 + H2O
Ac-TEPQYQPGE-NH2 + phosphate
-
Lck Tyr505 peptide
-
-
?
Ac-YGEEpYDDLY-NH2 + H2O
Ac-YGEEYDDLY-NH2 + phosphate
-
consensus peptide 1
-
-
?
Ac-YGYEpYDDEY-NH2 + H2O
Ac-YGYEYDDEY-NH2 + phosphate
-
consensus peptide 2
-
-
?
acetyl-DADEpY-NH2 + H2O
acetyl-DADEY-NH2 + phosphate
-
-
-
?
acetyl-DADEpYL-NH2 + H2O
acetyl-DADEYL-NH2 + phosphate
-
-
?
ADEDFpYAA + H2O
ADEDFYAA + phosphate
-
substrate of SHP-2
-
-
?
AKFEDTpYAA + H2O
AKFEDTYAA + phosphate
-
substrate of SHP-1
-
-
?
angiotensin I + H2O
? + phosphate
-
-
-
-
?
ApYR + H2O
AYR + phosphate
-
-
-
-
?
ARKRIpYAA + H2O
ARKRIYAA + phosphate
-
substrate of RPTPalpha
-
-
?
ASSDDpYAA + H2O
ASSDDYAA + phosphate
-
substrate of RPTPalpha
-
-
?
ATP + H2O
ADP + phosphate
AVWEFpYpYAA + H2O
? + phosphate
-
substrate of SHP-1
-
-
?
AWSpYADpYAA + H2O
? + phosphate
-
substrate of SHP-1
-
-
?
AYTEpYTpYAA + H2O
? + phosphate
-
substrate of SHP-1
-
-
?
beta-naphthyl phosphate + H2O
beta-naphthol + phosphate
-
-
-
-
?
bis(4-nitrophenyl) phosphate + H2O
?
-
-
-
?
bis-(p-phosphophenyl) methane + H2O
?
synthetic high-affinity low-molecular weight nonpeptide substrate
-
-
?
bovine serum albumin + H2O
? + phosphate
carboxyamidomethylated and maleylated lysozyme + H2O
?
-
-
-
-
?
carrier protein-Cdc2-phosphotyrosine + H2O
carrier protein-Cdc2-tyrosine + phosphate
-
-
-
-
?
carrier protein-Y3-phosphotyrosine + H2O
carrier protein-Y3-tyrosine + phosphate
-
-
-
-
?
carrier protein-Y5-phosphotyrosine + H2O
carrier protein-Y5-tyrosine + phosphate
-
-
-
-
?
casein tyrosine phosphate + H2O
casein tyrosine + phosphate
-
-
-
-
?
Cdk2-pTpY + H2O
Cdk2-TpY + phosphate
-
dephosphorylates Cdk/cyclins on pThr14 and/or pTyr15 residues
-
-
?
Cdk2-pTpY/CycA + H2O
Cdk2-pTY/CycA + phosphate
-
-
-
-
?
D-fructose 1,6-diphosphate + H2O
?
DADE(pY)LIPQQG + H2O
DADEYLIPQQG + phosphate
DADEpYIPQQG + H2O
DADEYIPQQG + phosphate
DADEpYLIPQQG + H2O
DADEYLIPQQG + phosphate
DAEDFpYAA + H2O
DAEDFYAA + phosphate
-
substrate of SHP-2
-
-
?
DDT-(3,5-difluoro)YDpYAA + H2O
DDT-(3,5-difluoro)YDYAA + phosphate
-
-
-
-
?
DDTYDpYAA + H2O
DDTYDYAA + phosphate
-
-
-
-
?
DFEDFpYAA + H2O
DFEDFYAA + phosphate
-
substrate of SHP-2
-
-
?
difluoromethylumbelliferyl phosphate + H2O
difluoromethylumbelliferone + phosphate
-
-
-
?
DNL-(3,5-difluoro)YpYWD + H2O
DNL-(3,5-difluoro)YYWD + phosphate
-
-
-
-
?
DNLYpYWD + H2O
DNLYYWD + phosphate
-
-
-
-
?
DRVpYIHPFHL + H2O
DRVYIHPFHL + phosphate
-
-
-
?
DWEDFpYAA + H2O
DWEDFYAA + phosphate
-
substrate of SHP-2
-
-
?
EADTApYAA + H2O
EADTAYAA + phosphate
-
substrate of RPTPalpha
-
-
?
EIFDFpYAA + H2O
EIFDFYAA + phosphate
-
substrate of SHP-1 and SHP-2
-
-
?
END(pY)INASL + H2O
ENDYINASL + phosphate
ENDpYINASL + H2O
ENDYINASL + phosphate
ENPE(pY)LGLD + H2O
ENPEYLGLD + phosphate
dephosphorylation at Tyr1248
-
-
?
ENPE(pY)LTPQ + H2O
ENPEYLTPQ + phosphate
dephosphorylation at Tyr1196
-
-
?
EphA3-phosphotyrosine + H2O
EphA3-tyrosine + phosphate
-
-
-
-
?
epidermal growth factor + H2O
? + phosphate
-
-
-
-
?
epidermal growth factor receptor + H2O
? + phosphate
-
with phosphotyrosine Tyr992
-
-
?
fatty acid binding protein + H2O
? + phosphate
-
i.e. ppI5
-
-
?
FDEDFpYAA + H2O
FDEDFYAA + phosphate
-
substrate of SHP-2
-
-
?
FDIDIpYAA + H2O
FDIDIYAA + phosphate
-
substrate of SHP-1 and SHP-2
-
-
?
FDNL(pY)2WDQD + H2O
FDNLYYWDQD + 2 phosphate
dephosphorylation at Tyr1221/1222
-
-
?
fluorescein diphosphate + H2O
?
-
-
-
-
?
fluorescein diphosphate + H2O
fluorescein phosphate + phosphate
-
-
-
?
FMN + H2O
?
-
lung enzyme
-
-
?
FMN + H2O
? + phosphate
-
71.8% of the activity with 4-nitrophenyl phosphate, lung enzyme
-
-
?
FYDIDpYAA + H2O
FYDIDYAA + phosphate
-
substrate of SHP-1 and SHP-2
-
-
?
Gab1 tyrosine phosphate + H2O
Gab1 tyrosine + phosphate
-
-
-
-
?
gastrin + H2O
? + phosphate
-
phosphorylated on tyrosine
-
-
?
GESDGGpYMDMSKD + H2O
GESDGGYMDMSKD + phosphate
-
this peptide corresponds to the sequence containing Tyr740 of the human platelet-derived growth factor receptor
-
-
?
GNGDpYMPMSPKS + H2O
GNGDYMPMSPKS + phosphate
-
-
-
-
?
H2O + O-phospho-L-tyrosyl-[Wzc]
L-tyrosyl-[Wzc] + phosphate
Wzb dephosphorylates protein tyrosine kinase Wzc
-
-
?
hirudin + H2O
? + phosphate
-
hirudin from leech, phosphorylated on tyrosine
-
-
?
human A431 membrane protein + H2O
? + phosphate
inositol hexakisphosphate + H2O
?
highest activity
-
-
?
insulin receptor phosphopeptide + H2O
insulin receptor peptide + phosphate
insulin-like growth factor-1 + H2O
? + phosphate
-
-
-
-
?
KRLIEDNE(pY)TARGQ + H2O
KRLIEDNEYTARGQ + phosphate
-
phosphopeptide derived from autophosphorylation of mammalian tyrosine kinase Lck
-
-
?
LDEpYVATR + H2O
LDEYVATR + phosphate
-
-
-
?
LIEDNEpYTARQGA + H2O
LIEDNEYTARQGA + phosphate
-
substrate of RPTPalpha
-
-
?
lysozyme + H2O
? + phosphate
-
reduced, carboxymethylated and maleylated
-
-
?
membrane protein 3 + H2O
? + phosphate
-
-
-
-
?
myelin basic protein + H2O
?
-
-
-
-
?
myelin basic protein + H2O
? + phosphate
-
-
-
-
?
myosin P-light chain + H2O
? + phosphate
-
-
-
-
?
n-nitrophenyl phosphate + H2O
n-nitrophenol + phosphate
-
-
-
-
?
nicotinic acetylcholine receptor + H2O
?
-
i.e. nAChR
-
-
?
nicotinic acetylcholine receptor + H2O
? + phosphate
-
i.e. nAChR
-
-
?
NKpYGN + H2O
NKYGN + phosphate
-
-
-
-
?
O-phospho-L-serine + H2O
L-serine + phosphate
-
very low activity with
-
-
?
O-phospho-L-threonine + H2O
L-threonine + phosphate
-
-
-
-
?
O-phospho-L-tyrosine + H2O
?
-
-
-
?
O-phospho-L-tyrosine + H2O
L-tyrosine + phosphate
O-phospho-L-tyrosine + H2O
tyrosine + phosphate
O-phospho-L-tyrosyl-[PTK1] + H2O
L-tyrosyl-[PTK1] + phosphate
p-nitrophenyl phosphate
p-nitrophenol + phosphate
-
-
-
-
?
p-nitrophenyl phosphate + H2O
p-nitrophenol + phosphate
p120ctn + H2O
120ctn + phosphate
paxilin tyrosine phosphate + H2O
paxilin tyrosine + phosphate
PGSAAP-pY-LKTKFI + H2O
PGSAAPYLKTKFI + phosphate
STAT3 peptide
-
-
?
phenolphthalein diphosphate + H2O
?
-
-
-
?
phenyl phosphate + H2O
phenol + phosphate
-
-
-
-
?
phosphocaveolin-1 + H2O
caveolin-1 + phosphate
-
phosphorylated at Y14
-
-
?
phosphoprotein + H2O
protein + phosphate
-
-
-
-
?
phosphorylated Abelson interacting protein + H2O
Abelson interacting protein + phosphate
-
-
-
-
?
phosphorylated Abl tyrosine kinase + H2O
Abl tyrosine kinase + phosphate
-
-
-
-
?
phosphorylated Ack protein + H2O
Ack protein + phosphate
-
-
-
-
?
phosphorylated actin + H2O
actin + phosphate
-
-
-
-
?
phosphorylated adenomatous Polyposis coli-protein + H2O
adenomatous Polyposis coli-protein + phosphate
-
-
-
-
?
phosphorylated alpha-actinin + H2O
alpha-actinin + phosphate
-
-
-
-
?
phosphorylated AMP-activated protein kinase + H2O
AMP-activated protein kinase + phosphate
phosphorylated BCAR3 + H2O
BCAR3 + phosphate
-
-
-
-
?
phosphorylated BCR-Abl + H2O
BCR-Abl + phosphate
-
-
-
?
phosphorylated c-Kit + H2O
c-Kit + phosphate
-
dephosphorylation occurs at tyrosines 567/569 and 719
-
-
?
phosphorylated c-MET + H2O
c-MET + phosphate
phosphorylated c-Src + H2O
c-Src + phosphate
phosphorylated CD3 epsilon + H2O
CD3 epsilon + phosphate
-
-
-
-
?
phosphorylated Cdk2-pTpY/CycA protein + H2O
Cdk2-pTpY/CycA protein + phosphate
-
-
-
?
phosphorylated colony-stimulating factor 1 receptor + H2O
colony-stimulating factor 1 + phosphate
-
-
-
-
?
phosphorylated Down syndrome cell adhesion molecule + H2O
Down syndrome cell adhesion molecule + phosphate
-
-
-
-
?
phosphorylated E-cadherin + H2O
E-cadherin + phosphate
phosphorylated EphA2 receptor + H2O
EphA2 receptor + phosphate
-
-
-
-
?
phosphorylated EphA5 + H2O
EphA5 + phosphate
-
-
-
-
?
phosphorylated epidermal growth factor receptor + H2O
epidermal growth factor receptor + phosphate
phosphorylated ErbB1 + H2O
ErbB1 + phosphate
-
-
-
-
?
phosphorylated ErbB2 + H2O
ErbB2 + phosphate
-
-
-
-
?
phosphorylated ERK + H2O
ERK + phosphate
phosphorylated ERK1 + H2O
ERK1 + phosphate
-
-
-
?
phosphorylated ERK2 + H2O
ERK2 + phosphate
HePTP binds the phosphorylated tyrosine of the Erk2 peptide (pY185), Erk2 residue T183, which is phosphorylated in maximally activated Erk2, is not essential for substrate recognition and binding by HePTP
-
-
?
phosphorylated eukaryotic-initiation-factor-4G + H2O
eukaryotic-initiation-factor-4G + phosphate
-
-
-
-
?
phosphorylated extracellular signal regulated kinase + H2O
extracellular signal regulated kinase + phosphate
-
-
-
-
?
phosphorylated extracellular signal-regulated kinase 1 + H2O
extracellular signal-regulated kinase 1 + phosphate
phosphorylated extracellular signal-regulated kinase 2 + H2O
extracellular signal-regulated kinase 2 + phosphate
phosphorylated Ezrin + H2O
Ezrin + phosphate
-
-
-
-
?
phosphorylated focal adhesion kinase + H2O
focal adhesion kinase + phosphate
-
dephosphorylation occurs at Tyr-397, PTPD1 activity is required for focal adhesion kinase autophosphorylation and adhesion plaque stability
-
-
?
phosphorylated fragile X related + H2O
fragile X related + phosphate
-
-
-
-
?
phosphorylated Gln3 + H2O
Gln3 + phosphate
-
Siw14, in combination with the protein kinase Npr1, regulates the intracellular localization of Gln3
-
-
?
phosphorylated HEM protein + H2O
HEM protein + phosphate
-
-
-
-
?
phosphorylated hepatocyte growth factor regulated tyrosine kinase substrate + H2O
hepatocyte growth factor regulated tyrosine kinase substrate + phosphate
-
-
-
-
?
phosphorylated Hsc-70-4 + H2O
Hsc-70-4 + phosphate
-
-
-
-
?
phosphorylated IGF-I receptor + H2O
IGF-I receptor + phosphate
-
isozyme p52shc
-
-
?
phosphorylated IGF-II mRNA-binding protein + H2O
IGF-II mRNA-binding protein + phosphate
-
-
-
-
?
phosphorylated insulin receptor + H2O
insulin receptor + phosphate
phosphorylated insulin receptor substrate-1 + H2O
insulin receptor substrate-1 + phosphate
-
-
-
-
?
phosphorylated insulin receptor substrate-2 + H2O
insulin receptor substrate-2 + phosphate
-
-
-
-
?
phosphorylated JAK2 + H2O
JAK2 + phosphate
-
SHP2 dephosphorylates the Tyr1007 site, preventing the formation of the JAK2-Socs1 complex
-
-
?
phosphorylated Janus kinase 2 + H2O
Janus kinase 2 + phosphate
phosphorylated JNK + H2O
JNK + phosphate
-
-
-
?
phosphorylated Jun amino-terminal kinase + H2O
Jun amino-terminal kinase + phosphate
-
-
-
-
?
phosphorylated Lasp protein + H2O
Lasp protein + phosphate
-
-
-
-
?
phosphorylated Lck + H2O
Lck + phosphate
-
component of the T cell receptor signaling pathway
-
-
?
phosphorylated mitogen-activated protein kinase + H2O
mitogen-activated protein kinase + phosphate
-
-
-
-
?
phosphorylated mitogen-activated protein kinase Pmk1p + H2O
mitogen-activated protein kinase Pmk1p + phosphate
phosphorylated Munc18c + H2O
Munc18c + phosphate
-
dephosphorylation at Tyr218/219 and Tyr521
-
-
?
phosphorylated p130 Crk-associated substrate + H2O
p130 Crk-associated substrate + phosphate
-
-
-
-
?
phosphorylated p130Cas + H2O
p130Cas + phosphate
-
-
-
-
?
phosphorylated p190B Rho-GTPase-activating protein + H2O
p190B Rho-GTPase-activating protein + phosphate
-
-
-
-
?
phosphorylated p38 mitogen-activated protein kinase + H2O
p38 mitogen-activated protein kinase + phosphate
phosphorylated p85
p85 + phosphate
-
-
-
-
?
phosphorylated PDGF- and VEGF-receptor related + H2O
PDGF- and VEGF-receptor related + phosphate
-
-
-
-
?
phosphorylated phospholipase Cgamma + H2O
phospholipase Cgamma + phosphate
phosphorylated platelet-derived growth factor receptor + H2O
platelet-derived growth factor receptor + phosphate
-
-
-
-
?
phosphorylated poly(A)-binding protein + H2O
poly(A)-binding protein + phosphate
-
-
-
-
?
phosphorylated polychaetoid + H2O
polychaetoid + phosphate
-
-
-
-
?
phosphorylated proline serine threonine-rich phosphatase interacting protein + H2O
proline serine threonine-rich phosphatase interacting protein + phosphate
-
-
-
-
?
phosphorylated proline-rich tyrosine kinase 2 + H2O
proline-rich tyrosine kinase 2 + phosphate
-
the enzyme directly binds to and dephosphorylates proline-rich tyrosine kinase 2 at Tyr402
-
-
?
phosphorylated protein kinase-like endoplasmic reticulum kinase + H2O
protein kinase-like endoplasmic reticulum kinase + phosphate
-
dephosphorylation at Tyr615
-
-
?
phosphorylated protein p85
protein p85 + phosphate
-
-
-
-
?
phosphorylated pyruvate kinase M2 + H2O
pyruvate kinase M2 + phosphate
-
-
-
-
?
phosphorylated rasputin + H2O
rasputin + phosphate
-
-
-
-
?
phosphorylated RET(C634R) oncoprotein + H2O
RET(C634R) oncoprotein + phosphate
-
dephosphorylation at Tyr905 and Tyr1062
-
-
?
phosphorylated RET-MEN2A oncoprotein + H2O
RET-MEN2A oncoprotein + phosphate
-
dephosphorylation at Tyr905 and Tyr1062
-
-
?
phosphorylated RET/PTC1 oncoprotein + H2O
RET/PTC1 oncoprotein + phosphate
-
dephosphorylation at Tyr905 and Tyr1062
-
-
?
phosphorylated RhoGAP15B + H2O
RhoGAP15B + phosphate
-
-
-
-
?
phosphorylated SCAR + H2O
SCAR + phosphate
-
-
-
-
?
phosphorylated SH3PX1 + H2O
SH3PX1 + phosphate
-
-
-
-
?
phosphorylated Shc protein + H2O
Shc protein + phosphate
-
-
-
-
?
phosphorylated signal transducer and activator of transcription 3 + H2O
signal transducer and activator of transcription 3 + phosphate
-
-
-
-
?
phosphorylated specifically Rac1-associated protein 1 + H2O
specifically Rac1-associated protein 1 + phosphate
-
-
-
-
?
phosphorylated Src + H2O
Src + phosphate
phosphorylated Src protein + H2O
Src protein + phosphate
-
-
-
-
?
phosphorylated Src tyrosine kinase + H2O
Src tyrosine kinase + phosphate
-
PTPD1 associates with and activates Src tyrosine kinase
-
-
?
phosphorylated STAT1 + H2O
STAT1 + phosphate
phosphorylated STAT1c + H2O
STAT1c + phosphate
phosphorylated STAT3 + H2O
STAT3 + phosphate
phosphorylated STAT5 + H2O
STAT5 + phosphate
-
purified SHP2 protein directly dephosphorylates STAT5 or tyrosine-phosphorylated peptides derived from STAT5
-
-
?
phosphorylated T cell antigen receptor chain zeta + H2O
T cell antigen receptor chain zeta + phosphate
-
-
-
-
?
phosphorylated T cell antigen receptor zeta + H2O
T cell antigen receptor zeta + phosphate
-
-
-
-
?
phosphorylated T-cell receptor-zeta subunit + H2O
T-cell receptor-zeta subunit + phosphate
-
dephosphorylates ITAMs of the T-cell receptor-zeta subunit
-
-
?
phosphorylated TCRzeta + H2O
TCRzeta + phosphate
-
PTPH1 dephosphorylates TCRzeta in vitro, inhibiting the downstream inflammatory signaling pathway
-
-
?
phosphorylated valosin containing protein + H2O
valosin containing protein + phosphate
-
-
-
-
?
phosphorylated vascular endothelial growth factor receptor 2 + H2O
vascular endothelial growth factor receptor 2 + phosphate
phosphorylated Vav + H2O
Vav + phosphate
-
component of the T cell receptor signaling pathway
-
-
?
phosphorylated voltage-gated potassium channel subunit Kv2.1 + H2O
voltage-gated potassium channel subunit Kv2.1 + phosphate
-
-
-
-
?
phosphorylated YwqD
YwqD + phosphate
-
protein implicated in UDP-glucuronate synthesis
-
-
?
phosphorylated YwqF
YwqF + phosphate
-
protein implicated in UDP-glucuronate synthesis
-
-
?
phosphorylated ZAP-70 + H2O
ZAP-70 + phosphate
-
-
-
-
?
phosphorylated Zap70 + H2O
Zap70 + phosphate
-
protein-tyrosine kinase
-
-
?
phosphoserine + H2O
serine + phosphate
-
-
-
-
?
phosphothreonine + H2O
threonine + phosphate
phosphotyrosine + H2O
tyrosine + phosphate
phosphotyrosine serum albumin + H2O
? + phosphate
phosphotyrosyl bovine serum albumin + H2O
tyrosyl-bovine serum albumin + phosphate
-
-
-
-
?
phosphotyrosyl casein + H2O
tyrosylcasein + phosphate
-
-
-
-
?
phosphotyrosyl histone + H2O
? + phosphate
-
-
-
-
?
phosphotyrosyl myelin basic protein + H2O
tyrosyl-myelin basic protein + phosphate
-
-
-
-
?
phosphotyrosyl reduced carboxyamidomethylated and maleylated lysozyme + H2O
tyrosyl-reduced carboxyamidomethylated and maleylated lysozyme + phosphate
-
-
-
-
?
phosphotyrosyl-casein + H2O
? + phosphate
phosphotyrosyl-STAT3 + H2O
STAT3 + phosphate
platelet-derived growth factor receptor + H2O
? + phosphate
PLC-gamma1 tyrosine phosphate + H2O
PLC-gamma1 tyrosine + phosphate
-
-
-
-
?
PLQR(pY)SEDP + H2O
PLQRYSEDP + phosphate
dephosphorylation at Tyr1112
-
-
?
poly(Glu,Tyr) + H2O
? + phosphate
PQDKEY-pY-KVKEPG + H2O
PQDKEYYKVKEPG + phosphate
JAK2 peptide
-
-
?
protein FAK + H2O
?
-
-
-
-
?
protein Shc + H2O
?
-
-
-
-
?
Raytide peptide + H2O
? + phosphate
-
-
-
-
?
RE-(3,5-difluoro)YEFpYAA + H2O
RE-(3,5-difluoro)YEFYAA + phosphate
-
-
-
-
?
REYEFpYAA + H2O
REYEFYAA + phosphate
-
-
-
-
?
RKGSGD-pY-MPMSPK + H2O
RKGSGDYMPMSPK + phosphate
IRS1 peptide
-
-
?
RRISTpYAA + H2O
RRISTYAA + phosphate
-
substrate of RPTPalpha
-
-
?
RRLIEDAEpYAARG + H2O
RRLIEDAEYAARG + phosphate
SASASpYDWEF + H2O
SASASYDWEF + phosphate
-
substrate of SHP-1 and SHP-2
-
-
?
SASASpYSASA + H2O
SASASYSASA + phosphate
SKAP-HOM + H2O
?
-
a cytosolic adaptor protein required for proper activation of the immune system, a bona fide Lyp substrate
-
-
?
soluble N-ethylmaleimide-sensitive factor attachment protein receptor + H2O
soluble N-ethylmaleimide-sensitive factor attachment protein receptor + phosphate
-
-
-
-
?
TATEPQpYQPGEN + H2O
TATEPQYQPGEN + phosphate
-
substrate of RPTPalpha
-
-
?
TATEPQpYQPGENL + H2O
TATEPQYQPGENL + phosphate
-
substrate of RPTPalpha
-
-
?
TEVGKRI(pY)RLVGDKN + H2O
TEVGKRIYRLVGDKN + phosphate
TGFLTELpYVATRWY + H2O
TGFLTELYVATRWY + phosphate
-
this peptide corresponds to the sequence containing Tyr204 of the human extracellular signal-regulated kinase
-
-
?
TRDIpYETDYYRK + H2O
TRDIYETDYYRK + phosphate
TSTEPQpYQPGENL + H2O
TSTEPQYQPGENL + phosphate
tyrosin kinase + H2O
? + phosphate
-
-
-
-
?
tyrosine-phosphorylated myelin basic protein + H2O
myelin basic protein + phosphate
-
-
-
?
tyrosine-phosphorylated Raytide + H2O
Raytide + phosphate
-
-
-
?
WAGDDpYAA + H2O
WAGDDYAA + phosphate
-
substrate of SHP-1 and SHP-2
-
-
?
WDEDFpYAA + H2O
WDEDFYAA + phosphate
-
substrate of SHP-2
-
-
?
WDEDFpYDWEF + H2O
WDEDFYDWEF + phosphate
-
substrate of SHP-1 and SHP-2
-
-
?
WDEDFpYRWKF + H2O
WDEDFYRWKF + phosphate
-
substrate of SHP-1 and SHP-2
-
-
?
WDEDFpYSASA + H2O
WDEDFYSASA + phosphate
WRKRFpYDWEF + H2O
WRKRFYDWEF + phosphate
-
substrate of SHP-1 and SHP-2
-
-
?
Y527-phosphorylated Src + H2O
Src + phosphate
-
-
-
-
?
YCRPESQEHPEADPGAAPpYLK + H2O
YCRPESQEHPEADPGAAYLK + phosphate
-
YCRPESQEHPEADPGAApYLK is signal transducer and activator of transcription 3, is dephosphorylated at Y705
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
[ATP synthase]-tyrosine phosphate + H2O
[ATP synthase]-tyrosine + phosphate
[casein]-tyrosine phosphate + H2O
[casein]-tyrosine + phosphate
-
-
-
?
[cytosolic 6-phosphofructokinase]-tyrosine phosphate + H2O
[cytosolic 6-phosphofructokinase]-tyrosine + phosphate
[diguanylate cyclase TpbB]-tyrosine phosphate + H2O
[diguanylate cyclase TpbB]-tyrosine + phosphate
[EGF receptor]-tyrosine1018 phosphate + H2O
[EGF receptor]-tyrosine1018 + phosphate
highest activity
-
-
?
[epidermal growth factor receptor 2]-tyrosine phosphate + H2O
[epidermal growth factor receptor 2]-tyrosine + phosphate
dephosphorylation of epidermal growth factor receptor 2 (HER2)-pY1196 site
-
-
?
[epidermal growth factor receptor]-tyrosine phosphate + H2O
[epidermal growth factor receptor]-tyrosine + phosphate
[Eps15 peptide846-854 P850V]-tyrosine phosphate + H2O
[Eps15 peptide846-854 P850V]-tyrosine + phosphate
-
-
-
?
[Eps15 peptide846-854]-tyrosine phosphate + H2O
[Eps15 peptide846-854]-tyrosine + phosphate
[Eps15 peptide]-tyrosine phosphate + H2O
[Eps15 peptide]-tyrosine + phosphate
[FAK]-tyrosine phosphate + H2O
[FAK]-tyrosine + phosphate
dephosphorylation at Tyr397
-
-
?
[FHA-1]-tyrosine phosphate + H2O
[FHA-1]-tyrosine + phosphate
[FYN kinase]-tyrosine phosphate + H2O
[FYN kinase]-tyrosine + phosphate
-
-
-
?
[HER2]-tyrosine phosphate + H2O
[HER2]-tyrosine + phosphate
dephosphorylation at Tyr1112, Tyr1196, Tyr1221, Tyr1222, and Tyr1248
-
-
?
[insulin receptor kinase]-tyrosine phosphate + H2O
[insulin receptor kinase]-tyrosine + phosphate
-
-
-
?
[myelin basic protein]-tyrosine phosphate + H2O
[myelin basic protein]-tyrosine + phosphate
-
-
-
?
[p130Cas]-tyrosine phosphate + H2O
[p130Cas]-tyrosine + phosphate
dephosphorylation at Tyr165
-
-
?
[p190RhoGAP]-tyrosine phosphate + H2O
[p190RhoGAP]-tyrosine + phosphate
dephosphorylation at Tyr1105
-
-
?
[paxillin]-tyrosine phosphate + H2O
[paxillin]-tyrosine + phosphate
dephosphorylation at Tyr118
-
-
?
[protein Golgi p230]-tyrosine phosphate + H2O
[protein Golgi p230]-tyrosine + phosphate
[protein]-L-tyrosine phosphate + H2O
[protein]-L-tyrosine + phosphate
[protein]-tyrosine phosphate + H2O
[protein]-tyrosine + phosphate
[SRC]-tyrosine phosphate + H2O
[SRC]-tyrosine + phosphate
dephosphorylation at Tyr416
-
-
?
[sulfide quinone oxidoreductase]-tyrosine phosphate + H2O
[sulfide quinone oxidoreductase]-tyrosine + phosphate
[trifunctional enzyme]-tyrosine phosphate + H2O
[trifunctional enzyme]-tyrosine + phosphate
[VAV2]-tyrosine phosphate + H2O
[VAV2]-tyrosine + phosphate
dephosphorylation at Tyr172
-
-
?
[Wzb]-tyrosine phosphate + H2O
[Wzb]-tyrosine + phosphate
Wzb i.e. bacterial tyrosine kinase
-
-
?
additional information
?
-
1-naphthyl phosphate + H2O
1-naphthol + phosphate
-
89.3% of the activity with 4-nitrophenyl phosphate, lung enzyme
-
-
?
1-naphthyl phosphate + H2O
1-naphthol + phosphate
-
-
-
-
?
3-o-methyl fluorescein phosphate + H2O
3-o-methyl fluorescein + phosphate
-
-
-
?
3-o-methyl fluorescein phosphate + H2O
3-o-methyl fluorescein + phosphate
-
-
-
?
3-o-methyl fluorescein phosphate + H2O
3-o-methyl fluorescein + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
663621, 665502, 692217, 693943, 694291, 694608, 694902, 707683, 708290, 709293, 710237, 714433, 729298, 729368, 729393, 730564, 730970 -
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
acid phosphatase activity, best tested substrate
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
Q6JHV2
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
?
6,8-difluoro-4-methylumbelliferyl phosphate + H2O
6,8-difluoro-4-methylumbelliferol + phosphate
-
-
-
-
?
6,8-difluoro-4-methylumbelliferyl phosphate + H2O
6,8-difluoro-4-methylumbelliferol + phosphate
-
-
-
?
6,8-difluoro-4-methylumbelliferyl phosphate + H2O
6,8-difluoro-4-methylumbelliferol + phosphate
-
-
-
-
?
6,8-difluoro-4-methylumbelliferyl phosphate + H2O
6,8-difluoro-4-methylumbelliferone + phosphate
-
-
-
-
?
6,8-difluoro-4-methylumbelliferyl phosphate + H2O
6,8-difluoro-4-methylumbelliferone + phosphate
-
-
-
-
?
6,8-difluoro-4-methylumbelliferyl phosphate + H2O
6,8-difluoro-4-methylumbelliferone + phosphate
-
-
-
?
6,8-difluoro-4-methylumbelliferyl phosphate + H2O
6,8-difluoro-4-methylumbelliferone + phosphate
-
-
-
?
6,8-difluoro-4-methylumbelliferyl phosphate + H2O
6,8-difluoro-4-methylumbelliferone + phosphate
-
-
-
?
6,8-difluoro-4-methylumbelliferyl phosphate + H2O
6,8-difluoro-4-methylumbelliferone + phosphate
-
-
-
?
6,8-difluoro-4-methylumbelliferyl phosphate + H2O
6,8-difluoro-4-methylumbelliferone + phosphate
-
-
-
?
6,8-difluoro-4-methylumbelliferyl phosphate + H2O
6,8-difluoro-4-methylumbelliferone + phosphate
-
-
-
-
?
ADP + H2O
?
-
-
-
?
ATP + H2O
?
-
-
-
?
ATP + H2O
ADP + phosphate
-
9.5% activity compared to TRDIpYETDYYRK
-
-
?
ATP + H2O
ADP + phosphate
-
9.5% activity compared to TRDIpYETDYYRK
-
-
?
bovine serum albumin + H2O
? + phosphate
-
-
-
-
?
bovine serum albumin + H2O
? + phosphate
-
reduced, carboxamide methylated and succinylated
-
-
?
D-fructose 1,6-diphosphate + H2O
?
-
-
-
?
D-fructose 1,6-diphosphate + H2O
?
-
-
-
?
DADE(pY)LIPQQG + H2O
DADEYLIPQQG + phosphate
-
-
-
?
DADE(pY)LIPQQG + H2O
DADEYLIPQQG + phosphate
a physiological phosphopeptide substrate of enzyme PTP1B
-
-
?
DADE(pY)LIPQQG + H2O
DADEYLIPQQG + phosphate
a phosphopeptide substrate of enzyme PTP1B and the modified enzyme asPTP1B. asPTP1B dephosphorylates DADE(pY)LIPQQG at a rate that is only slightly lower than the rate of dephosphorylation induced by wild-type PTP1B
-
-
?
DADE(pY)LIPQQG + H2O
DADEYLIPQQG + phosphate
sequence equivalent to residues 988-998 of the epidermal growth factor receptor
-
-
?
DADE(pY)LIPQQG + H2O
DADEYLIPQQG + phosphate
phosphopeptide-2
-
-
?
DADE(pY)LIPQQG + H2O
DADEYLIPQQG + phosphate
phosphopeptide-2
-
-
?
DADEpYIPQQG + H2O
DADEYIPQQG + phosphate
-
specific substrate for PTP1B
-
-
?
DADEpYIPQQG + H2O
DADEYIPQQG + phosphate
-
specific substrate for PTP1B
-
-
?
DADEpYLIPQQG + H2O
DADEYLIPQQG + phosphate
-
-
-
?
DADEpYLIPQQG + H2O
DADEYLIPQQG + phosphate
-
-
-
?
DADEpYLIPQQG + H2O
DADEYLIPQQG + phosphate
a phosphopeptide substrate
-
-
?
END(pY)INASL + H2O
ENDYINASL + phosphate
phosphopeptide-1
-
-
?
END(pY)INASL + H2O
ENDYINASL + phosphate
phosphopeptide-1
-
-
?
ENDpYINASL + H2O
ENDYINASL + phosphate
Bracoviriform demolitoris
-
-
-
-
?
ENDpYINASL + H2O
ENDYINASL + phosphate
-
-
-
-
?
human A431 membrane protein + H2O
? + phosphate
-
-
-
-
?
human A431 membrane protein + H2O
? + phosphate
-
-
-
-
?
insulin receptor phosphopeptide + H2O
insulin receptor peptide + phosphate
-
-
-
-
?
insulin receptor phosphopeptide + H2O
insulin receptor peptide + phosphate
-
-
-
-
?
O-phospho-L-tyrosine + H2O
L-tyrosine + phosphate
-
-
-
-
?
O-phospho-L-tyrosine + H2O
L-tyrosine + phosphate
-
-
-
-
?
O-phospho-L-tyrosine + H2O
L-tyrosine + phosphate
-
-
-
-
?
O-phospho-L-tyrosine + H2O
tyrosine + phosphate
-
-
-
?
O-phospho-L-tyrosine + H2O
tyrosine + phosphate
-
-
-
?
O-phospho-L-tyrosine + H2O
tyrosine + phosphate
-
-
-
?
O-phospho-L-tyrosyl-[PTK1] + H2O
L-tyrosyl-[PTK1] + phosphate
-
-
-
?
O-phospho-L-tyrosyl-[PTK1] + H2O
L-tyrosyl-[PTK1] + phosphate
-
-
-
?
p-nitrophenyl phosphate + H2O
p-nitrophenol + phosphate
-
-
-
-
?
p-nitrophenyl phosphate + H2O
p-nitrophenol + phosphate
-
-
-
?
p-nitrophenyl phosphate + H2O
p-nitrophenol + phosphate
-
-
-
-
?
p-nitrophenyl phosphate + H2O
p-nitrophenol + phosphate
-
-
?
p-nitrophenyl phosphate + H2O
p-nitrophenol + phosphate
-
-
-
?
p-nitrophenyl phosphate + H2O
p-nitrophenol + phosphate
-
-
-
?
p-nitrophenyl phosphate + H2O
p-nitrophenol + phosphate
-
-
-
-
?
p-nitrophenyl phosphate + H2O
p-nitrophenol + phosphate
-
-
-
-
?
p-nitrophenyl phosphate + H2O
p-nitrophenol + phosphate
-
-
-
-
?
p-nitrophenyl phosphate + H2O
p-nitrophenol + phosphate
-
60.3% activity compared to TRDIpYETDYYRK
-
-
?
p-nitrophenyl phosphate + H2O
p-nitrophenol + phosphate
-
60.3% activity compared to TRDIpYETDYYRK
-
-
?
p-nitrophenyl phosphate + H2O
p-nitrophenol + phosphate
-
-
-
-
?
p-nitrophenyl phosphate + H2O
p-nitrophenol + phosphate
-
-
-
-
?
p-nitrophenyl phosphate + H2O
p-nitrophenol + phosphate
-
-
-
?
p-nitrophenyl phosphate + H2O
p-nitrophenol + phosphate
-
-
-
-
?
p120ctn + H2O
120ctn + phosphate
-
-
-
-
?
p120ctn + H2O
120ctn + phosphate
-
-
-
-
?
p38 + H2O
?
-
-
-
-
?
paxilin tyrosine phosphate + H2O
paxilin tyrosine + phosphate
-
PTPRT specifically regulates paxillin phosphorylation at Tyr88 in colorectal cancer cells
-
-
?
paxilin tyrosine phosphate + H2O
paxilin tyrosine + phosphate
-
substrate of PTPRT, inactive with paxilin mutant Y88F
-
-
?
phosphorylated AMP-activated protein kinase + H2O
AMP-activated protein kinase + phosphate
-
PTPB1 is involved in AMPK regulation through its phosphorylation in a tissue-specific manner, overview
-
-
?
phosphorylated AMP-activated protein kinase + H2O
AMP-activated protein kinase + phosphate
-
phosphorylation of the AMPK alpha subunit at Thr172
-
-
?
phosphorylated c-MET + H2O
c-MET + phosphate
-
-
-
-
?
phosphorylated c-MET + H2O
c-MET + phosphate
-
PTP1B and SHP-2 are bound to the c-Met receptor to control its activity, PTP1B acts as a negative regulator, increased binding and phosphorylation of SHP-2 coincide with maximal stimulation of c-Met, therefore acting as a positive regulator
-
-
?
phosphorylated c-MET + H2O
c-MET + phosphate
-
PTP1B and SHP-2 are bound to the c-Met receptor to control its activity, PTP1B acts as a negative regulator, increased binding and phosphorylation of SHP-2 coincide with maximal stimulation of c-Met, therefore acting as a positive regulator
-
-
?
phosphorylated c-Src + H2O
c-Src + phosphate
-
dephosphorylation activates c-Src
-
-
?
phosphorylated c-Src + H2O
c-Src + phosphate
-
dephosphorylation occurs at Tyr-527
-
-
?
phosphorylated E-cadherin + H2O
E-cadherin + phosphate
-
-
-
-
?
phosphorylated E-cadherin + H2O
E-cadherin + phosphate
-
-
-
-
?
phosphorylated epidermal growth factor receptor + H2O
epidermal growth factor receptor + phosphate
-
-
-
-
?
phosphorylated epidermal growth factor receptor + H2O
epidermal growth factor receptor + phosphate
-
-
preferential dephosphorylation at Y1068 and Y1173
-
?
phosphorylated epidermal growth factor receptor + H2O
epidermal growth factor receptor + phosphate
-
PTP1B negatively regulates EGF-induced signaling in HCEC cells by dephosphorylating the epidermal growth factor receptor
-
-
?
phosphorylated epidermal growth factor receptor + H2O
epidermal growth factor receptor + phosphate
-
inactivation of EGFR
-
-
?
phosphorylated epidermal growth factor receptor + H2O
epidermal growth factor receptor + phosphate
-
-
-
-
?
phosphorylated ERK + H2O
ERK + phosphate
-
dephosphorylation at Tyr-1175
-
-
?
phosphorylated ERK + H2O
ERK + phosphate
-
the cleavage of STEP leads to a catalytically active form, but this cleaved form no longer binds to and dephosphorylates its substrate phosphorylated ERK
-
-
?
phosphorylated extracellular signal-regulated kinase 1 + H2O
extracellular signal-regulated kinase 1 + phosphate
-
-
-
-
?
phosphorylated extracellular signal-regulated kinase 1 + H2O
extracellular signal-regulated kinase 1 + phosphate
-
-
-
-
?
phosphorylated extracellular signal-regulated kinase 2 + H2O
extracellular signal-regulated kinase 2 + phosphate
-
-
-
-
?
phosphorylated extracellular signal-regulated kinase 2 + H2O
extracellular signal-regulated kinase 2 + phosphate
-
-
-
-
?
phosphorylated insulin receptor + H2O
insulin receptor + phosphate
-
-
-
-
?
phosphorylated insulin receptor + H2O
insulin receptor + phosphate
-
-
-
?
phosphorylated insulin receptor + H2O
insulin receptor + phosphate
-
-
preferential dephosphorylation of Y1162/1163 of insulin receptor
-
?
phosphorylated Janus kinase 2 + H2O
Janus kinase 2 + phosphate
-
-
-
-
?
phosphorylated Janus kinase 2 + H2O
Janus kinase 2 + phosphate
-
-
-
-
?
phosphorylated mitogen-activated protein kinase Pmk1p + H2O
mitogen-activated protein kinase Pmk1p + phosphate
-
-
-
-
?
phosphorylated mitogen-activated protein kinase Pmk1p + H2O
mitogen-activated protein kinase Pmk1p + phosphate
-
-
-
-
?
phosphorylated p38 mitogen-activated protein kinase + H2O
p38 mitogen-activated protein kinase + phosphate
-
-
-
-
?
phosphorylated p38 mitogen-activated protein kinase + H2O
p38 mitogen-activated protein kinase + phosphate
-
-
-
?
phosphorylated phospholipase Cgamma + H2O
phospholipase Cgamma + phosphate
-
dephosphorylation occurs at Tyr-783
-
-
?
phosphorylated phospholipase Cgamma + H2O
phospholipase Cgamma + phosphate
-
dephosphorylation occurs at Tyr-783
-
-
?
phosphorylated Src + H2O
Src + phosphate
-
-
-
-
?
phosphorylated Src + H2O
Src + phosphate
-
DEP-1 is able to dephosphorylate the inhibitory Y529 and activate Src
-
-
?
phosphorylated STAT1 + H2O
STAT1 + phosphate
-
-
-
-
?
phosphorylated STAT1 + H2O
STAT1 + phosphate
-
purified GST-SHP2 dephosphorylates STAT1 at both tyrosine and serine residues when immunoprecipitated phosphorylated STAT1 or phosphor-peptides corresponding to the sequence surrounding Tyr701 or Ser727 of STAT1 are used as the substrates, SHP2 negatively regulates the interferon-induced JAK/STAT pathway by dephosphorylating STAT1
-
-
?
phosphorylated STAT1c + H2O
STAT1c + phosphate
-
-
-
-
?
phosphorylated STAT1c + H2O
STAT1c + phosphate
-
mode of STAT activation, whereby serine-threonine phosphorylation of the cognate protein tyrosine phosphatase PTP3 results in the inhibition of its activity, shifting the phosphorylation-dephosphorylation equilibrium in favour of phosphorylation, overview
-
-
?
phosphorylated STAT3 + H2O
STAT3 + phosphate
-
-
-
-
?
phosphorylated STAT3 + H2O
STAT3 + phosphate
-
SHP2 negatively regulates the activity of STAT3
-
-
?
phosphorylated vascular endothelial growth factor receptor 2 + H2O
vascular endothelial growth factor receptor 2 + phosphate
-
-
-
-
?
phosphorylated vascular endothelial growth factor receptor 2 + H2O
vascular endothelial growth factor receptor 2 + phosphate
-
dephosphorylation occurs at Tyr-1175, PTP1B binds to vascular endothelial growth factor receptor 2 cytoplasmic domain and directly dephosphorylates activated vascular endothelial growth factor receptor 2 immunoprecipitates
-
-
?
phosphothreonine + H2O
threonine + phosphate
-
-
-
-
?
phosphothreonine + H2O
threonine + phosphate
-
-
-
-
?
phosphothreonine + H2O
threonine + phosphate
-
-
-
-
?
phosphotyrosine + H2O
tyrosine + phosphate
-
-
-
-
?
phosphotyrosine + H2O
tyrosine + phosphate
-
-
-
?
phosphotyrosine + H2O
tyrosine + phosphate
-
45.2% of the activity with 4-nitrophenyl phosphate, lung enzyme
-
-
?
phosphotyrosine + H2O
tyrosine + phosphate
-
lung enzyme
-
-
?
phosphotyrosine + H2O
tyrosine + phosphate
Bracoviriform demolitoris
-
-
-
-
?
phosphotyrosine + H2O
tyrosine + phosphate
-
-
-
-
?
phosphotyrosine + H2O
tyrosine + phosphate
-
-
-
-
?
phosphotyrosine + H2O
tyrosine + phosphate
-
-
-
?
phosphotyrosine + H2O
tyrosine + phosphate
-
-
-
-
?
phosphotyrosine + H2O
tyrosine + phosphate
O14522, P10586, P17706, P18031, P18433, P23467, P23468, P23469, P23470, P23471, P26045, P28827, P29074, P29350, P35236, P43378, P54829, Q05209, Q06124, Q0VAE8, Q12913, Q12923, Q13332, Q15256, Q15262, Q15678, Q16825, Q16827, Q16849, Q4JDK3, Q92729, Q92932, Q99952, Q9H3S7, Q9HD43, Q9UMZ3, Q9Y2R2 -
-
-
?
phosphotyrosine + H2O
tyrosine + phosphate
-
-
-
?
phosphotyrosine + H2O
tyrosine + phosphate
-
-
-
?
phosphotyrosine + H2O
tyrosine + phosphate
-
-
-
-
?
phosphotyrosine + H2O
tyrosine + phosphate
-
-
-
-
?
phosphotyrosine + H2O
tyrosine + phosphate
-
-
-
-
?
phosphotyrosine + H2O
tyrosine + phosphate
-
-
-
-
?
phosphotyrosine + H2O
tyrosine + phosphate
-
-
-
-
?
phosphotyrosine + H2O
tyrosine + phosphate
-
best substrate
-
-
?
phosphotyrosine + H2O
tyrosine + phosphate
-
-
-
-
?
phosphotyrosine + H2O
tyrosine + phosphate
-
-
-
-
?
phosphotyrosine serum albumin + H2O
? + phosphate
-
-
-
-
?
phosphotyrosine serum albumin + H2O
? + phosphate
-
-
-
-
?
phosphotyrosyl-casein + H2O
? + phosphate
-
-
-
-
?
phosphotyrosyl-casein + H2O
? + phosphate
-
-
-
-
?
phosphotyrosyl-casein + H2O
? + phosphate
-
-
-
-
?
phosphotyrosyl-STAT3 + H2O
STAT3 + phosphate
-
-
-
-
?
phosphotyrosyl-STAT3 + H2O
STAT3 + phosphate
-
signal transducers and activator of transcription 3, STAT3, is a transcription factor that is associated with survival, proliferation, chemoresistance, and angiogenesis of tumor cells
-
-
?
platelet-derived growth factor receptor + H2O
? + phosphate
-
-
-
?
platelet-derived growth factor receptor + H2O
? + phosphate
-
with phosphotyrosine Tyr1021 or Tyr1009
-
-
?
poly(Glu,Tyr) + H2O
? + phosphate
-
-
-
-
?
poly(Glu,Tyr) + H2O
? + phosphate
-
-
-
-
?
poly(Glu,Tyr) + H2O
? + phosphate
-
-
-
-
?
RRLIEDAEpYAARG + H2O
RRLIEDAEYAARG + phosphate
-
-
-
-
?
RRLIEDAEpYAARG + H2O
RRLIEDAEYAARG + phosphate
-
-
-
-
?
SASASpYSASA + H2O
SASASYSASA + phosphate
-
substrate of RPTPalpha
-
-
?
SASASpYSASA + H2O
SASASYSASA + phosphate
-
substrate of SHP-1 and SHP-2
-
-
?
TEVGKRI(pY)RLVGDKN + H2O
TEVGKRIYRLVGDKN + phosphate
-
-
-
?
TEVGKRI(pY)RLVGDKN + H2O
TEVGKRIYRLVGDKN + phosphate
-
-
-
?
TRDIpYETDYYRK + H2O
TRDIYETDYYRK + phosphate
-
100% activity
-
-
?
TRDIpYETDYYRK + H2O
TRDIYETDYYRK + phosphate
-
100% activity
-
-
?
TSTEPQpYQPGENL + H2O
TSTEPQYQPGENL + phosphate
-
this sequence contains the C-terminal phosphorylation site of c-src with phosphorylated Tyr527
-
-
?
TSTEPQpYQPGENL + H2O
TSTEPQYQPGENL + phosphate
-
substrate of RPTPalpha
-
-
?
TSTEPQpYQPGENL + H2O
TSTEPQYQPGENL + phosphate
-
-
-
?
WDEDFpYSASA + H2O
WDEDFYSASA + phosphate
-
substrate of RPTPalpha
-
-
?
WDEDFpYSASA + H2O
WDEDFYSASA + phosphate
-
substrate of SHP-1 and SHP-2
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
-
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
-
-
-
-
?
[ATP synthase]-tyrosine phosphate + H2O
[ATP synthase]-tyrosine + phosphate
-
-
-
?
[ATP synthase]-tyrosine phosphate + H2O
[ATP synthase]-tyrosine + phosphate
-
-
-
?
[ATP synthase]-tyrosine phosphate + H2O
[ATP synthase]-tyrosine + phosphate
-
-
-
?
[cytosolic 6-phosphofructokinase]-tyrosine phosphate + H2O
[cytosolic 6-phosphofructokinase]-tyrosine + phosphate
-
-
-
?
[cytosolic 6-phosphofructokinase]-tyrosine phosphate + H2O
[cytosolic 6-phosphofructokinase]-tyrosine + phosphate
-
-
-
?
[cytosolic 6-phosphofructokinase]-tyrosine phosphate + H2O
[cytosolic 6-phosphofructokinase]-tyrosine + phosphate
-
-
-
?
[diguanylate cyclase TpbB]-tyrosine phosphate + H2O
[diguanylate cyclase TpbB]-tyrosine + phosphate
the substrate is involved in motility, biofilm formation
-
-
?
[diguanylate cyclase TpbB]-tyrosine phosphate + H2O
[diguanylate cyclase TpbB]-tyrosine + phosphate
the substrate is involved in motility, biofilm formation
-
-
?
[diguanylate cyclase TpbB]-tyrosine phosphate + H2O
[diguanylate cyclase TpbB]-tyrosine + phosphate
the substrate is involved in motility, biofilm formation
-
-
?
[diguanylate cyclase TpbB]-tyrosine phosphate + H2O
[diguanylate cyclase TpbB]-tyrosine + phosphate
the substrate is involved in motility, biofilm formation
-
-
?
[diguanylate cyclase TpbB]-tyrosine phosphate + H2O
[diguanylate cyclase TpbB]-tyrosine + phosphate
the substrate is involved in motility, biofilm formation
-
-
?
[diguanylate cyclase TpbB]-tyrosine phosphate + H2O
[diguanylate cyclase TpbB]-tyrosine + phosphate
the substrate is involved in motility, biofilm formation
-
-
?
[diguanylate cyclase TpbB]-tyrosine phosphate + H2O
[diguanylate cyclase TpbB]-tyrosine + phosphate
the substrate is involved in motility, biofilm formation
-
-
?
[diguanylate cyclase TpbB]-tyrosine phosphate + H2O
[diguanylate cyclase TpbB]-tyrosine + phosphate
the substrate is involved in motility, biofilm formation
-
-
?
[epidermal growth factor receptor]-tyrosine phosphate + H2O
[epidermal growth factor receptor]-tyrosine + phosphate
-
-
-
?
[epidermal growth factor receptor]-tyrosine phosphate + H2O
[epidermal growth factor receptor]-tyrosine + phosphate
-
-
-
?
[epidermal growth factor receptor]-tyrosine phosphate + H2O
[epidermal growth factor receptor]-tyrosine + phosphate
enzyme SP-PTP dephosphorylates the activated EGFR (170 kDa protein migrating at about 240 kDa) present in MDA-MB-231 cell lines
-
-
?
[epidermal growth factor receptor]-tyrosine phosphate + H2O
[epidermal growth factor receptor]-tyrosine + phosphate
-
-
-
?
[epidermal growth factor receptor]-tyrosine phosphate + H2O
[epidermal growth factor receptor]-tyrosine + phosphate
-
-
-
?
[Eps15 peptide846-854]-tyrosine phosphate + H2O
[Eps15 peptide846-854]-tyrosine + phosphate
-
-
-
?
[Eps15 peptide846-854]-tyrosine phosphate + H2O
[Eps15 peptide846-854]-tyrosine + phosphate
active with enzyme mutant F182H, wild-type shows poor activity
-
-
?
[Eps15 peptide]-tyrosine phosphate + H2O
[Eps15 peptide]-tyrosine + phosphate
substrate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for enzyme PTPN3
-
-
?
[Eps15 peptide]-tyrosine phosphate + H2O
[Eps15 peptide]-tyrosine + phosphate
substrate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for enzyme PTPN3
-
-
?
[Eps15 peptide]-tyrosine phosphate + H2O
[Eps15 peptide]-tyrosine + phosphate
substrate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for enzyme PTPN3. Pro850 of Eps15 and His812 of PTPN3 plays a central role in substrate specificity. E811 in WPE loop is unfavorable to act as a general acid during dephosphorylation. Critical role of the additional residue Tyr676 of PTPN3. The atypical binding conformation of Eps15 is mediated by its pTyr-Pro motif
-
-
?
[FHA-1]-tyrosine phosphate + H2O
[FHA-1]-tyrosine + phosphate
-
-
-
?
[FHA-1]-tyrosine phosphate + H2O
[FHA-1]-tyrosine + phosphate
-
-
-
?
[FHA-1]-tyrosine phosphate + H2O
[FHA-1]-tyrosine + phosphate
-
-
-
?
[FHA-1]-tyrosine phosphate + H2O
[FHA-1]-tyrosine + phosphate
-
-
-
?
[FHA-1]-tyrosine phosphate + H2O
[FHA-1]-tyrosine + phosphate
-
-
-
?
[FHA-1]-tyrosine phosphate + H2O
[FHA-1]-tyrosine + phosphate
-
-
-
?
[FHA-1]-tyrosine phosphate + H2O
[FHA-1]-tyrosine + phosphate
-
-
-
?
[FHA-1]-tyrosine phosphate + H2O
[FHA-1]-tyrosine + phosphate
-
-
-
?
[protein Golgi p230]-tyrosine phosphate + H2O
[protein Golgi p230]-tyrosine + phosphate
-
-
-
?
[protein Golgi p230]-tyrosine phosphate + H2O
[protein Golgi p230]-tyrosine + phosphate
-
-
-
?
[protein]-L-tyrosine phosphate + H2O
[protein]-L-tyrosine + phosphate
-
-
-
?
[protein]-L-tyrosine phosphate + H2O
[protein]-L-tyrosine + phosphate
-
-
-
?
[protein]-tyrosine phosphate + H2O
[protein]-tyrosine + phosphate
-
-
-
?
[protein]-tyrosine phosphate + H2O
[protein]-tyrosine + phosphate
-
-
-
?
[protein]-tyrosine phosphate + H2O
[protein]-tyrosine + phosphate
-
-
-
?
[protein]-tyrosine phosphate + H2O
[protein]-tyrosine + phosphate
-
-
-
?
[protein]-tyrosine phosphate + H2O
[protein]-tyrosine + phosphate
-
-
-
?
[protein]-tyrosine phosphate + H2O
[protein]-tyrosine + phosphate
-
-
-
?
[protein]-tyrosine phosphate + H2O
[protein]-tyrosine + phosphate
-
-
-
?
[protein]-tyrosine phosphate + H2O
[protein]-tyrosine + phosphate
-
-
-
?
[sulfide quinone oxidoreductase]-tyrosine phosphate + H2O
[sulfide quinone oxidoreductase]-tyrosine + phosphate
-
-
-
?
[sulfide quinone oxidoreductase]-tyrosine phosphate + H2O
[sulfide quinone oxidoreductase]-tyrosine + phosphate
-
-
-
?
[sulfide quinone oxidoreductase]-tyrosine phosphate + H2O
[sulfide quinone oxidoreductase]-tyrosine + phosphate
-
-
-
?
[trifunctional enzyme]-tyrosine phosphate + H2O
[trifunctional enzyme]-tyrosine + phosphate
-
-
-
?
[trifunctional enzyme]-tyrosine phosphate + H2O
[trifunctional enzyme]-tyrosine + phosphate
also dephosphorylates the human trifunctional enzyme
-
-
?
[trifunctional enzyme]-tyrosine phosphate + H2O
[trifunctional enzyme]-tyrosine + phosphate
-
-
-
?
[trifunctional enzyme]-tyrosine phosphate + H2O
[trifunctional enzyme]-tyrosine + phosphate
-
-
-
?
additional information
?
-
-
PTP is an element of the abscisic acid signaling pathway that leads to stomatal closure
-
-
?
additional information
?
-
-
no substrate: phosphoeptides RRA(pS)VA, KR(pT)IRR
-
-
?
additional information
?
-
the enzyme does not display catalytic activity against some common protein tyrosine phosphatase substrates (O-nitrophenyl beta-D-galactopyranoside, O-phospho-L-threonine, D-fructose 6-phosphate, D-ribose 5-phosphate, D-glucose 6-phosphate, D-glucose 1-phosphate) but is highly specific for hydrolysis of phosphomonoester bonds of inositol hexakisphosphate
-
-
?
additional information
?
-
-
the enzyme does not display catalytic activity against some common protein tyrosine phosphatase substrates (O-nitrophenyl beta-D-galactopyranoside, O-phospho-L-threonine, D-fructose 6-phosphate, D-ribose 5-phosphate, D-glucose 6-phosphate, D-glucose 1-phosphate) but is highly specific for hydrolysis of phosphomonoester bonds of inositol hexakisphosphate
-
-
?
additional information
?
-
the enzyme does not display catalytic activity against some common protein tyrosine phosphatase substrates (O-nitrophenyl beta-D-galactopyranoside, O-phospho-L-threonine, D-fructose 6-phosphate, D-ribose 5-phosphate, D-glucose 6-phosphate, D-glucose 1-phosphate) but is highly specific for hydrolysis of phosphomonoester bonds of inositol hexakisphosphate
-
-
?
additional information
?
-
Bracoviriform demolitoris
-
PTP-H2 functions as an inhibitor of phagocytosis, PTP-H2 mediates cell death of infected Sf-21 cells, expression of PTP-H2 triggers mitochondrial membrane depolarisation and caspase-dependent apoptosis
-
-
?
additional information
?
-
Bracoviriform demolitoris
-
no activity with DADEpYLIPQQG, poor activity with 4-nitrophenyl phosphate
-
-
?
additional information
?
-
-
STATc becomes tyrosine phosphorylated and accumulates in the nucleus when Dictyostelium cells are exposed to the prestalk cell inducer Differentiation inducing factor 1, DIF-1, or are subjected to hyperosmotic stress
-
-
?
additional information
?
-
the enzyme is a dual-specificity Ser/Thr/Tyr phosphatase also exhibiting the activity of EC 3.1.3.16
-
-
?
additional information
?
-
-
no hydrolysis of serine phosphate, threonine phosphate, nicotinamide adenine dinucleotide phosphate
-
-
?
additional information
?
-
-
kinetic constants for several peptide substrates
-
?
additional information
?
-
study on substrate specificity
-
?
additional information
?
-
-
study on substrate specificity, screen of peptide substrate library
-
?
additional information
?
-
-
PTPases regulate the ligand-induced autophosphorylation of PTK growth factor receptors, the phosphotyrosine-mediated binding s of src homology 2 (SH2)-domain-containing proteins to autophosphorylated PTK growth factor receptors and the activation state of the src family pf PTK
-
-
?
additional information
?
-
-
LMW-PTP is involved in the negative regulation of the mitogenic stimulus starting from the activated PDGF receptor. The interaction between LMW-PTP results in the dephosphorylation of the PDGF-R phosphortyrosine and a negative regulation of the mitogenic signal
-
-
?
additional information
?
-
-
regulation of the function of epidermal growth factor receptor in keratinocytes by its dephosphorylation
-
-
?
additional information
?
-
-
SHP-1 may regulate the tethering of receptors to the cytoskeleton and/or the extent of cross-linking of actin filaments in platelets
-
-
?
additional information
?
-
-
Cdc25 phosphatases prefer a bisanionic over a monoanionic substrate
-
-
?
additional information
?
-
-
no activity on phosphothreonine substrates
-
-
?
additional information
?
-
-
activation of SPH-1 and SPH-2 is accompanied by reduced responsiveness to aggregating agents, phosphorylation of SPH-1 and SPH-2 introduces docking sites for adaptor molecules like growth factor receptor-bound protein 2 regulating further signaling to integrin alphaIIbbeta3
-
-
?
additional information
?
-
-
by modulating Src-focal adhesion kinase signaling at adhesion sites, PTPD1 promotes the cytoskeleton events that induce cell adhesion and migration
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additional information
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functional inactivation of the protein tyrosine phosphatase DEP-1 leads to increased endothelial cell proliferation and failure of vessels to remodel and branch
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additional information
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human LMW-PTP is critical in the regulation of mitogenic signalling and Rho-mediated cytoskeletal rearrangements after platelet derived growth factor stimulation
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additional information
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SHP-2, MKP-1, LAR, and PTEN are targets of platelet-derived growth factor-induced reversible oxidation
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additional information
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DEP-1 is a positive regulator of VEGF-mediated Src and Akt activation and endothelial cell survival
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additional information
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ED-Eya2 is bifunctional acting as protein tyrosine phosphatase and as transcription factor. The transcriptional activity of Eya proteins is regulated by a dephosphorylating activity within its Eya domain, structure-function analysis, overview
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additional information
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ED-Eya2 is bifunctional acting as protein tyrosine phosphatase and as transcription factor. The transcriptional activity of Eya proteins is regulated by a dephosphorylating activity within its Eya domain, structure-function analysis, overview
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additional information
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isozyme p52shc associates with the growth factor receptor-bound protein-2, Grb2. Overexpression of isozyme p66shc impaires IGF-I-stimulated p52shc tyrosine phosphorylation and p52shc-Grb2 association. Isozyme p66shc inhibits IGF-I signal transduction via competitively inhibiting the binding of Src homology 2 domain-containing SHP-2 to SHP substrate-1, leading to the disruption of SHPS-1/SHP-2/Src/p52shc complex formation, an event that is essential for p52shc phosphorylation and Grb2 recruitment, overview. p66shc inhibits IGF-I signal transduction via impairing membrane recruitment of Grb2
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additional information
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protein tyrosine phosphatase 1B, PTP1B, is an intracellular non-receptor type PTP
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additional information
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formation and structure of a transition state analogue for the first catalytic step comprising a ternary complex between the catalytic cysteine of PTP1B, vanadate, and the peptide DADEYL, a fragment of a physiological substrate, overview. The equatorial vanadate oxygen atoms bind to the P-loop, and the apical positions are occupied by the peptide tyrosine oxygen and by the PTP1B cysteine sulfur atom. The vanadate assumes a trigonal bipyramidal geometry in both transition state analogue structures, with very similar apical O-O distances, denoting similar transition states for both phosphoryl transfer steps
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additional information
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PTEN phosphoprotein phosphatase catalysis of phosphoprotein dephosphorylation follows a two-step mechanism with Cys124 transiently phosphorylated to form the phosphoenzyme intermediate
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additional information
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Ser380, Thr382 and Thr383 C-terminal tail residues do not affect the recruitment of the WPD-loop into the active site to participate in the phosphoprotein dephosphorylation reaction, catalytic mechanism of PTEN phosphoprotein phosphatase activity, overview. The phosphoPTEN protein is not the cysteinyl phosphoenzyme intermediate formed by transient phosphorylation of Cys124 in the course of phosphopeptide dephosphorylation reaction. PTEN can adopt the closed conformation to allow Asp92 to participate in catalysis when it dephosphorylates the physiological protein substrates such as FAK and Shc in cells
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additional information
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substrate specificity analysis using a trapping mutant of the phosphatase, which is a point mutation that maintains specificity but does not allow detachment of the phosphate, overview. The enzyme is also active on 4-nitrophenyl phosphate, but is not active on GRB2
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additional information
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substrate specificity of lymphoid-specific tyrosine phosphatase, identification of consensus sequence motifs for Lyp substrate recognition using an inverse alanine scanning combinatorial library approach, molecular determinants and molecular basis for Lyp substrate recognition, crystal structure analysis, overview
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additional information
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the PTP1B catalytic domain has modest preference for acidic residues on both sides of phosphotyrosine, is highly active toward multiply phosphorylated peptides, but disfavors basic residues at any position, a Gly at the phosphotyrosine-1 position, or a Pro at the pY-/-1 position. By contrast, SHP-1 and SHP-2 share similar but much narrower substrate specificities, with a strong preference for acidic and aromatic hydrophobic amino acids on both sides of the phosphotyrosine residue. An efficient SHP-1/2 substrate generally contains two or more acidic residues on the N-terminal side and one or more acidic residues on the C-terminal side of pY but no basic residues, substrate specificities of the protein tyrosine phosphatases PTP1B, RPTPalpha, SHP-1, and SHP-2, and reported PTP1B, SHP-1, and SHP-2 substrates and their dephosphorylation sites, overview. The catalytic domain of RPTPalpha has very weak sequence specificity and is approximately 2 orders of magnitude less active than the other three enzyme variants
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additional information
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does not dephosphorylate c-Abl
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additional information
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does not dephosphorylate c-Abl
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additional information
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PTP1B exhibits higher affinity (about 70fold) for tandem phosphotyrosine-containing peptides compared with mono-phosphotyrosine derivatives
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additional information
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activity detection by malachite green phosphatase method for phosphate determination
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additional information
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activity detection by malachite green phosphatase method for phosphate determination
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additional information
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development and optimization of non-radiometric immunoassays for the efficient detection of IA-2 autoantibodies (IA-2A)
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additional information
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human protein VHR is a dual specificity protein phosphatase 3, that also exhibits serine/threonine phosphatase activity, EC 3.1.3.16
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additional information
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human protein VHR is a dual specificity protein phosphatase 3, that also exhibits serine/threonine phosphatase activity, EC 3.1.3.16
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additional information
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human protein VHR is a dual specificity protein phosphatase 3, that also exhibits serine/threonine phosphatase activity, EC 3.1.3.16
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additional information
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PTP1B is a classical PTP with a deep active site pocket suited for phosphotyrosine, that also efficiently hydrolyzes other phosphorylated phenols
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additional information
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PTP1B is a classical PTP with a deep active site pocket suited for phosphotyrosine, that also efficiently hydrolyzes other phosphorylated phenols
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additional information
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PTP1B is a classical PTP with a deep active site pocket suited for phosphotyrosine, that also efficiently hydrolyzes other phosphorylated phenols
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additional information
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receptor protein tyrosine phosphatase isoform delta (PTPRdelta) displays substrate promiscuity by hydrolyzing the diester bond while showing a high-level of discrimination in its primary monoesterase substrate preference. The phosphatase domain of receptor protein tyrosine phosphatases catalyzes the hydrolysis of glycosidic (COC) bonds apart from its primary activity of cleaving phosphomonoester (COP) bond. This is important because the hydrolysis of COC bond in beta-galactosides and COP bond in phosphomonoesters require different functional groups and different mechanism of cleavage. No activity with adenosine monophosphate, inosine monophosphate, guanosine monophosphate, nicotinamide adenine dinucleotide phosphate, and pyridoxal 5'-phosphate, also no activity with tris-(4-nitrophenyl) phosphate, tris-(4-nitrobenzyl) phosphate, tetrakis-(4-nitrophenyl) diphosphate, NADP+, and peptide H-Gly-PNA. The enzyme shows low activity with several nitrophenyl glycosides cleaving the glycosidic bond. Substrate specificity, overview. No phosphocysteinyl hydrolysis of isozyme PTPRdelta
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additional information
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receptor protein tyrosine phosphatase isoform delta (PTPRdelta) displays substrate promiscuity by hydrolyzing the diester bond while showing a high-level of discrimination in its primary monoesterase substrate preference. The phosphatase domain of receptor protein tyrosine phosphatases catalyzes the hydrolysis of glycosidic (COC) bonds apart from its primary activity of cleaving phosphomonoester (COP) bond. This is important because the hydrolysis of COC bond in beta-galactosides and COP bond in phosphomonoesters require different functional groups and different mechanism of cleavage. No activity with adenosine monophosphate, inosine monophosphate, guanosine monophosphate, nicotinamide adenine dinucleotide phosphate, and pyridoxal 5'-phosphate, also no activity with tris-(4-nitrophenyl) phosphate, tris-(4-nitrobenzyl) phosphate, tetrakis-(4-nitrophenyl) diphosphate, NADP+, and peptide H-Gly-PNA. The enzyme shows low activity with several nitrophenyl glycosides cleaving the glycosidic bond. Substrate specificity, overview. No phosphocysteinyl hydrolysis of isozyme PTPRdelta
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additional information
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receptor protein tyrosine phosphatase isoform delta (PTPRdelta) shows catalytic and substrate promiscuity. The phosphatase domain of receptor protein tyrosine phosphatases catalyzes the hydrolysis of glycosidic (COC) bonds apart from its primary activity of cleaving phosphomonoester (COP) bond. This is important because the hydrolysis of COC bond in beta-galactosides and COP bond in phosphomonoesters require different functional groups and different mechanism of cleavage. No activity with adenosine monophosphate, inosine monophosphate, guanosine monophosphate, nicotinamide adenine dinucleotide phosphate, and pyridoxal 5'-phosphate, also no activity with tris-(4-nitrophenyl) phosphate, tris-(4-nitrobenzyl) phosphate, tetrakis-(4-nitrophenyl) diphosphate, NADP+, and peptide H-Gly-PNA. The enzyme shows low activity with several nitrophenyl glycosides cleaving the glycosidic bond. Substrate specificity, overview. Isozyme PD-PTPRomega shows rate-limiting phosphocysteinyl hydrolysis leading to a biphasic time-dependence of substrate to product conversion
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additional information
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receptor protein tyrosine phosphatase isoform delta (PTPRdelta) shows catalytic and substrate promiscuity. The phosphatase domain of receptor protein tyrosine phosphatases catalyzes the hydrolysis of glycosidic (COC) bonds apart from its primary activity of cleaving phosphomonoester (COP) bond. This is important because the hydrolysis of COC bond in beta-galactosides and COP bond in phosphomonoesters require different functional groups and different mechanism of cleavage. No activity with adenosine monophosphate, inosine monophosphate, guanosine monophosphate, nicotinamide adenine dinucleotide phosphate, and pyridoxal 5'-phosphate, also no activity with tris-(4-nitrophenyl) phosphate, tris-(4-nitrobenzyl) phosphate, tetrakis-(4-nitrophenyl) diphosphate, NADP+, and peptide H-Gly-PNA. The enzyme shows low activity with several nitrophenyl glycosides cleaving the glycosidic bond. Substrate specificity, overview. Isozyme PD-PTPRomega shows rate-limiting phosphocysteinyl hydrolysis leading to a biphasic time-dependence of substrate to product conversion
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additional information
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the [Eps15 peptide]-tyrosine phosphate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for PTP enzyme PTPN3. A conserved aspartic acid, which functions as a general acid for nucleophilic attack on the substrate in the first step of catalysis, must appear in the WPD loop among active PTPs, except for enzyme PTPN21, this critical residue in PTPN21 is substituted with a glutamic acid, thus resulting in a WPE loop instead. Enzyme PTPN21 shows no activity with 4-nitrophenyl phosphate or Eps15846-854 peptide as substrate in the phosphatase activity assay. Once the glutamic acid in the WPE loop is replaced by an aspartic acid, the E1067D mutant form of PTPN21PTP exhibits a significantly higher level of phosphatase activity compared with its wild-type counterpart
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additional information
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the [Eps15 peptide]-tyrosine phosphate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for PTP enzyme PTPN3. A conserved aspartic acid, which functions as a general acid for nucleophilic attack on the substrate in the first step of catalysis, must appear in the WPD loop among active PTPs, except for enzyme PTPN21, this critical residue in PTPN21 is substituted with a glutamic acid, thus resulting in a WPE loop instead. Enzyme PTPN21 shows no activity with 4-nitrophenyl phosphate or Eps15846-854 peptide as substrate in the phosphatase activity assay. Once the glutamic acid in the WPE loop is replaced by an aspartic acid, the E1067D mutant form of PTPN21PTP exhibits a significantly higher level of phosphatase activity compared with its wild-type counterpart
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additional information
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the [Eps15 peptide]-tyrosine phosphate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for PTP enzyme PTPN3. A conserved aspartic acid, which functions as a general acid for nucleophilic attack on the substrate in the first step of catalysis, must appear in the WPD loop among active PTPs, except for enzyme PTPN21, this critical residue in PTPN21 is substituted with a glutamic acid, thus resulting in a WPE loop instead. Enzyme PTPN21 shows no activity with 4-nitrophenyl phosphate or Eps15846-854 peptide as substrate in the phosphatase activity assay. Once the glutamic acid in the WPE loop is replaced by an aspartic acid, the E1067D mutant form of PTPN21PTP exhibits a significantly higher level of phosphatase activity compared with its wild-type counterpart
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additional information
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the [Eps15 peptide]-tyrosine phosphate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for PTP enzyme PTPN3. A conserved aspartic acid, which functions as a general acid for nucleophilic attack on the substrate in the first step of catalysis, must appear in the WPD loop among active PTPs, except for enzyme PTPN21, this critical residue in PTPN21 is substituted with a glutamic acid, thus resulting in a WPE loop instead. Enzyme PTPN21 shows no activity with 4-nitrophenyl phosphate or Eps15846-854 peptide as substrate in the phosphatase activity assay. Once the glutamic acid in the WPE loop is replaced by an aspartic acid, the E1067D mutant form of PTPN21PTP exhibits a significantly higher level of phosphatase activity compared with its wild-type counterpart
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additional information
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the [Eps15 peptide]-tyrosine phosphate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for PTP enzyme PTPN3. A conserved aspartic acid, which functions as a general acid for nucleophilic attack on the substrate in the first step of catalysis, must appear in the WPD loop among active PTPs, except for enzyme PTPN21, this critical residue in PTPN21 is substituted with a glutamic acid, thus resulting in a WPE loop instead. Enzyme PTPN21 shows no activity with 4-nitrophenyl phosphate or Eps15846-854 peptide as substrate in the phosphatase activity assay. Once the glutamic acid in the WPE loop is replaced by an aspartic acid, the E1067D mutant form of PTPN21PTP exhibits a significantly higher level of phosphatase activity compared with its wild-type counterpart
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additional information
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the [Eps15 peptide]-tyrosine phosphate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for PTP enzyme PTPN3. Analysis of enzymes PTPN13 and PTPN14 within the FERM domain-containing PTP subfamily, overview. The catalytic domain of enzyme PTP1B cannot dephosphorylate Eps15846-854 or Eps15836-858 efficiently compared with wild-type PTPN3, supporting a critical role of H812 in recognition of Eps15. The position of H812 in PTPN3 is a phenylalanine (F182) in PTP1B, His812 of PTPN3 plays a central role in substrate specificity. Enzyme PTPN13 binds to Eps15846-854 more strongly largely because of the unique H2379 responsible for substrate recognition. The other difference is an aspartic acid (D2380) in PTPN13 instead of a glycine residue in PTPN3 inside the WPD loop. The presence of an additional aspartic acid suggests that the side chain of H2379 in PTPN13 might interact with the side chains of D2378 and D2380. Such interaction likely causes a perturbation of H2379, rendering this particular residue unable to form a stable stacked-like contact to Eps15846-854, wild-type PTPN13 shows a 3fold increase in Km compared with PTPN3
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additional information
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the [Eps15 peptide]-tyrosine phosphate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for PTP enzyme PTPN3. Analysis of enzymes PTPN13 and PTPN14 within the FERM domain-containing PTP subfamily, overview. The catalytic domain of enzyme PTP1B cannot dephosphorylate Eps15846-854 or Eps15836-858 efficiently compared with wild-type PTPN3, supporting a critical role of H812 in recognition of Eps15. The position of H812 in PTPN3 is a phenylalanine (F182) in PTP1B, His812 of PTPN3 plays a central role in substrate specificity. Enzyme PTPN13 binds to Eps15846-854 more strongly largely because of the unique H2379 responsible for substrate recognition. The other difference is an aspartic acid (D2380) in PTPN13 instead of a glycine residue in PTPN3 inside the WPD loop. The presence of an additional aspartic acid suggests that the side chain of H2379 in PTPN13 might interact with the side chains of D2378 and D2380. Such interaction likely causes a perturbation of H2379, rendering this particular residue unable to form a stable stacked-like contact to Eps15846-854, wild-type PTPN13 shows a 3fold increase in Km compared with PTPN3
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additional information
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the [Eps15 peptide]-tyrosine phosphate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for PTP enzyme PTPN3. Analysis of enzymes PTPN13 and PTPN14 within the FERM domain-containing PTP subfamily, overview. The catalytic domain of enzyme PTP1B cannot dephosphorylate Eps15846-854 or Eps15836-858 efficiently compared with wild-type PTPN3, supporting a critical role of H812 in recognition of Eps15. The position of H812 in PTPN3 is a phenylalanine (F182) in PTP1B, His812 of PTPN3 plays a central role in substrate specificity. Enzyme PTPN13 binds to Eps15846-854 more strongly largely because of the unique H2379 responsible for substrate recognition. The other difference is an aspartic acid (D2380) in PTPN13 instead of a glycine residue in PTPN3 inside the WPD loop. The presence of an additional aspartic acid suggests that the side chain of H2379 in PTPN13 might interact with the side chains of D2378 and D2380. Such interaction likely causes a perturbation of H2379, rendering this particular residue unable to form a stable stacked-like contact to Eps15846-854, wild-type PTPN13 shows a 3fold increase in Km compared with PTPN3
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additional information
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the [Eps15 peptide]-tyrosine phosphate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for PTP enzyme PTPN3. Analysis of enzymes PTPN13 and PTPN14 within the FERM domain-containing PTP subfamily, overview. The catalytic domain of enzyme PTP1B cannot dephosphorylate Eps15846-854 or Eps15836-858 efficiently compared with wild-type PTPN3, supporting a critical role of H812 in recognition of Eps15. The position of H812 in PTPN3 is a phenylalanine (F182) in PTP1B, His812 of PTPN3 plays a central role in substrate specificity. Enzyme PTPN13 binds to Eps15846-854 more strongly largely because of the unique H2379 responsible for substrate recognition. The other difference is an aspartic acid (D2380) in PTPN13 instead of a glycine residue in PTPN3 inside the WPD loop. The presence of an additional aspartic acid suggests that the side chain of H2379 in PTPN13 might interact with the side chains of D2378 and D2380. Such interaction likely causes a perturbation of H2379, rendering this particular residue unable to form a stable stacked-like contact to Eps15846-854, wild-type PTPN13 shows a 3fold increase in Km compared with PTPN3
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additional information
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the [Eps15 peptide]-tyrosine phosphate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for PTP enzyme PTPN3. Analysis of enzymes PTPN13 and PTPN14 within the FERM domain-containing PTP subfamily, overview. The catalytic domain of enzyme PTP1B cannot dephosphorylate Eps15846-854 or Eps15836-858 efficiently compared with wild-type PTPN3, supporting a critical role of H812 in recognition of Eps15. The position of H812 in PTPN3 is a phenylalanine (F182) in PTP1B, His812 of PTPN3 plays a central role in substrate specificity. Enzyme PTPN13 binds to Eps15846-854 more strongly largely because of the unique H2379 responsible for substrate recognition. The other difference is an aspartic acid (D2380) in PTPN13 instead of a glycine residue in PTPN3 inside the WPD loop. The presence of an additional aspartic acid suggests that the side chain of H2379 in PTPN13 might interact with the side chains of D2378 and D2380. Such interaction likely causes a perturbation of H2379, rendering this particular residue unable to form a stable stacked-like contact to Eps15846-854, wild-type PTPN13 shows a 3fold increase in Km compared with PTPN3
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additional information
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the [Eps15 peptide]-tyrosine phosphate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for PTP enzyme PTPN3. Analysis of enzymes PTPN13 and PTPN14 within the FERM domain-containing PTP subfamily, overview. The catalytic domain of enzyme PTP1B cannot dephosphorylate Eps15846-854 or Eps15836-858 efficiently compared with wild-type PTPN3, supporting a critical role of H812 in recognition of Eps15. The position of H812 in PTPN3 is a phenylalanine (F182) in PTP1B, His812 of PTPN3 plays a central role in substrate specificity. Enzyme PTPN14 shows a substitution of tyrosine in the pY loop with an isoleucin. The wild-type PTPN14PTP is catalytically inactive when four structurally characterized phosphopeptides are used as the substrate in the assay
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additional information
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the [Eps15 peptide]-tyrosine phosphate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for PTP enzyme PTPN3. Analysis of enzymes PTPN13 and PTPN14 within the FERM domain-containing PTP subfamily, overview. The catalytic domain of enzyme PTP1B cannot dephosphorylate Eps15846-854 or Eps15836-858 efficiently compared with wild-type PTPN3, supporting a critical role of H812 in recognition of Eps15. The position of H812 in PTPN3 is a phenylalanine (F182) in PTP1B, His812 of PTPN3 plays a central role in substrate specificity. Enzyme PTPN14 shows a substitution of tyrosine in the pY loop with an isoleucin. The wild-type PTPN14PTP is catalytically inactive when four structurally characterized phosphopeptides are used as the substrate in the assay
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additional information
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the [Eps15 peptide]-tyrosine phosphate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for PTP enzyme PTPN3. Analysis of enzymes PTPN13 and PTPN14 within the FERM domain-containing PTP subfamily, overview. The catalytic domain of enzyme PTP1B cannot dephosphorylate Eps15846-854 or Eps15836-858 efficiently compared with wild-type PTPN3, supporting a critical role of H812 in recognition of Eps15. The position of H812 in PTPN3 is a phenylalanine (F182) in PTP1B, His812 of PTPN3 plays a central role in substrate specificity. Enzyme PTPN14 shows a substitution of tyrosine in the pY loop with an isoleucin. The wild-type PTPN14PTP is catalytically inactive when four structurally characterized phosphopeptides are used as the substrate in the assay
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additional information
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the [Eps15 peptide]-tyrosine phosphate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for PTP enzyme PTPN3. Analysis of enzymes PTPN13 and PTPN14 within the FERM domain-containing PTP subfamily, overview. The catalytic domain of enzyme PTP1B cannot dephosphorylate Eps15846-854 or Eps15836-858 efficiently compared with wild-type PTPN3, supporting a critical role of H812 in recognition of Eps15. The position of H812 in PTPN3 is a phenylalanine (F182) in PTP1B, His812 of PTPN3 plays a central role in substrate specificity. Enzyme PTPN14 shows a substitution of tyrosine in the pY loop with an isoleucin. The wild-type PTPN14PTP is catalytically inactive when four structurally characterized phosphopeptides are used as the substrate in the assay
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additional information
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the [Eps15 peptide]-tyrosine phosphate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for PTP enzyme PTPN3. Analysis of enzymes PTPN13 and PTPN14 within the FERM domain-containing PTP subfamily, overview. The catalytic domain of enzyme PTP1B cannot dephosphorylate Eps15846-854 or Eps15836-858 efficiently compared with wild-type PTPN3, supporting a critical role of H812 in recognition of Eps15. The position of H812 in PTPN3 is a phenylalanine (F182) in PTP1B, His812 of PTPN3 plays a central role in substrate specificity. Enzyme PTPN14 shows a substitution of tyrosine in the pY loop with an isoleucin. The wild-type PTPN14PTP is catalytically inactive when four structurally characterized phosphopeptides are used as the substrate in the assay
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additional information
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the [Eps15 peptide]-tyrosine phosphate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for PTP enzyme PTPN3. The catalytic domain of PTP1B cannot dephosphorylate Eps15846-854 or Eps15836-858 efficiently compared with wild-type N3PTP, supporting a critical role of H812 in recognition of Eps15. The position of H812 in PTPN3 is a phenylalanine (F182) in PTP1B, His812 of PTPN3 plays a central role in substrate specificity
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additional information
?
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the [Eps15 peptide]-tyrosine phosphate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for PTP enzyme PTPN3. The catalytic domain of PTP1B cannot dephosphorylate Eps15846-854 or Eps15836-858 efficiently compared with wild-type N3PTP, supporting a critical role of H812 in recognition of Eps15. The position of H812 in PTPN3 is a phenylalanine (F182) in PTP1B, His812 of PTPN3 plays a central role in substrate specificity
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additional information
?
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the [Eps15 peptide]-tyrosine phosphate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for PTP enzyme PTPN3. The catalytic domain of PTP1B cannot dephosphorylate Eps15846-854 or Eps15836-858 efficiently compared with wild-type N3PTP, supporting a critical role of H812 in recognition of Eps15. The position of H812 in PTPN3 is a phenylalanine (F182) in PTP1B, His812 of PTPN3 plays a central role in substrate specificity
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additional information
?
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the [Eps15 peptide]-tyrosine phosphate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for PTP enzyme PTPN3. The catalytic domain of PTP1B cannot dephosphorylate Eps15846-854 or Eps15836-858 efficiently compared with wild-type N3PTP, supporting a critical role of H812 in recognition of Eps15. The position of H812 in PTPN3 is a phenylalanine (F182) in PTP1B, His812 of PTPN3 plays a central role in substrate specificity
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additional information
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the [Eps15 peptide]-tyrosine phosphate is a phosphopeptide fragment of substrate epidermal growth factor receptor. Eps15 is a scaffolding adaptor that regulates endocytosis and trafficking of the EGFR and is a substrate for PTP enzyme PTPN3. The catalytic domain of PTP1B cannot dephosphorylate Eps15846-854 or Eps15836-858 efficiently compared with wild-type N3PTP, supporting a critical role of H812 in recognition of Eps15. The position of H812 in PTPN3 is a phenylalanine (F182) in PTP1B, His812 of PTPN3 plays a central role in substrate specificity
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additional information
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VHZ is an atypical PTP, with the deep active site of classical PTPs but several structural differences, including an immobile loop bearing the general acid
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additional information
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VHZ is an atypical PTP, with the deep active site of classical PTPs but several structural differences, including an immobile loop bearing the general acid
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additional information
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VHZ is an atypical PTP, with the deep active site of classical PTPs but several structural differences, including an immobile loop bearing the general acid
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additional information
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strict specificity of Spd1837 for phosphotyrosine residues
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additional information
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strict specificity of Spd1837 for phosphotyrosine residues
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additional information
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strict specificity of Spd1837 for phosphotyrosine residues
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additional information
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physiological substrates, overview
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additional information
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possible specific substrate is p190Rho-GAP
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additional information
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no activity against phytic acid, ADP, AMP, O-phospho-L-serine or O-phospho-L-threonine
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additional information
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substrate specificity evaluation, the purified recombinant enzyme exhibits high activity on O-phospho-L-tyrosine
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additional information
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substrate specificity evaluation, the purified recombinant enzyme exhibits high activity on O-phospho-L-tyrosine
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additional information
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no activity against phytic acid, ADP, AMP, O-phospho-L-serine or O-phospho-L-threonine
-
-
?
additional information
?
-
substrate specificity evaluation, the purified recombinant enzyme exhibits high activity on O-phospho-L-tyrosine
-
-
?
additional information
?
-
the isoforms of PRP36 may function as adapter molecules rather than as a phosphatase
-
-
?
additional information
?
-
-
protein tyrosine phosphatase alpha regulates the activity of raft Fyn
-
-
?
additional information
?
-
-
N-cadherin, VE-cadherin, desmoglein, alpha-catenin, beta-catenin, gamma-catenin, and alpha-actinin are not dephosphorylated by RPTPrho
-
-
?
additional information
?
-
-
PTP-PEST most likely also participates in regulating osteoclast differentiation and adhesion to bone matrix
-
-
?
additional information
?
-
-
PTPalpha is required for stem cell factor-stimulated Src family kinase activation and signaling, and for mast cell migration
-
-
?
additional information
?
-
-
SHP-1 is a negative regulator of osteoclastogenic signalling
-
-
?
additional information
?
-
-
phospho-p38 mitogen-activated protein kinase and Akt are not dephosphorylated
-
-
?
additional information
?
-
-
HePTP plays a role in regulating the level of p38 MAPK phosphorylation in B-lymphocytes, HePTP can be phosphorylated by PKA, which inactivates the phosphatase and causes it to release p38 MAPK into the cytoplasm
-
-
?
additional information
?
-
-
PTPN4 does not dephosphorylate Lck at tyrosine residue 394
-
-
?
additional information
?
-
in vivo phagocytosis assay and in vivo microglial migration assay, overview
-
-
?
additional information
?
-
enzyme additionally catalyzes the hydrolysis of 2-phosphoglycolate, reaction of EC 3.1.3.18
-
-
?
additional information
?
-
PTP1 is a classical PTP with a deep active site pocket suited for phosphotyrosine, that also efficiently hydrolyzes other phosphorylated phenols
-
-
?
additional information
?
-
-
N-cadherin, VE-cadherin, desmoglein, alpha-catenin, beta-catenin, gamma-catenin, and alpha-actinin are not dephosphorylated by RPTPrho
-
-
?
additional information
?
-
in vivo phagocytosis assay and in vivo microglial migration assay, overview
-
-
?
additional information
?
-
-
both isozymes act only on phosphotyrosine residues
-
?
additional information
?
-
-
little or no effect on the residues of phosphoserine or phosphothreonine
-
-
?
additional information
?
-
-
inactive towards phosphoseryl histone
-
-
?
additional information
?
-
-
acts specifically on phosphorylated tyrosine
-
?
additional information
?
-
-
protein-tyrosine phosphatases are signaling molecules that are involved in numerous cellular mechanisms such as cell growth and proliferation, cell cycle regulation, and cytoskeletal integrity
-
-
?
additional information
?
-
-
LAR, PTPalpha and PTP1B may act upon cell surface insulin receptors
-
?
additional information
?
-
-
enzyme activity is correlated with sperm thiol status and tyrosine phosphorylation of sperm proteins during maturation is promoted by thiol oxidation and diminished enzyme
-
-
?
additional information
?
-
-
enzyme isoform Shp2 is required for complete activation of mitogen-activated protein kinases MAPKs by brain-derived neurotropic factor
-
-
?
additional information
?
-
-
phosphoserine and phosphothreonine are no substrates
-
-
?
additional information
?
-
the enzyme shows high activity and exquisite specificity for the 5-diphosphate group of inositol diphosphates (5-PP-InsP), substrate-binding pocket structure analysis, overview. Enzyme Siw14 also acts as a 5-PP-InsP phosphatase, EC 3.1.3.56 (inositol-polyphosphate 5-phosphatase)
-
-
?
additional information
?
-
-
the enzyme shows high activity and exquisite specificity for the 5-diphosphate group of inositol diphosphates (5-PP-InsP), substrate-binding pocket structure analysis, overview. Enzyme Siw14 also acts as a 5-PP-InsP phosphatase, EC 3.1.3.56 (inositol-polyphosphate 5-phosphatase)
-
-
?
additional information
?
-
the enzyme shows high activity and exquisite specificity for the 5-diphosphate group of inositol diphosphates (5-PP-InsP), substrate-binding pocket structure analysis, overview. Enzyme Siw14 also acts as a 5-PP-InsP phosphatase, EC 3.1.3.56 (inositol-polyphosphate 5-phosphatase)
-
-
?
additional information
?
-
Stp1 is a low molecular weight cytosolic acid phosphatase or phosphotyrosine protein phosphatase
-
-
?
additional information
?
-
Stp1 is a low molecular weight cytosolic acid phosphatase or phosphotyrosine protein phosphatase
-
-
?
additional information
?
-
-
substrate specificity of enzyme PRL, overview. The enzyme also hydrolyzes adenosine diphosphate, fructose 6-phosphate, sodium alpha-naphthyl phosphate, and phosphoenol pyruvate
-
-
?
additional information
?
-
-
PtpA, PtpB act specifically on phosphotyrosine residues
-
?
additional information
?
-
Spd1837 has activity against two phosphotyrosine-containing peptides, phosphopeptide-1 (END(pY)INASL) and phosphopeptide-2 (DADE(pY)LIPQQG), as the mutant protein Spd1837C8S lacks activity against these two phosphotyrosine-containing phosphopeptides
-
-
?
additional information
?
-
Spd1837 has activity against two phosphotyrosine-containing peptides, phosphopeptide-1 (END(pY)INASL) and phosphopeptide-2 (DADE(pY)LIPQQG), as the mutant protein Spd1837C8S lacks activity against these two phosphotyrosine-containing phosphopeptides
-
-
?
additional information
?
-
enzyme SP-PTP does not dephosphorylate the C-terminal fragment of EGFR with intact catalytic domain in vitro. SP-PTP possesses a tyrosine phosphatase activity that varies based on the type of substrates and reaction conditions. Enzyme SP-PTP also possesses Ser/Thr phosphatase activity dephosphorylating the autophosphorylated SP-STKK, i.e. the kinase domain of kinase SP-STK
-
-
?
additional information
?
-
enzyme SP-PTP shares high similarity with typical low molecular weight protein tyrosine phosphatases (LMWPTPs), which are specific for phosphotyrosine, but not with dual-specificity phosphatases, in overall folding and active site composition. In the dephosphorylation activity test, SP-PTP consistently acts on phosphotyrosine substrates, but not or only minimally on phosphoserine/phosphothreonine substrates. PTP as a canonical tyrosine-specific LMWPTP
-
-
?
additional information
?
-
enzyme SP-PTP does not dephosphorylate the C-terminal fragment of EGFR with intact catalytic domain in vitro. SP-PTP possesses a tyrosine phosphatase activity that varies based on the type of substrates and reaction conditions. Enzyme SP-PTP also possesses Ser/Thr phosphatase activity dephosphorylating the autophosphorylated SP-STKK, i.e. the kinase domain of kinase SP-STK
-
-
?
additional information
?
-
enzyme SP-PTP does not dephosphorylate the C-terminal fragment of EGFR with intact catalytic domain in vitro. SP-PTP possesses a tyrosine phosphatase activity that varies based on the type of substrates and reaction conditions. Enzyme SP-PTP also possesses Ser/Thr phosphatase activity dephosphorylating the autophosphorylated SP-STKK, i.e. the kinase domain of kinase SP-STK
-
-
?
additional information
?
-
-
SynPTP displays catalytic activity towards all tyrosyl-phosphorylated proteins, but fails to dephosphorylate the same serylphosphorylated substrates, SynPTP functions as a protein tyrosine phosphatase not as a dual-specific phosphatase
-
-
?
additional information
?
-
-
the enzyme is also active on 4-nitrophenyl phosphate
-
-
?
additional information
?
-
the enzyme shows dual specificity, protein tyrosine/serine/threonine phosphatase activity
-
-
?
additional information
?
-
the enzyme shows dual specificity, protein tyrosine/serine/threonine phosphatase activity
-
-
?
additional information
?
-
the enzyme shows dual specificity, protein tyrosine/serine/threonine phosphatase activity
-
-
?
additional information
?
-
-
PPM displays little activity toward P-Ser/Thr histones
-
-
?
additional information
?
-
-
essential for virulence of the bacteria responsible for the plague
-
?
additional information
?
-
-
the enzyme contains a Cys(X5)Arg catalytic domain
-
-
?
additional information
?
-
-
in the YopH PTP catalytic mechanism, the active site Cys403 sits at the bottom of the pTyr-binding pocket, i.e., the active site, such that its Sgamma atom is poised 3 A from the phosphorus atom of the substrate ready for nucleophilic attack
-
-
?
additional information
?
-
-
YopH is a classical PTP with a deep active site pocket suited for phosphotyrosine, that also efficiently hydrolyzes other phosphorylated phenols
-
-
?
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((1E)-2-nitroprop-1-en-1-yl)benzene
-
50% inhibition at 0.023 mM in absence of 2-mercaptoethanol, at 0.515 mM in presence of 1 mM 2-mercaptoethanol
((2-bromo-4-((((2E)-3-phenylprop-2-en-1-yl)sulfanyl)methyl)phenyl)carbonyl)phosphonate
50% inhibition at 810 nM for wild-type, at 1290 nM for mutant S295F
((2-bromo-4-(((4-chlorobenzyl)thio)methyl)phenyl)(difluoro)methyl)phosphonate
50% inhibition at 285 nM for wild-type, at 1644 nM for mutant S295F
((2-phenyl-2-(phenylcarbonyl)propane-1,3-diyl)bis(benzene-4,1-diyl(difluoromethanediyl)))bis(phosphonate)
50% inhibition at 82 nM for wild-type, at 399 nM for mutant S295F
((4-((((3'-(acetylsulfamoyl)biphenyl-4-yl)methyl)sulfanyl)methyl)-2-bromophenyl)(difluoro)methyl)phosphonate
50% inhibition at 2.2 nM for wild-type, at 11 nM for mutant S295F
((4-((4E)-2-(1,3-benzothiazol-2-yl)-2-(1H-benzotriazol-1-yl)-5-phenylpent-4-en-1-yl)phenyl)(difluoro)methyl)phosphonate
50% inhibition at 47 nM for wild-type, at 260 nM for mutant S295F
((4-((4E)-2-(1,3-benzothiazol-2-yl)-2-(1H-benzotriazol-1-yl)-5-phenylpent-4-en-1-yl)phenyl)(fluoro)methyl)phosphonate
50% inhibition at 570 nM for wild-type, at 830 nM for mutant S295F
((4-((4E)-2-(1H-benzotriazol-1-yl)-2,5-diphenylpent-4-en-1-yl)phenyl)(difluoro)methyl)phosphonic acid
-
50% inhibition at 109 nM for isoform PTP-1B, at 95 nM for isoform TCPTP
((E)-2-nitrovinyl)benzene
-
i.e. trans-beta-nitrostyrene, slow-binding inhibitor, acting as a pY mimetic and binding to the enzyme active site to form an initial noncovalent E*I complex, followed by nucleophilic attack on the nitrostyrene nitro group by C215 of enzyme to form a reversible, covalent adduct. 50% inhibition at 0.0025 mM in absence of 2-mercaptoethanol, at 0.4 mM in presence of 1 mM 2-mercaptoethanol
(1-benzyl-3-methyl-2,3-dihydro-1H-imidazol-2-yl)(chloro)gold
-
i.e. [(BzMeIm)AuICl]
(1R,3aS,3bS,10aR,10bS,12aR)-1-[(2R)-4-carboxybutan-2-yl]-6,6,10a,12a-tetramethyl-1,2,3,3a,3b,4,6,7,10,10a,10b,11,12,12a-tetradecahydrocyclopenta[5,6]naphtho[1,2-f]indazole-9-carboxylic acid
-
-
(1R,5S,6S,6aR,7S,10S,10aS,11S)-10-(acetyloxy)-7-hydroxy-7,10a-dimethyl-4-methylidene-6-[(2-methylpropanoyl)oxy]-3-oxodecahydro-1H-1,5-methano-2-benzoxocin-11-yl 2-methylprop-2-enoate
no inhibition at 0.021 mM
(1S,3aR,8S,8aS,8bR)-4-henicosyl-1,8-dimethyl-3a-[(1E)-tricos-1-en-1-yl]-1,3a,5a,8,8a,8b-hexahydrobenzo[1,2-c:3,4-c']difuran-3,6-dione
-
-
(1S,3aS,4R,8S,8aS,8bR)-4-icosyl-1,8-dimethyl-3a-[(1E)-tricos-1-en-1-yl]-1,3a,4,8,8a,8b-hexahydrobenzo[1,2-c:3,4-c']difuran-3,6-dione
-
-
(2alpha,3alpha)-2,3-dihydroxyolean-12-en-28-oic acid
-
-
(2aS,3R,6aR,7aS,7bR,7cS)-2a-(hydroxymethyl)-3-icosyl-6a,7a-dimethyl-2a,3,6a,7a,7b,7c-hexahydrodifuro[2,3,4-cd:4',3',2'-hi][2]benzofuran-2,5-dione
-
-
(2aS,3R,6aR,7aS,7bR,7cS)-3-icosyl-6a,7a-dimethyl-2,5-dioxo-3,5,6a,7a,7b,7c-hexahydrodifuro[2,3,4-cd:4',3',2'-hi][2]benzofuran-2a(2H)-carbaldehyde
-
-
(2beta,3beta)-2,3-dihydroxyolean-12-en-28-oic acid
-
-
(2E)-1-(2'-hydroxyphenyl)-3-(1-naphthyl)-2-propen-1-one
-
76% inhibition at 0.025 mM
(2E)-1-(2,4-dihydroxyphenyl)-3-(4-hydroxyphenyl)prop-2-en-1-one
-
isolated from the CH2Cl2 extract of Glycyrrhiza inflata
(2E)-1-(2,4-dimethoxyphenyl)-3-(naphthalen-1-yl)prop-2-en-1-one
-
20% inhibition at 0.025 mM
(2E)-1-(2,4-dimethoxyphenyl)-3-(naphthalen-2-yl)prop-2-en-1-one
-
-
(2E)-1-(2,5-dimethoxyphenyl)-3-(2-naphthyl)-2-propen-1-one
-
58% inhibition at 0.025 mM
(2E)-1-(2,5-dimethoxyphenyl)-3-(naphth-1-yl)-2-propen-1-one
-
46% inhibition at 0.025 mM
(2E)-1-(2-hydroxy-4,6-dimethoxyphenyl)-3-(3-nitrophenyl)prop-2-en-1-one
-
8% inhibition at 0.025 mM
(2E)-1-(2-hydroxy-4,6-dimethoxyphenyl)-3-(naphthalen-1-yl)prop-2-en-1-one
-
16% inhibition at 0.025 mM
(2E)-1-(2-hydroxyphenyl)-3-(naphthalen-2-yl)prop-2-en-1-one
-
26% inhibition at 0.025 mM
(2E)-1-(3,4-dimethoxyphenyl)-3-(2-naphthyl)-2-propen-1-one
-
-
(2E)-1-(3,4-dimethoxyphenyl)-3-(naphthalen-2-yl)prop-2-en-1-one
-
68.5% inhibition at 0.025 mM
(2E)-1-(3-aminophenyl)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-1-(3-hydroxyphenyl)-3-(naphthalen-1-yl)prop-2-en-1-one
-
20% inhibition at 0.025 mM
(2E)-1-(3-methoxy-4-hydroxyphenyl)-3-(2-naphthyl)-2-propen-1-one
-
-
(2E)-1-(3-methoxyphenyl)-3-(naphthalen-2-yl)prop-2-en-1-one
-
18.5% inhibition at 0.025 mM
(2E)-1-(4-aminophenyl)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-1-(4-bromophenyl)-3-(naphthalen-1-yl)prop-2-en-1-one
-
25% inhibition at 0.025 mM
(2E)-1-(4-bromophenyl)-3-(naphthalen-2-yl)prop-2-en-1-one
-
11% inhibition at 0.025 mM
(2E)-1-(4-hydroxy-3-methoxyphenyl)-3-(naphthalen-2-yl)prop-2-en-1-one
-
39% inhibition at 0.025 mM
(2E)-1-(4-methoxyphenyl)-3-(naphthalen-1-yl)prop-2-en-1-one
-
18% inhibition at 0.025 mM
(2E)-1-[3-(benzyloxy)phenyl]-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-2-[1-carbamothioyl-3-(4-nitrophenyl)-5-oxo-1,5-dihydro-4H-pyrazol-4-ylidene]-1-(4-sulfophenyl)diazanide
-
-
(2E)-2-[[5-(3-carboxy-4-hydroxycyclohexa-1,5-dien-1-yl)furan-2-yl]methylidene]-1-[6-[(4-fluorophenyl)amino][1,2,5]oxadiazolo[3,4-b]pyrazin-5-yl]diazanide
-
-
(2E)-3-(1,3-benzodioxol-5-yl)-1-(2,4-dimethoxyphenyl)prop-2-en-1-one
-
8% inhibition at 0.025 mM
(2E)-3-(1,3-benzodioxol-5-yl)-1-(2,5-dimethoxyphenyl)prop-2-en-1-one
-
9% inhibition at 0.025 mM
(2E)-3-(1,3-benzodioxol-5-yl)-1-(2-hydroxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(1,3-benzodioxol-5-yl)-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
-
18% inhibition at 0.025 mM
(2E)-3-(1,3-benzodioxol-5-yl)-1-(3,4-dimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(1,3-benzodioxol-5-yl)-1-(3-nitrophenyl)prop-2-en-1-one
-
26% inhibition at 0.025 mM
(2E)-3-(1,3-benzodioxol-5-yl)-1-(4-bromophenyl)prop-2-en-1-one
-
14% inhibition at 0.025 mM
(2E)-3-(1,3-benzodioxol-5-yl)-1-(4-hydroxy-3-methoxyphenyl)prop-2-en-1-one
-
20% inhibition at 0.025 mM
(2E)-3-(1,3-benzodioxol-5-yl)-1-(4-methoxyphenyl)prop-2-en-1-one
-
6% inhibition at 0.025 mM
(2E)-3-(1,3-benzodioxol-5-yl)-1-(4-nitrophenyl)prop-2-en-1-one
-
19.5% inhibition at 0.025 mM
(2E)-3-(1,3-benzodioxol-5-yl)-1-phenylprop-2-en-1-one
-
-
(2E)-3-(3,4-dichlorophenyl)-1-(2,4,6-trimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(3-chlorophenyl)-1-(2,4,6-trimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(3-chlorophenyl)-1-(2-hydroxy-4,6-dimethoxyphenyl)prop-2-en-1-one
-
13% inhibition at 0.025 mM
(2E)-3-(3-nitrophenyl)-1-(2,4,6-trimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(4-hydroxy-2-methoxyphenyl)-1-(4-hydroxyphenyl)prop-2-en-1-one
-
isolated from the CH2Cl2 extract of Glycyrrhiza inflata
(2E)-3-(5-bromo-2,4-dihydroxyphenyl)-1-[4-methoxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(3-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(3-[[(methoxycarbonyl)sulfanyl]amino]phenyl)prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(4-butoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(4-hydroxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(4-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[2-(dimethylamino)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[2-(piperidin-1-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[2-[di(prop-2-en-1-yl)amino]phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[3-(3-methylbut-3-en-2-yl)-4-[(3-methylbut-2-en-1-yl)oxy]phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[3-(dimethylamino)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[3-(piperidin-1-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[3-[di(prop-2-en-1-yl)amino]phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(1H-pyrazol-1-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(dimethylamino)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(methylsulfonyl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(morpholin-4-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(piperidin-1-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-hydroxy-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-hydroxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-hydroxy-3-(prop-2-en-1-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-methoxy-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-methoxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-methoxy-3-(prop-2-en-1-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-[(3-methylbut-2-en-1-yl)oxy]phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-[(4-methylphenyl)sulfonyl]phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-[di(prop-2-en-1-yl)amino]phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[6-(dimethylamino)-1,3-benzodioxol-5-yl]prop-2-en-1-one
-
-
(2E)-3-(naphthalen-1-yl)-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(naphthalen-1-yl)-1-(3-nitrophenyl)prop-2-en-1-one
-
12% inhibition at 0.025 mM
(2E)-3-(naphthalen-1-yl)-1-(4-nitrophenyl)prop-2-en-1-one
-
18% inhibition at 0.025 mM
(2E)-3-(naphthalen-1-yl)-1-phenylprop-2-en-1-one
-
37% inhibition at 0.025 mM
(2E)-3-(naphthalen-2-yl)-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
-
9% activation at 0.025 mM
(2E)-3-(naphthalen-2-yl)-1-(3-nitrophenyl)prop-2-en-1-one
-
16% inhibition at 0.025 mM
(2E)-3-(naphthalen-2-yl)-1-(4-nitrophenyl)prop-2-en-1-one
-
11% inhibition at 0.025 mM
(2E)-3-(naphthalen-2-yl)-1-phenylprop-2-en-1-one
-
12% inhibition at 0.025 mM
(2E)-3-[2,4-dimethoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
-
a semisynthetic licochalcone A derivative
(2E)-3-[2,4-dimethoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-methoxyphenyl)prop-2-en-1-one
-
a semisynthetic licochalcone A derivative
(2E)-3-[4-hydroxy-2-methoxy-3-(3-methylbut-2-en-1-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
-
isolated from the CH2Cl2 extract of Glycyrrhiza inflata
(2E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
-
isolated from the CH2Cl2 extract of Glycyrrhiza inflata
(2E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-methoxyphenyl)prop-2-en-1-one
-
a semisynthetic licochalcone A derivative
(2E)-3-[4-hydroxy-2-methoxy-5-(3-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
-
isolated from the CH2Cl2 extract of Glycyrrhiza inflata
(2E)-3-[5-bromo-2-hydroxy-4-(tetrahydro-2H-pyran-2-yloxy)phenyl]-1-[4-methoxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-[5-bromo-2-methoxy-4-(tetrahydro-2H-pyran-2-yloxy)phenyl]-1-[4-hydroxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one
-
-
(2R)-2-benzyl-3-[2,6-dibromo-4-(6-bromo-5a,11a-dihydrobenzo[b]naphtho[2,3-d]furan-11-yl)phenyl]propanoic acid
-
(2Z)-2-([5-[4-(1H-tetrazol-1-yl)phenyl]furan-2-yl]methylidene)[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[[5-(2-methyl-5-nitrophenyl)furan-2-yl]methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(3alpha,5beta,8alpha,9beta,10alpha,13alpha)-3-[[(2E)-4-phenylbut-2-enoyl]oxy]kaur-16-en-18-oic acid
-
(3aR,4R,4aR,5R,8R,8aR,9S,9aR)-8-(acetyloxy)-5-hydroxy-5,8a-dimethyl-3-methylidene-4-[(2-methylpropanoyl)oxy]-2-oxododecahydronaphtho[2,3-b]furan-9-yl 3-methylbutanoate
no inhibition at 0.020 mM
(3aR,4R,4aR,5R,8R,8aS,9S,9aR)-8-(acetyloxy)-5,9-dihydroxy-5,8a-dimethyl-3-methylidene-2-oxododecahydronaphtho[2,3-b]furan-4-yl 2-methylprop-2-enoate
no inhibition at 0.025 mM
(3aR,4R,4aR,5R,8R,8aS,9S,9aR)-8-(acetyloxy)-5,9-dihydroxy-5,8a-dimethyl-3-methylidene-2-oxododecahydronaphtho[2,3-b]furan-4-yl 2-methylpropanoate
no inhibition at 0.024 mM
(3beta)-3-(acetyloxy)olean-12-en-28-oic acid
-
-
(3beta)-3-hydroxyolean-12-en-28-oic acid
-
-
(3beta)-3-hydroxyoleana-11,13(18)-dien-28-oic acid
-
-
(3S,3aR,4S,5R,7aR)-4-acetyl-7-henicosyl-3-methyl-1-oxo-7a-[(1E)-tricos-1-en-1-yl]-1,3,3a,4,5,7a-hexahydro-2-benzofuran-5-carboxylic acid
-
-
(3S,3aR,4S,7R,7aS)-4-acetyl-7-icosyl-3-methyl-1-oxo-7a-[(1E)-tricos-1-en-1-yl]-1,3,3a,4,7,7a-hexahydro-2-benzofuran-5-carboxylic acid
-
-
(3S,6S,9R)-3,6-dimethyl-9-[(R)-phenyl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione
-
-
(3S,6S,9R,12R)-3,6,9-trimethyl-12-[(R)-phenyl(phenylamino)methyl]-1,4,7,10-tetraazacyclotridecane-2,5,8,11-tetrone
-
-
(3S,9R)-3-(4-hydroxybenzyl)-9-[(R)-phenyl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione
-
-
(3Z)-5-bromo-3-[4-oxo-2-thioxo-3-[3-(trifluoromethyl)phenyl]-1,3-thiazolidin-5-ylidene]-1,3-dihydro-2H-indol-2-one
-
-
(4-((4E)-2-(1,3-benzothiazol-2-yl)-2-(1H-benzotriazol-1-yl)-5-phenylpent-4-en-1-yl)benzyl)phosphonate
50% inhibition at 3260 nM for wild-type, at 5030 nM for mutant S295F
(4-fluorophenyl)[[(Z)-(2,2,2-trifluoro-1-[1-(4-fluorophenyl)-2-methyl-5-[4-(methylsulfonyl)phenyl]-1H-pyrrol-3-yl]ethylidene)amino]oxy]methanone
-
-
(4-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-methoxy-3-oxopropyl]phenyl)methaneseleninic acid
-
inactivates the PTPs, e.g. YopH, by covalent modification, binds at the active site Cys403, kinetics, overview
(4aR,6aR,6bS,8aR,12aS,14aR,14bR)-8a-hydroxy-4,4,6a,6b,11,11,14b-heptamethyl-1,4a,5,6,6a,6b,7,8a,9,10,11,12,12a,14,14a,14b-hexadecahydropicene-3,8(2H,4H)-dione
-
-
(4aR,6aS,6bR,8aR,10S,12aR,12bR,14bS)-4a,10-dihydroxy-2,2,6a,6b,9,9,12a-heptamethyl-2,3,4,4a,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,13,14b-octadecahydropicen-5(1H)-one
-
-
(4aS,6aS,6bR,13aR)-10-acetyl-2,2,6a,6b,9,9,13a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
-
-
(4aS,6aS,6bR,13aR)-10-hexanoyl-2,2,6a,6b,9,9,13a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
-
-
(4aS,6aS,6bR,13aR)-11-amino-2,2,6a,6b,9,9,13a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,13,13a,13b,14,15b-hexadecahydropiceno[3,2-d][1,3]thiazole-4a(2H)-carboxylic acid
-
-
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
-
-
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,13,13a,13b,14,15b-hexadecahydropiceno[2,3-d][1,2]oxazole-4a(2H)-carboxylic acid
-
-
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-10-(pyridin-3-ylcarbonyl)-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
-
-
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-10-(pyridin-4-ylcarbonyl)-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
-
-
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-10-phenyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
-
-
(4aS,6aS,6bR,14aR)-11-amino-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
-
-
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,11,14a-octamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
-
-
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinoxaline-4a(2H)-carboxylic acid
-
-
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-11-(methylamino)-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
-
-
(4aS,6aS,6bR,15aR)-2,2,6a,6b,9,9,15a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,15,15a,15b,16,17b-octadecahydro-4aH-chryseno[2,1-b]carbazole-4a-carboxylic acid
-
-
(4aS,6aS,6bR,16aR)-2,2,6a,6b,9,9,16a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,16,16a,16b,17,18b-hexadecahydrochryseno[1,2-b]phenazine-4a(2H)-carboxylic acid
-
-
(4E)-2-(3,4-dichlorophenyl)-4-(3,4,5-trimethoxybenzylidene)-1,3-oxazol-5(4H)-one
-
-
(4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-1,2,3,3a,3b,4,6,6a,7,9a,10,10a,10b,11,12,12a-hexadecahydrocyclopenta[5,6]naphtho[1,2-f]indazol-1-yl]pentanoic acid
-
-
(4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-2,3,3a,3b,4,6,10,10a,10b,11,12,12a-dodecahydro-1H-cyclopenta[7,8]phenanthro[2,3-d][1,2,3]thiadiazol-1-yl]pentanoic acid
-
-
(4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-2,3,3a,3b,4,6,6a,9a,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2-d][1,2]oxazol-1-yl]pentanoic acid
-
-
(4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-7-phenyl-1,2,3,3a,3b,4,6,6a,7,9a,10,10a,10b,11,12,12a-hexadecahydrocyclopenta[5,6]naphtho[1,2-f]indazol-1-yl]pentanoic acid
-
competitive PTP1B inhibitor
(4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-8-amino-6,6,10a,12a-tetramethyl-2,3,3a,3b,4,6,10,10a,10b,11,12,12a-dodecahydro-1H-cyclopenta[7,8]phenanthro[2,3-d][1,3]thiazol-1-yl]pentanoic acid
-
-
(4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinazolin-1-yl]pentanoic acid
-
-
(4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinoxalin-1-yl]pentanoic acid
-
-
(4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-6,6,8,11a,13a-pentamethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinazolin-1-yl]pentanoic acid
-
-
(4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-8-amino-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinazolin-1-yl]pentanoic acid
-
-
(5beta,8alpha,9beta,10alpha,13alpha)-kaur-16-en-18-oic acid
-
(5R)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
(5S)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
(5Z)-3-benzyl-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
(5Z)-3-benzyl-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-3-benzyl-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-3-butyl-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-3-butyl-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(4-hydroxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-3-butyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-3-methyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-3-butyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-4-hydroxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-(3-methylbut-2-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-(prop-2-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-(propan-2-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-methyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-(benzyloxy)-5-bromo-2-methoxybenzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-(benzyloxy)-5-bromo-2-methoxybenzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-(benzyloxy)-5-bromo-2-methoxybenzylidene]-3-methyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-(3-methylbut-2-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-(prop-2-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-(propan-2-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-methyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-(prop-2-en-1-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-(prop-2-en-1-yloxy)benzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-(prop-2-en-1-yloxy)benzylidene]-3-butyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-(propan-2-yloxy)benzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-(propan-2-yloxy)benzylidene]-3-butyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-[(3-methylbut-2-en-1-yl)oxy]benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-[(4-methylpent-3-en-1-yl)oxy]benzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(6aS,6bR,8aR,10S,12aS,12bR)-10-hydroxy-2,2,6a,6b,9,9,12a-heptamethyl-2,3,4,4a,6,6a,6b,7,8,8a,9,10,11,12,12a,12b-hexadecahydropicen-5(1H)-one
-
-
(6R)-6-[(R)-phenyl(phenylamino)methyl]-1,4-diazepane-2,5-dione
-
-
(7bS,9R,13bR,15R)-7-amino-9-(hydroxymethyl)-10,13-dioxo-2,3,3a,3b,4,5,6,7,7a,7b,9,10,13,13b-tetradecahydro-1H-6,8-methanobenzo[h]imidazo[1,2-a]pyrido[3,2-c][1,5]naphthyridine-15-carbonitrile
inhibits Cdc25B modestly
(7bS,9R,13bR,15S)-7-amino-15-hydroxy-9-(hydroxymethyl)-2,3,3a,3b,4,5,6,7,7a,7b,9,13b-dodecahydro-1H-6,8-methanobenzo[h]imidazo[1,2-a]pyrido[3,2-c][1,5]naphthyridine-10,13-dione
-
(9R)-9-[(R)-furan-2-yl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione
-
-
(9R)-9-[(R)-phenyl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione
-
-
(difluoro(4-((4E)-2-((4-fluorophenyl)carbonyl)-2-(4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)-5-phenylpent-4-en-1-yl)phenyl)methyl)phosphonic acid
-
50% inhibition at 163 nM for PTP-1B wild-type, at 1903 nM for PTP-1B mutant L119V, and at 1600 nM for isoform TCPTP wild-type and 138 nM for TCPTP mutant V121L
(difluoro[4-[(2,2,2-trifluoroethyl)carbamoyl]phenyl]methyl)phosphonic acid
-
(difluoro[4-[(2-fluorophenyl)carbamoyl]phenyl]methyl)phosphonic acid
-
(difluoro[4-[(2-phenylethyl)carbamoyl]phenyl]methyl)phosphonic acid
-
(difluoro[4-[(3-fluorophenyl)carbamoyl]phenyl]methyl)phosphonic acid
-
(difluoro[4-[(4-fluorophenyl)carbamoyl]phenyl]methyl)phosphonic acid
-
(difluoro[4-[(phenylamino)methyl]phenyl]methyl)phosphonic acid
-
(difluoro[4-[2-oxo-2-(phenylamino)ethyl]phenyl]methyl)phosphonic acid
-
(difluoro[4-[methyl(phenyl)carbamoyl]phenyl]methyl)phosphonic acid
-
(E)-N-(4,5-diphenyl-1,3-thiazol-2-yl)-2-naphthalen-2-ylethenesulfonamide
-
(E)-N-[4-(4-chlorophenyl)-5-propyl-1,3-thiazol-2-yl]-2-(3,4-dichlorophenyl)ethenesulfonamide
-
(Z)-1-(3-(3-carboxy-3-hydroxyacryloyl)benzyl)-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
IC50 of 2.4 mg/ml
(Z)-1-(3-(4-ethoxy-3-hydroxy-4-oxobut-2-enoyl)benzyl)-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
IC50 of 3.1 mg/ml
(Z)-2-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(2-carboxyphenyl)hydrazono)-2-oxoindoline-5-carboxylic acid
-
-
(Z)-3-(2-(2-nitrophenyl)hydrazono)-2-oxoindoline-5-sulfonic acid
-
NSC-117199
(Z)-3-(2-(3-carboxyphenyl)hydrazono)-2-oxoindoline-5-carboxylic acid
-
-
(Z)-3-(2-(5-(4-chlorobenzylcarbamoyl)-2-oxoindolin-3-ylidene)-hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(2,4-dichlorophenethyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(2-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(3-chloro-4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(3-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(4-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(4-methylbenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-4-(2-(5-(N-(2-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-4-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-4-(2-(5-(N-(4-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-4-(2-(5-(N-(4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-4-(2-(5-(N-benzylsulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl) benzoic acid
-
-
([2-bromo-4-(3-oxo-2,3-diphenylpropyl)phenyl](difluoro)methyl)phosphonic acid
-
1,1'-(piperazine-1,4-diyl)bis(4-(3-(dibenzylamino)phenyl)butane-1,2,4-trione)
-
-
1,2-Cyclohexanedione
-
40% inhibition at 1 mM
1,3-difluoro-2-[(E)-2-nitroethenyl]benzene
-
50% inhibition at 0.0048 mM in absence of 2-mercaptoethanol, at 0.34 mM in presence of 1 mM 2-mercaptoethanol
1,6-dibenzyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
15.1% inhibition at 0.02 mg/ml
1,6-dimethyl-3-(thiophen-2-yl)pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
-
-
1-(1,3-benzodioxol-5-yl)-2-([1-(4-hydroxyphenyl)-1H-1,2,3,4-tetraazol-5-yl]sulfanyl)-1-ethanone
88% inhibition at 0.2 mM
1-(2,6-dihydroxy-4-methoxy-3-methylphenyl)ethanone
-
isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
1-(4-fluorobenzyl)-6-nitro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
36.2% inhibition at 0.02 mg/ml
1-(4-hydroxy-3-(methoxycarbonyl)benzyl)-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
IC50 of 8.1 mg/ml
1-benzyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
15.1% inhibition at 0.02 mg/ml
1-benzyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
3.1% inhibition at 0.02 mg/ml
1-benzyl-7-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
0.7% inhibition at 0.02 mg/ml
1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
0.8% inhibition at 0.02 mg/ml
1-cyclopropyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
3.5% inhibition at 0.02 mg/ml
1-cyclopropyl-N-(4-fluorobenzyl)-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxamide
-
3.3% inhibition at 0.02 mg/ml
1-ethyl-3-dimethylaminopropyl carbodiimide
-
90% inhibition at 25 mM
1-ethyl-6-methyl-3-phenyl-1H-pyrimido(5,4-e)(1,2,4)triazine-5,7-dione
1-methoxy-4-((E)-2-nitrovinyl)benzene
-
50% inhibition at 0.0045 mM in absence of 2-mercaptoethanol, at 0.27 mM in presence of 1 mM 2-mercaptoethanol
1-methyl-4-((E)-2-nitrovinyl)benzene
-
50% inhibition at 0.003 mM in absence of 2-mercaptoethanol, at 0.225 mM in presence of 1 mM 2-mercaptoethanol
1-p-Bromotetramisole oxalate
-
tetramizole no effect
1-[(5Z)-5-(1-butyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperidine-4-carboxamide
-
-
1-[4-[(2-nitrophenyl)sulfonyl]piperazin-1-yl]-2-phenoxyethanone
-
-
15-hydroxykaur-9(11),16-dien-19-oic acid
-
16alphaH,17-isovaleryloxy-ent-kauran-19-oic acid
-
diterpenoid isolated from Acanthopanax koreanum, 50% inhibition at 0.007 mM, noncompetitive
19alpha,24-dihydroxyurs-12-en-3-on-28-oic acid
-
-
2',4'-dihydroxy-1,1'-biphenyl
-
2,2'-[benzene-1,4-diylbis(methanediyloxybenzene-4,1-diyl)]bis(oxoacetic acid)
-
-
2,2-dioxo-2,3-dihydro-2-OMEGA-16-benzo (1,2,3)oxathiazole-6-carboxylic acid (5-phenylsulfanyl-1H-benzoimidazol-2-ylmethyl)-amide
2,4-dihydroxy-6-methylbenzoic acid
-
45% inhibition of PTPB1 at 0.178 mM
2,4-dimethoxy-1-((E)-2-nitrovinyl)benzene
-
50% inhibition at 0.028 mM in absence of 2-mercaptoethanol, at 0.390 mM in presence of 1 mM 2-mercaptoethanol
2,5-dihydroxy-3-[7-(2-methylbenzyl)-1H-indol-3-yl]cyclohexa-2,5-diene-1,4-dione
-
2,5-dihydroxy-3-[7-(3-methylbut-2-en-1-yl)-1H-indol-3-yl]cyclohexa-2,5-diene-1,4-dione
-
2-((carboxycarbonyl)amino)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
i.e. OATP
2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
2-((carboxycarbonyl)amino)-5-((4-fluoro-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
2-((carboxycarbonyl)amino)-5-((4-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
2-((carboxycarbonyl)amino)-5-((5-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
2-(2,5-dimethyl-1H-pyrrol-1-yl)-5-hydroxybenzoic acid
-
36% residual activity at 0.1 mM; 3% residual activity at 0.1 mM; 7% residual activity at 0.1 mM; 9% residual activity at 0.1 mM
2-(4-hydroxyphenyl)-3-[(3,4-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
2-(4-hydroxyphenyl)-3-[(4-carboxy-3-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
2-(oxalyl-amino)-4,5,6,7-tetrahydro-thieno[2,3-c]pyridine-3-carboxylic acid
-
2-(oxalyl-amino)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid
-
2-(oxalyl-amino)-4,7-dihydro-5H-thieno[2,3-c]thiopyran-3-carboxylic acid
-
-
2-carboperoxybenzoate
-
complete inhibition at 150 mM
2-chloro-4-(2,5-dimethyl-1H-pyrrol-1-yl) benzoic acid
-
36% residual activity at 0.1 mM; 46% residual activity at 0.1 mM; 95% residual activity at 0.1 mM; 98% residual activity at 0.1 mM
2-chloro-5-(2,5-dimethyl-1H-pyrrol-1-yl) benzoic acid
-
37% residual activity at 0.1 mM; 77% residual activity at 0.1 mM; 88% residual activity at 0.1 mM; 91% residual activity at 0.1 mM
2-hydroperoxytetrahydrofuran
-
inactivation by 2-hydroperoxytetrahydrofuran (0.05 mM, 10 min) is reversed upon reaction of the enzyme with dithiothreitol (54% return of activity, following treatment with 100 mM dthiothreitol for 1 h)
2-[(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)imino]-1H-indene-1,3(2H)-dione
-
-
2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
i.e. TCS401, binds to the active site
2-[4,5-bis(1,3,2-dithiarsolan-2-yl)-6-hydroxy-3-oxo-3H-xanthen-9-yl]benzoic acid
i.e. FlAsH
2-[6-chloro-5-(1-naphthalyloxy)-1H-benzimidazol-2-yl]thio-N-(thiazol-2-yl)acetamide
mixed-type inhibition, 99% inhibition at 0.2 mM
24-hydroxyursolic acid
-
-
28-(10-decanoic)-oleanolic acid
-
28-(12-dodecanoic)-oleanolic acid
-
28-(2-acetic)-oleanolic acid
-
28-(4-butyric)-oleanolic acid
-
28-(6-hexanoic)-oleanolic acid
-
28-(8-octanoic)-oleanolic acid
-
28-(glycine)-oleanolic acid amide
-
28-(L-glutamic acid)-oleanolic acid amide
-
28-(L-phenylalanine)-oleanolic acid amide
-
28-(p-carboxyphenyl)-oleanolic acid amide
-
28-[4-butyric((R)-1-carboxy-phenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric((S)-1-carboxy-3-indole-ethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric((S)-1-carboxy-5-imidazole-ethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric((S)-1-carboxy-methylthioethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric((S)-1-carboxy-phenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-2,3-dimethoxyphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-3,4-dimethoxyphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-3,4-oxymethyleneoxyphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-3,5-dimethoxyphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-m-chlorophenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-m-methoxyphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-o-chlorophenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-o-methoxyphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-o-methylphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-p-chlorophenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-p-fluorophenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-p-methoxyphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-p-methylphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-p-nitrophenylethyl)-amide]-DELTA12-oleanene
-
2alpha,3alpha,19alpha,23-tetrahydroxyurs-12-en-28-oic acid
-
50% inhibition at 0.0421 mM
2beta,3beta-2,3-dihydroxyolean-12-en-28-oic acid
-
-
3',4'-dihydroxy-1,1'-biphenyl
no inhibition of LMW-PTP isozymes, but 5% inhibition of PTP-B1 at 0.02 mM
3,16-dioxo-olean-12(13),17(18)-diene
-
-
3-((3,5-dibromo-4-hydroxyphenyl)carbonyl)-2-ethyl-N-(4-(1,3-thiazol-2-ylsulfamoyl)phenyl)-1-benzofuran-6-sulfonamide
50% inhibition of PTP1B at 0.008 mM, noncompetitive noncompetitive allosteric inhibitor, prevents formation of the active form of the enzyme by blocking the mobility of the catalytic loop
3-((3,5-dibromo-4-hydroxyphenyl)carbonyl)-2-ethyl-N-(4-sulfamoylphenyl)-1-benzofuran-6-sulfonamide
50% inhibition of PTP1B at 0.022 mM, noncompetitive allosteric inhibitor, prevents formation of the active form of the enzyme by blocking the mobility of the catalytic loop
3-(1-carboxy-ethoxy)-6-chloro-benzo(b)-thiophene-2-carboxylic acid
-
-
3-(2,2'-dimethyl-carboxypropanoyloxy)-oleanolic acid
-
3-(2,5-dimethyl-1H-pyrrol-1-yl)-4-hydroxybenzoic acid
-
20% residual activity at 0.1 mM; 3% residual activity at 0.1 mM; 52% residual activity at 0.1 mM; 7% residual activity at 0.1 mM
3-(2-carboxy-benzyloxy)-oleanolic acid
-
3-(2-carboxybenzoyloxy)-oleanolic acid
-
3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethyl-N,N-dimethyl-1-benzofuran-6-sulfonamide
50% inhibition of PTP1B at 0.35 mM
3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethyl-N-[4-(1,3-thiazol-2-ylsulfamoyl)phenyl]-1-benzofuran-6-sulfonamide
-
3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethylbenzofuran-6-sulfonic acid-(4-(thiazol-2-yl-sulfamyl)-phenyl)-amide
-
a PTP1b inhibitor, inhibit 50% tog the infectivity of Trypanosoma cruzi trypomastigotes
3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethylbenzofuran-6-sulfonic acid-[4-(thiazol-2-ylsulfamyl)phenyl]-amide
i.e. BBR
3-(3-carboxy-benzyloxy)-oleanolic acid
-
3-(4-carboxy-benzyloxy)-28-[4-butyric((s)-1-carboxyphenylethyl)-amide]-DELTA12-oleanene
-
3-(4-carboxy-benzyloxy)-oleanolic acid
-
3-(4-chlorophenyl)-1,6-dimethylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
-
-
3-(biphenyl-4-ylmethyl)-6-hydroxy-2-(4-hydroxybenzyl)-4H-chromen-4-one
-
3-(carboxy-fluoro-methoxy)-6-chloro-benzo(b)thiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-2-naphthoic acid
-
-
3-(carboxymethoxy)-5-((cyclohexylmethyl)-amino)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-5-(cyclohexylamino)-thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-5-chlorothieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-6-((1-(ethylsulfonyl)-piperidin-4-yl)amino)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-6-((cyclohexylmethyl)-amino)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-6-(cyclohexylamino)-thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-6-(tetrahydro-2H-pyran-4-ylamino)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-6-chlorothieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-6-methylthieno(3,2-c)pyridine-2-carboxylic acid
-
-
3-(carboxymethoxy)benzo(b)thiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)furo(2,3-b)pyridine-2-carboxylic acid
-
-
3-(carboxymethoxy)thieno(2,3-b)pyridine-2-carboxylic acid
-
reversible, competitive
3-(carboxymethoxy)thieno(3,2-b)(1)benzo-thiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)thieno(3,2-b)pyridine-2-carboxylic acid
-
-
3-(carboxymethoxy)thieno(3,2-b)thiophene-2-carboxylic acid
-
-
3-([2-chloro-6-methoxy-4-[(E)-(3-oxo[1,3]thiazolo[3,2-a]benzimidazol-2(3H)-ylidene)methyl]phenoxy]methyl)benzoic acid
-
3-benzyl-7-hydroxy-2-(4-hydroxybenzyl)-4H-chromen-4-one
10% inhibition of LMW-PTP isozymes 1 and 2,no inhibition of PTP-B1, at 0.015 mM
3-benzyloxy-oleanolic acid
-
3-butyl-7-(2,4-dihydroxy-6-pentylphenoxy)-3,5-dimethoxy-2-benzofuran-1(3H)-one
-
a pseudodepsidone-type compound, isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
3-carboxymethoxy-6-(4-hydroxyphenyl)-benzo(b)-thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-6-(5-methyl-1-phenyl-1H-pyrazol-3-ylcarbamoyl)-benzo(b)thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-6-chloro-benzo(b)-thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-6-phenylbenzo(b)-thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-6-thiophen-2-yl-benzo(b)-thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-7-chloro-benzo(b)-thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-7-methyl-benzo(b)-thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-naphtho(1,2-b)thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-thieno(3,2-c)quinoline-2-carboxylic acid
-
-
3-carboxypropanoyloxy-oleanolic acid
-
3-chlorobenzenecarboperoxoic acid
-
complete inhibition at 150 mM
3-dehydroxy-oleanolic acid
-
3-ethyl oxalyl-oleanolic acid
-
3-hydroxy-4-(methoxycarbonyl)-2,5-dimethylphenyl 3-acetyl-2,4-dihydroxy-6-methylbenzoate
-
isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
3-hydroxy-4-(methoxycarbonyl)-5-methylphenyl 4-(beta-D-galactopyranosyloxy)-2-hydroxy-6-pentadecylbenzoate
-
-
3-methyl-2-butenal
-
95% remaining activity at 0.5 mM
3-methylene-oleanolic acid
-
3-oxalyl-oleanolic acid
-
3-[(1-butyl-1,6-dimethoxy-3-oxo-1,3-dihydro-2-benzofuran-4-yl)oxy]-4,6-dihydroxy-2-pentylbenzoic acid
-
a pseudodepsidone-type compound, isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
3-[(2-nitrophenyl)hydrazono]-2-oxo-2,3-dihydro-1H-indole-5-sulfonamide
-
-
3-[(2-nitrophenyl)hydrazono]-2-oxo-2,3-dihydro-1H-indole-5-sulfonic acid 4-chlorobenzylamide
-
-
3-[(3-[(E)-[3-(4-carboxybenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
3-[(4-[(Z)-[3-(4-carboxybenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
3-[(E)-(3-oxo[1,3]thiazolo[3,2-a]benzimidazol-2(3H)-ylidene)methyl]benzoic acid
-
3-[2,5-dimethyl-3-[(3-oxo-2,3-dihydro[1,3]thiazolo[3,2-a]benzimidazol-2-yl)methyl]-1H-pyrrol-1-yl]benzoic acid
irreversible inhibition, detailed kinetic analysis of the interaction between E4 and the catalytic domain of enzyme STEP, overview. kinact is 0.068/s
3-[3-(2,4-dichlorophenyl)propanoyl]-2-hydroxycyclohepta-2,4,6-trien-1-one
-
3-[N'-(5-isopropylsulfamoyl-2-oxo-1,2-dihydroindol-3-ylidene)-hydrazino]benzoic acid
-
-
3-[oxalyl-amino]naphthalene-2-carboxylic acid
-
3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4,6-dicarboxylic acid
-
25% residual activity at 0.1 mM; 39% residual activity at 0.1 mM; 65% residual activity at 0.1 mM; 73% residual activity at 0.1 mM
3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4,8-dicarboxylic acid
-
30% residual activity at 0.1 mM; 53% residual activity at 0.1 mM; 63% residual activity at 0.1 mM; 79% residual activity at 0.1 mM
3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid
-
23% residual activity at 0.1 mM; 75% residual activity at 0.1 mM; 80% residual activity at 0.1 mM; 9% residual activity at 0.1 mM
3alpha-angeloyloxypterokaurene L3
18% inhibition at 0.024 mM
3alpha-cinnamoyloxypterokaurene L3
-
3alpha-tigloyloxypterokaurene L3
no inhibition at 0.024 mM
3beta,16a,17-trihydroxy-olean-12-ene
-
-
3beta-acetoxy-17beta-hydroxy-28-norolean-12-ene
-
-
3beta-acetoxy-28-hydroxyolean-12-ene
-
-
3beta-acetoxyolean-12-en-28-acid
-
-
3beta-acetoxyolean-12-en-28-aldehyde
-
-
3beta-hydroxyolean-12-en-28-oic acid
-
-
4'-carboxy-3'-hydroxy-1,1'-biphenyl
no inhibition of LMW-PTP isozymes, but 10% inhibition of PTP-B1 at 0.02 mM
4'-[(2-butyl-1-benzofuran-3-yl)methyl]biphenyl-4-ol
-
4'-[2-(4-hydroxybutyl)-1-benzofuran-3-yl]biphenyl-4-ol
-
4,4'-[benzene-1,4-diylbis(methanediyloxy)]dibenzoic acid
-
4,6-bis(1,3,2-dithiarsolan-2-yl)-7-hydroxy-3H-phenoxazin-3-one
i.e. ReAsH
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(3-phenoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(3-phenylmethoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(4-phenoxyphenyl)methylidene]thiazolidin-3-yl) methyl)benzoic acid
-
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(4-phenylmethoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-4-oxo-5-[(3-phenoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-4-oxo-5-[(3-phenylmethoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-4-oxo-5-[(4-phenoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-4-oxo-5-[(4-phenylmethoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
-
4-((3E)-1-(1H-benzotriazol-1-yl)-1-(4-(difluoro(phosphono)methyl)benzyl)-4-phenylbut-3-en-1-yl)benzoic acid
-
50% inhibition at 39 nM for wild-type PTP-1B, at 39 nM for mutant V113I, at 45 nM for mutant M114V, at 29 nM for mutant V113I/M114V, at 32 nM for mutant G117E, at 142 nM for mutant L119V, and at 87 nM for isoform TCPTP wild-type and 24 nM for isoform TCPTP mutant V121L
4-((E)-2-nitrovinyl)benzoic acid
-
50% inhibition at 0.0027 mM in absence of 2-mercaptoethanol, at 0.425 mM in presence of 1 mM 2-mercaptoethanol
4-(2,5-dimethyl-1H-pyrrol-1-yl) benzoic acid
-
63% residual activity at 0.1 mM; 6% residual activity at 0.1 mM; 88% residual activity at 0.1 mM; 9% residual activity at 0.1 mM
4-(2,5-dimethyl-1H-pyrrol-1-yl)-3-hydroxybenzoic acid
-
21% residual activity at 0.1 mM; 67% residual activity at 0.1 mM; 72% residual activity at 0.1 mM; 9% residual activity at 0.1 mM
4-(2,5-dimethyl-1H-pyrrol-1-yl)phthalic acid
-
18% residual activity at 0.1 mM; 54% residual activity at 0.1 mM; 78% residual activity at 0.1 mM; 80% residual activity at 0.1 mM
4-(3-(dibenzylamino)phenyl)-2,4-dioxobutanoic acid
-
-
4-(5-bromo-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-2-hydroxybenzoic acid
-
4-(5-[5-(3,5-dichlorophenoxy)-2-furyl]-1,2,4-oxadiazol-3-yl)phenyl-N,N-dimethylsulfamate
85% inhibition at 0.2 mM
4-(beta-D-galactopyranosyloxy)-2-hydroxy-6-pentadecylbenzoic acid
-
-
4-(difluoro(phosphono)methyl)-N-pentadecanoyl-L-phenylalanyl-L-a-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide
-
-
4-(difluoro(phosphono)methyl)-N-pentadecanoyl-L-phenylalanyl-L-alpha-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide
-
dose-dependent increase in Y527 phosphorylation of Src
4-([(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2-[(4-methoxyphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2-[(4-tert-butylphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2-[(4-methoxyphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2-[(4-tert-butylphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5E)-5-[3-(benzyloxy)benzylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5Z)-2,4-dioxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5Z)-2,4-dioxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5Z)-2-(4-fluorophenylimino)-4-oxo-5-([3-(2-phenylethoxy)phenyl]methylidene)thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5Z)-2-(4-fluorophenylimino)-4-oxo-5-([4-(2-phenylethoxy)phenyl]methylidene)thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5Z)-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene)-2-thioxothiazolidin-3-yl]methyl]benzoic acid
-
4-([(5Z)-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene)-2-thioxothiazolidin-3-yl]methyl]benzoic acid
-
4-([(5Z)-5-[4-(benzyloxy)benzylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-chloro-N-(6-ethoxy-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
4-chloro-N-(6-methoxy-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
4-chloro-N-(6-methyl-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
4-chloro-N-(6-nitro-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
4-fluoro-N-(6-nitro-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
4-fluorobenzyl-1-cyclopropyl-6-(4-fluorobenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylate
-
73% inhibition at 0.02 mg/ml
4-hydroxymercuribenzoate
-
62% inhibition at 2.5 mM
4-isoavenaciolide
potent irreversible inhibitor of VHR; potent irreversible inhibitor of VHR; potent irreversible inhibitor of VHR
4-methoxy-3-(5-methoxy-1-benzofuran-6-yl)-5-(4-methoxyphenyl)isoxazole
-
4-methoxy-3-(5-methoxy-1-benzofuran-6-yl)-5-phenylisoxazole
-
4-methoxy-N-(6-methoxy-1,3-benzothiazol -2-yl)benzenesulfonamide
-
-
4-methoxy-N-(6-methyl-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
4-methoxy-N-(6-nitro-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
4-methyl-N-(6-methyl-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
4-methyl-N-(6-nitro-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
4-nitro-N-(6-nitro-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
4-nitrocatechol sulfate
-
applied from from bare and amine functionalized mesoporous silica, MCM-48, and mesoporous alumina for sustained delivery, competitive inhibition, kinetics, overview
4-nitrophenyl phosphate
substrate inhibition at higher concentrations; substrate inhibition at higher concentrations
4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.073 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
4-oxo-6,8-diphenyl-4H-chromene-3-carbaldehyde
50% inhibition at 0.0033 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM
4-oxo-6-(2-phenyl-1-benzothien-3-yl)-4H-chromene-3-carbaldehyde
50% inhibition at 0.0062 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
4-oxo-6-phenyl-4H-chromene-3-carbaldehyde
50% inhibition at 0.014 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
4-oxo-8-(phenylsulfanyl)-1,4-dihydro-1,7-naphthyridine-3-carboxylic acid
-
4-oxo-8-phenyl-4H-chromene-3-carbaldehyde
50% inhibition at 0.016 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
4-[(1E)-3-(4-hydroxyphenyl)-3-oxoprop-1-en-1-yl]-5-methoxy-2-(2-methylbut-3-en-2-yl)phenyl acetate
-
a semisynthetic licochalcone A derivative
4-[(2,4-dihydroxy-6-pentadecylbenzoyl)oxy]-2-hydroxy-6-methylbenzoic acid
-
-
4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenyl 4-bromobenzoate
-
-
4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenyl 4-tert-butylbenzoate
-
-
4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenyl benzoate
-
-
4-[(2E)-3-[2,4-dimethoxy-5-(2-methylbut-3-en-2-yl)phenyl]prop-2-enoyl]phenyl acetate
-
a semisynthetic licochalcone A derivative
4-[(2E)-3-[4-(acetyloxy)-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]prop-2-enoyl]phenyl acetate
-
a semisynthetic licochalcone A derivative
4-[(2E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]prop-2-enoyl]phenyl acetate
-
a semisynthetic licochalcone A derivative
4-[(3-[(E)-[(2Z)-3-(4-carboxybenzyl)-4-oxo-2-(phenylimino)-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
4-[(3-[(E)-[3-(4-carboxybenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
4-[(4-[(Z)-[(2Z)-3-(4-carboxybenzyl)-4-oxo-2-(phenylimino)-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
4-[(4-[(Z)-[3-(4-carboxybenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
4-[1,3-dioxo-5-(4-oxo-4H-3,1-benzoxazin-2-yl)-1,3-dihydro-2H-isoindol-2-yl]benzoate
-
-
4-[2-[(5-chloro-1,3-benzoxazol-2-yl)sulfanyl]acetamido]benzoic acid
-
4-[4,5-di(biphenyl-4-yl)-1H-imidazol-2-yl]benzoic acid
-
-
4-[4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenoxy]butanoic acid
-
-
4-[difluoro(phosphono)methyl]benzoic acid
-
4-[N'-(5-isopropylsulfamoyl-2-oxo-1,2-dihydroindol-3-ylidene)-hydrazino]benzoic acid
-
-
4-[[(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-4-oxo-5-[(3-phenoxyphenyl)methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-4-oxo-5-[(4-phenoxyphenyl)methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2Z,5E)-5-(3-[[4-(hydroxymethyl)benzyl]oxy]benzylidene)-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2Z,5E)-5-[3-(benzyloxy)benzylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2Z,5Z)-5-(4-[[4-(hydroxymethyl)benzyl]oxy]benzylidene)-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2Z,5Z)-5-[4-(benzyloxy)benzylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5E)-5-(3-[[4-(hydroxymethyl)benzyl]oxy]benzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5Z)-2,4-dioxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5Z)-2,4-dioxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5Z)-5-(4-[[4-(hydroxymethyl)benzyl]oxy]benzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
5,7-bis[(E)-2-[4-(dimethylamino)phenyl]ethenyl]-2-methyltetrazolo[1,5-a]pyrimidin-2-ium
-
-
5-(1,3,2-dithiarsolan-2-yl)-2-[(1E,3E)-3-[5-(1,3,2-dithiarsolan-2-yl)-3,3-dimethyl-1-(4-sulfobutyl)-1,3-dihydro-2H-indol-2-ylidene]prop-1-en-1-yl]-3,3-dimethyl-1-(4-sulfobutyl)-3H-indol-1-ium
i.e. AsCy3, 70% inhibition at 250 nM AsCy3, AsCy3 is capable of specifically and potently inhibiting mutant enzyme asPTP1B in the presence of a complex proteome, while AsCy3 does not inhibit wild-type PTP1B activity in a cell lysate
5-(1,3,2-dithiarsolan-2-yl)-2-[(1E,3E,5E)-5-[5-(1,3,2-dithiarsolan-2-yl)-3,3-dimethyl-1-(4-sulfobutyl)-1,3-dihydro-2H-indol-2-ylidene]penta-1,3-dien-1-yl]-3,3-dimethyl-1-(4-sulfobutyl)-3H-indol-1-ium
i.e. AsCy5
5-(2-fluoro-5-((1E)-3-[3-hydroxy-2-(methoxycarbonyl)phenoxy]prop-1-en-1-yl)phenyl)isoxazole-3-carboxylic acid
-
5-([(E)-[2-(4-chlorophenyl)-5-oxo-1,3-oxazol-4(5H)-ylidene]methyl]amino)-2-hydroxybenzoic acid
-
-
5-([1-[(2-chloro-1,3-thiazol-5-yl)methyl]-1H-indol-3-yl]methylidene)-1,3-dimethylpyrimidine-2,4,6(1H,3H,5H)-trione
-
-
5-acetylamino-2-(2,5-dimethyl-1H-pyrrol-1-yl) benzoic acid
-
45% residual activity at 0.1 mM; 46% residual activity at 0.1 mM; 82% residual activity at 0.1 mM; 94% residual activity at 0.1 mM
5-chloro-2-[methyl(methylidene)-lambda4-sulfanyl]-6-[(naphthalen-2-yl)oxy]-1H-benzimidazole
65% inhibition at 0.2 mM
5-chloro-N-[6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazol-2-yl]-1-methyl-2-(methylthio)-1H-benz-imidazole-6-carboxamide
mixed-type inhibition, complete inhibition at 0.2 mM
5-methoxy-4-[(1E)-3-(4-methoxyphenyl)-3-oxoprop-1-en-1-yl]-2-(2-methylbut-3-en-2-yl)phenyl acetate
-
a semisynthetic licochalcone A derivative
5-[3-bromo-4-[(4-nitrobenzyl)oxy]benzylidene]pyrimidine-2,4,6(1H,3H,5H)-trione
-
-
5-[4-(3,4-dihydroisoquinolin-2(1H)-yl)-3-nitrobenzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
-
5-[4-[(2-chloro-6-fluorobenzyl)oxy]benzylidene]-1,3-dimethylpyrimidine-2,4,6(1H,3H,5H)-trione
-
-
6,7-dihydroxy-2-(4-hydroxyphenyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
6,8-dibenzyl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.013 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-((1-(benzylsulfonyl)piperidin-4-yl)amino)-3-(carboxymethoxy)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
6-((2-benzyl-1-benzothien-3-yl)methyl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0032 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM
6-((E)-1,2-diphenylvinyl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0097 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-(1-benzothien-2-ylmethyl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.006 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-(1-benzothien-3-yl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0077 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-(1-benzothien-3-ylmethyl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.06 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-(10-bromo-9-anthryl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0025 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR at 0.57 mM
6-(4-((2-benzyl-1-benzothiophen-3-yl)methyl)phenyl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0011 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM
6-(4-((2-benzyl-1-benzothiophen-3-yl)methyl)phenyl)-4-oxo-8-phenyl-4H-chromene-3-carbaldehyde
50% inhibition at 0.001 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR at 0.52 mM
6-(4-(3-(3-(benzyloxy)-2-(methoxycarbonyl)phenoxy)propyl)piperazin-1-yl)-1-cyclopropyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
IC50 of 45.2 mg/ml
6-(4-benzylpiperazin-1-yl)-1-cyclopropyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
62.3% inhibition at 0.02 mg/ml
6-(9-anthryl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0071 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-amino-1-(4-fluorobenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
12.4% inhibition at 0.02 mg/ml
6-benzyl-1-cyclopropyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
87.5% inhibition at 0.02 mg/ml
6-benzyl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.036 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-biphenyl-4-yl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0043 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-biphenyl-4-yl-4-oxo-8-phenyl-4H-chromene-3-carbaldehyde
50% inhibition at 0.002 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM
6-bromo-3-carboxymethoxy-benzo(b)-thiophene-2-carboxylic acid
-
-
6-bromo-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.020 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-chloro-7-(2,3-dihydro-1H-inden-1-ylamino)quinoline-5,8-dione
-
6-chloro-7-[(2-morpholin-4-ylethyl)amino]quinoline-5,8-dione
-
6-dibenzo(b,d)thien-1-yl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0076 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-dibenzo(b,d)thien-4-yl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.011 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-fluoro-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid
-
35% residual activity at 0.1 mM; 63% residual activity at 0.1 mM; 72% residual activity at 0.1 mM; 75% residual activity at 0.1 mM
6-hydroxy-2-(4-hydroxybenzyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
20% inhibition of PTP-B1 at 0.015 mM
6-hydroxy-2-phenyl-3-((3-trifluoromethyl)phenyl)benzofuran-5-carboxylic acid
-
most potent, reversible and noncompetitive inhibitor, highly selective towards isoform PTPB
6-hydroxy-3-[1-[4-(naphthalen-1-ylamino)-4-oxobutyl]-1H-1,2,3-triazol-4-yl]-2-phenyl-1-benzofuran-5-carboxylic acid
-
-
6-hydroxy-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylate
-
80% residual activity at 0.1 mM
6-hydroxy-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid
-
38% residual activity at 0.1 mM; 50% residual activity at 0.1 mM; 73% residual activity at 0.1 mM
6-iodo-1-(4-methoxy-3-(methoxycarbonyl)benzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
IC50 of more than 20 mg/ml
6-oxo-6H-cyclohepta[b]furan-5,7-dicarboxylic acid
-
7-(2-((1H-imidazol-2-yl)thio)ethoxy)-2-phenyl-4H-chromen-4-one
-
7-(2-(1H-1,2,4-triazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
the inhibitor is significantly selective for enzyme protein tyrosine phosphatase 1B (PTP1B) versus other phosphatases, i.e. T-cell protein tyrosine phosphatase (TCPTP), megakaryocyte protein tyrosine phosphatase (PTP-MEG2), and src homology phosphatase 2
7-(2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
-
7-(2-(4-nitro-1H-imidazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
-
7-(2-(5-methyl-1H-tetrazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
-
7-(2-bromoethoxy)-2-phenyl-4H-1-benzopyran-4-one
-
7-(3-(4-nitro-1H-imidazol-1-yl)propoxy)-2-phenyl-4H-chromen-4-one
-
7-(4-((1H-imidazol-2-yl)thio)butoxy)-2-phenyl-4H-chromen-4-one
-
7-(4-(1H-1,2,4-triazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
-
7-(4-(2-methyl-5-nitro-1H-imidazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
-
7-(4-(5-methyl-1H-tetrazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
-
7-(4-bromobutoxy)-2-phenyl-4H-1-benzopyran-4-one
-
7-bromo-6-difluoromethylphosphonate 3-naphthalenenitrile
50% inhibition at 230 nM for wild-type, at 886 nM for mutant S295F
7-chloro-6-[(2-morpholin-4-ylethyl)amino]quinoline-5,8-dione
-
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3'',4''-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3''-carboxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-carboxy-3''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
7-hydroxy-2-(4-hydroxybenzyl)-4H-chromen-4-one
10% inhibition of LMW-PTP isozymes 1 and 2,no inhibition of PTP-B1, at 0.015 mM
7-hydroxy-2-(4-hydroxyphenyl)-2,3-dihydro-4H-chromen-4-one
-
isolated from the CH2Cl2 extract of Glycyrrhiza inflata
7-hydroxy-2-(4-hydroxyphenyl)-3-[(3',4'-dihydroxy-1,1-biphenyl-3-yl)methyl]-4H-1-benzopyran-4-one
60% inhibition of LMW-PTP isozyme 2, 25% inhibition of LMW-PTP 1, and 50% inhibition of PTP-B1, at 0.02 mM
7-hydroxy-2-(4-hydroxyphenyl)-3-[(4'-carboxy-3'-hydroxy-1,1-biphenyl-3-yl)methyl]-4H-1-benzopyran-4-one
5% inhibition of LMW-PTP isozyme 2, 10% inhibition of LMW-PTP 1, and 59% inhibition of PTP-B1, at 0.02 mM
7-hydroxy-2-(4-hydroxyphenylethyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
20% inhibition of PTP-B1 at 0.015 mM
7-hydroxy-2-(4-hydroxyphenylmethyl)-3-[(1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
10% inhibition of PTP-B1 at 0.015 mM
7-hydroxy-2-(4-hydroxyphenylpropyl)-3-[(1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
10% inhibition of LMW-PTP isozymes 1 and 2,no inhibition of PTP-B1, at 0.015 mM
8-acetyl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid
-
48% residual activity at 0.1 mM; 66% residual activity at 0.1 mM; 81% residual activity at 0.1 mM; 83% residual activity at 0.1 mM
8-benzyl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.018 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-bromo-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid
-
33% residual activity at 0.1 mM; 41% residual activity at 0.1 mM; 8% residual activity at 0.1 mM; 90% residual activity at 0.1 mM
8-bromo-4-oxo-6-(2-phenyl-1-benzothien-3-yl)-4H-chromene-3-carbaldehyde
50% inhibition at 0.0078 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-bromo-6-(10-bromo-9-anthryl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.011 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-bromo-6-(2-bromo-1-benzothien-3-yl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0082 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-bromo-6-dibenzo(b,d)thien-1-yl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.010 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-bromo-6-dibenzo(b,d)thien-4-yl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.016 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-hydroxy-3-methoxy-11-oxo-1-pentanoyl-6-pentyl-11H-dibenzo[b,e][1,4]dioxepine-7-carboxylic acid
-
isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
abietic acid
a nonpolar inhibitor and weak mixed-type inhibitor of PTP1B, inhibits the enzyme by binding to its active site in a nonsubstrate-like manner that stabilizes the catalytically essential WPD loop in an inactive conformation, modelling of enzyme binding. Upon binding to the active site, abietic acid forms a hydrogen bond with R221 that weakens a bond between R221 and E115 and prevents the formation of a hydrogen bond between W179 and R221 that forms when the WPD loop closes
acanthoic acid
-
diterpenoid isolated from Acanthopanax koreanum, 50% inhibition at 0.024 mM
acetaldehyde
-
more than 95% remaining activity at 0.5 mM
Acetylsalicylic acid
-
80% inhibition at 0.2 mM
acrolein
-
4% remaining activity at 0.5 mM, potent irreversible time-dependent inhibitor, addition of 1 mM vanadate slows inactivation of PTP1B by 0.5 mM acrolein
antimonate
-
inhibition of protein tyrosine phosphatase activity
aquastatin A
-
derived from marine fungus Cosmospora sp. SF-5060, competitive inhibition
arsenate
-
inhibition of protein tyrosine phosphatase activity
benzyl (3R,6S)-4,9-dioxo-3-[(R)-phenyl(phenylamino)methyl]-1,5-diazonane-6-carboxylate
-
-
benzyl 1,6-dibenzyl-4-oxo-1,4-dihydroquinoline-3-carboxylate
-
0.1% inhibition at 0.02 mg/ml
benzyl 1-cyclopropyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylate
-
80.5% inhibition at 0.02 mg/ml
benzyl oleanolic acid amide
-
benzyl oleanolic acid ester
-
Berberine
binding structure, molecular modeling, overview
betulinic acid
-
95.1% PTP1B inhibitory activity with 0.0007 mg/ml
betulinic acid methyl ester
-
89.4% PTP1B inhibitory activity with 0.00093 mg/ml
biphenyl-3,4-diol
25% inhibition of LMW-PTP isozyme 2, and 10% inhibition of LMW-PTP 1 and PTP-B1 at 0.02 mM
bis(2-ethyl-maltolato)oxidovanadium(IV)
noncompetitive inhibition of hydrolysis of 4-nitrophenyl phosphate and of phosphorylated undecapeptide substrate EGFR988-998 in the presence of bis(2-ethyl-maltolato)oxidovanadium(IV)
bis(2-methyl-maltolato)oxidovanadium(IV)
-
bis(3-hydroxy-2-methyl-4(1H)pyridinonato)oxidovanadium(IV)
-
bis(acetylacetonato)oxidovanadium(IV)
acts as an uncompetitive inhibitor of PTP1B with DADEpYLIPQQG as the substrate, but this VO2+-chelate exhibits only apparent competitive inhibition of 4-nitrophenyl phosphate hydrolysis when catalyzed by PTP1B, differing from that observed in the hydrolysis of the phosphotyrosine-containing undecapeptide DADEpYLIPQQG mimicking residues 988-998 of the epidermal growth factor receptor (EGFR). Addition of 4-nitrophenyl phosphate after addition of saturating amounts of bis(acetylacetonato)oxidovanadium(IV) to PTP1B causes complete loss of catalytic activity
cantharidin
-
17% inhibition at 1 mM
chloro(1,3-dimethyl-1,3-dihydro-2H-imidazol-2-ylidene)gold
-
i.e. [(p-MeMeIm)AuICl]
chloro(1-methyl-1,3-dihydro-2H-imidazol-2-ylidene)gold
-
i.e. [(MeIm)AuICl]
chloro[1-methyl-3-(4-methylbenzyl)-2,3-dihydro-1H-imidazol-2-yl]gold
-
i.e. [(p-MeBzMeIm)AuICl]
continentalic acid
modelling of enzyme binding
corosolic acid
-
50% inhibition at 0.0072mM, mixed-type inhibition
Cr(VI)
-
as Na2CrO4, induces clonogenic lethality
crotonaldehyde
-
85% remaining activity at 0.5 mM
cyclopropyl-6-(4-fluorobenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
71.1% inhibition at 0.02 mg/ml
dehydroabietic acid
modelling of enzyme binding
dehydrocostuslactone
-
86.2% PTP1B inhibitory activity with 0.00651 mg/ml
diethylcarbamazine
-
12% inhibition at 0.2 mM
diethyldicarbonate
-
7% inhibition at 1 mM
Differentiation inducing factor 1
-
DIF-1, inhibits PTP3 by induction of serine-threonine phosphorylation of PTP3
-
dihydroabietic acid
modelling of enzyme binding
disodium 3-(((4-methyl-3-(((2-methyl-5-((3-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)benzenesulfonate
-
suramin-derivative, 50% inhibition at 0.030 mM, reversible and competitive
disodium 4-(((4-methyl-3-(((3-(((3-((2-methyl-5-((4-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)benzenesulfonate
disodium hydrogen (3-(((4-(((4-((3-(hydroxyphosphinato)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)phosphonate
DTT
-
inhibition of cytosolic enzyme form
dysidiolide
inhibits Cdc25A
EDTA
-
51% inhibition at 5 mM
ent-17-hydroxykaur-15-en-19-oic acid
40% inhibition at 0.033 mM
ent-3beta-angeloyloxykaur-16-en-19-oic acid
-
ent-3beta-tigloyloxykaur-16-en-19-oic acid
-
ent-kaur-16-en-19-oic acid
-
diterpenoid isolated from Acanthopanax koreanum, 50% inhibition at 0.020 mM
ent-kaur-9(11),16-dien-19-oic acid
29% inhibition at 0.033 mM
erylysins A
-
i.e. 3''-hydroxy-2',2'-dimethylpyrano[6',5':3,4]-2'',2''-dimethyldihydropyrano[6'',5'':9,10]pterocarpan, a pterocarpan isolated from stem bark of Erythrina lysistemon, inhibits PTPB1
erylysins B
-
i.e. furano[5',4':3,4]-9-hydroxy-10-prenylpterocarpan, a pterocarpan isolated from stem bark of Erythrina lysistemon, inhibits PTPB1
ethyl (4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-1,2,3,3a,3b,4,6,6a,7,9a,10,10a,10b,11,12,12a-hexadecahydrocyclopenta[5,6]naphtho[1,2-f]indazol-1-yl]pentanoate
-
-
ethyl (4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-8-amino-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinazolin-1-yl]pentanoate
-
-
ethyl 4-[4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenoxy]butanoate
-
-
ethyl [4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenoxy]acetate
-
-
FlAsH
the small molecule biarsenical fluorescein derivative, FlAsH, is no inhibitor of the wild-type enzyme but of the engineered WPD insertion mutant enzyme that displays FlAsH-binding cysteine residues. Inhibition of the FlAsH-sensitized TCPTP mutants is rapid and specific, and strong FlAsH sensitivity is observed in mutants that contain as few as two cysteine point mutations in their engineered WPD loops, minimization of FlAsH-binding determinants, overview
fluorescein arsenical hairpin binder
fluorescein arsenical hairpin binder does not inhibit any wild type PTP, but insertion of a fluorescein arsenical hairpin binder-binding peptide (CCPGCC) at a conserved position in the PTP catalytic-domain's WPD loop confers fluorescein arsenical hairpin binder sensitivity upon divergent PTPs
-
Glyoxal
-
93% remaining activity at 0.5 mM
glyoxalbis(N(4)-methylthiosemicarbazonato)Cu(II)
-
inhibition of protein tyrosine phosphatase activity is the prerequisite for activation of epidermal growth factor receptor by the compound, overview
hexadecanoyl-5-hydroxymethyl tetronic acid
potent irreversible inhibitor of VHR; potent irreversible inhibitor of VHR; potent irreversible inhibitor of VHR
hexasodium 8,8'-(((2E)-1,4-dioxobut-2-ene-1,4-diyl)bis(iminobenzene-3,1-diylcarbonylimino(4-methylbenzene-3,1-diyl)carbonylimino))dinaphthalene-1,3,5-trisulfonate
hexasodium 8,8'-(benzene-1,3-diylbis(carbonyliminobenzene-3,1-diylcarbonylimino(4-methylbenzene-3,1-diyl)carbonylimino))dinaphthalene-1,3,5-trisulfonate
hexasodium 8-(((2'-(((3'-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)biphenyl-2-yl)carbamoyl)amino)biphenyl-4-yl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
hexasodium 8-(((3-methyl-4-(((3-(((3-((2-methyl-4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
hexasodium 8-(((3-methyl-4-(((4-(((4-((4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
hexasodium 8-(((4-(((3-(((3-((4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
hexasodium 8-(((4-(1-methylethyl)-3-(((3-(((3-((2-(1-methylethyl)-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate
hexasodium 8-(((4-ethyl-3-(((3-(((3-((2-ethyl-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate
hexasodium 8-(((4-tert-butyl-3-(((3-(((3-((2-tert-butyl-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate
hexasodium 8-([[2-(3-[[(3-[5-[(4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl]-1H-benzimidazol-2-yl]phenyl)carbamoyl]amino]phenyl)-1H-benzimidazol-5-yl]carbonyl]amino)naphthalene-1,3,5-trisulfonate
isopimaric acid
modelling of enzyme binding
L-(+)-Tartrate
-
6.5% inhibition at 5 mM
lithocholic acid
-
natural inhibitor against PTP1B
lobaric acid
-
a depsidone-type compound, isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
lupenone
-
isolated from Sorbus commixta stem bark, inhibits PTP1B in a selective and noncompetitive manner
lupeol
-
isolated from Sorbus commixta stem bark, inhibits PTP1B in a selective and noncompetitive manner
menadione
inhibits Cdc25B irreversibly
methyl (4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-8-amino-6,6,10a,12a-tetramethyl-2,3,3a,3b,4,6,10,10a,10b,11,12,12a-dodecahydro-1H-cyclopenta[7,8]phenanthro[2,3-d][1,3]thiazol-1-yl]pentanoate
-
-
methyl (4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinoxalin-1-yl]pentanoate
-
-
methyl (6S,10S)-12-(2-chloro-3-hydroxybenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
-
methyl (6S,10S)-12-(2-fluoro-5-iodobenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
-
methyl (6S,10S)-12-(2-hydroxybenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
absolutely specific for MptpB, no inhibition of MptpA
methyl (6S,10S)-12-(3,4-dichlorobenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
absolutely specific for MptpB, no inhibition of MptpA
methyl (6S,10S)-12-(3,4-difluorobenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
-
methyl (6S,10S)-12-(3-bromo-4-fluorobenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
absolutely specific for MptpB, no inhibition of MptpA
methyl (6S,10S)-12-(3-hydroxybenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
absolutely specific for MptpB, no inhibition of MptpA
methyl (6S,10S)-12-benzyl-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
-
methyl (6S,10S)-12-[(4,6-dichloro-2H-chromen-3-yl)methyl]-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
absolutely specific for MptpB, no inhibition of MptpA
methyl (6S,10S)-12-[(4-chloro-6-fluoro-2H-chromen-3-yl)methyl]-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
absolutely specific for MptpB, no inhibition of MptpA, inhibition kinetics, overview
methyl (6S,10S)-12-[(5-chloro-1H-indol-3-yl)methyl]-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
absolutely specific for MptpB, no inhibition of MptpA
methyl (6S,10S)-12-[(5-methylfuran-2-yl)methyl]-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
absolutely specific for MptpB, no inhibition of MptpA
methyl (6S,10S)-9-hydroxy-12-(3-hydroxybenzyl)-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
-
methyl (6S,10S)-9-oxo-12-(pyridin-3-ylmethyl)-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
-
methyl 2,4-dihydroxy-6-methylbenzoate
-
isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
methyl 2-(3-(1-(4-fluorobenzyl)-6-nitro-4-oxo-1,4-dihydroquinoline-3-carboxamido)propoxy)-6-hydroxybenzoate
-
IC50 of 6.5 mg/ml
methyl 2-(3-(1-benzyl-7-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxamido)propoxy)-6-hydroxybenzoate
-
IC50 of 9.4 mg/ml
methyl 2-[4-[(4-[[ethoxy(oxo)acetyl][2-(methoxycarbonyl)phenyl]amino]-3-ethylphenylalanyl)amino]butoxy]-6-hydroxybenzoate
-
methyl 3,8-dimethoxy-11-oxo-1-pentanoyl-6-pentyl-11H-dibenzo[b,e][1,4]dioxepine-7-carboxylate
-
isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
methyl 3-formyl-2,4-dihydroxy-6-methylbenzoate
-
isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
methyl 4,4-dimethyl-3-oxochol-5-en-24-oate
-
-
methyl 4-[(benzylseleninyl)methyl]-N-(tert-butoxycarbonyl)-L-phenylalaninate
-
-
methyl 5-amino-6-(7-amino-6-methoxy-5,8-dioxo-5,8-dihydroquinolin-2-yl)-4-(2-hydroxy-3,4-dimethoxyphenyl)-3-methylpyridine-2-carboxylate
-
methyl 8-hydroxy-3-methoxy-11-oxo-1-pentanoyl-6-pentyl-11H-dibenzo[b,e][1,4]dioxepine-7-carboxylate
-
isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
methyl N-(tert-butoxycarbonyl)-4-(hydroxymethyl)-L-phenylalaninate
-
-
methyl N-(tert-butoxycarbonyl)-4-[(5R)-5-(methoxycarbonyl)-9,9-dimethyl-7-oxo-8-oxa-3-thia-2-selena-6-azadec-1-yl]-L-phenylalaninate
-
-
methyl oleanolic acid amide
-
methyl oleanolic acid ester
-
methyl-5-((3-(benzylcarbamoyl)-6-iodo-4-oxoquinolin-1(4H)-yl)methyl)-2-methoxybenzoate
-
IC50 of more than 20 mg/ml
mokko lactone
-
93.1% PTP1B inhibitory activity with 0.00141 mg/ml
mpV(pic)
-
potent and selective PTP inhibitor, inhibits SPH-1 in a dose-dependent manner
MSI-1436
small molecule inhibitor MSI-1436 binds to the disordered C-terminal domain of PTP1B, C-terminal to the catalytic domain, MSI-1436 functions using an allosteric mechanism to direct the enzymatic activity of PTP1B
N,1-dibenzyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxamide
-
41.4% inhibition at 0.02 mg/ml
N,1-dibenzyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxamide
-
61.8% inhibition at 0.02 mg/ml
N,N'-[benzene-1,4-diylbis(propane-2,2-diylbenzene-4,1-diyl)]bis(1,1,1-trifluoromethanesulfonamide)
-
-
N-((4-((E)-2-nitroethenyl)phenyl)carbonyl)glycyl-L-alpha-glutamyl-L-glutamic acid
-
50% inhibition at 0.0014 mM in absence of 2-mercaptoethanol, at 0.275 mM in presence of 1 mM 2-mercaptoethanol
N-((4-(difluoro(phosphono)methyl)phenyl)acetyl)-L-a-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide
-
inhibition of enzyme increases caveolin-1 phosphorylation
N-((4-(difluoro(phosphono)methyl)phenyl)acetyl)-L-alpha-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide
-
-
N-(1,4-dioxo-1,4-dihydronaphthalen-2-yl)-N-(4-methylphenyl)acetamide
-
N-(3-chloro-4-fluorophenyl)-2-[(6,7-dimethoxy-4-oxo-3-phenyl-3,4-dihydro-2-quinazolinyl)sulfanyl]acetamide
80% inhibition at 0.2 mM
N-(3-formylphenyl)-3-(((3-((3-formylphenyl)carbamoyl)phenyl)carbamoyl)amino)benzamide
N-(3-[(3,5-difluorobenzyl)oxy]pyridin-2-yl)-4-pentylbenzenesulfonamide
74% inhibition at 0.2 mM
N-(3-[(4-chlorophenyl)sulfanyl]-1,4-dioxo-1,4-dihydronaphthalen-2-yl)acetamide
-
N-(4-([(6-ethoxy-1,3-benzothiazol-2-yl)amino]sulfonyl)phenyl)acetamide
-
-
N-(4-([(6-methoxy-1,3-benzothiazol-2-yl)amino]sulfonyl)phenyl)acetamide
-
-
N-(4-([(6-methyl-1,3-benzothiazol-2-yl)amino]sulfonyl)phenyl)acetamide
-
-
N-(4-[[(6-nitro-1,3-benzothiazol-2-yl)amino]sulfonyl]-phenyl)acetamide
-
-
N-(6-chloro-1,3-benzothiazol-2-yl)-4-nitrobenzenesulfonamide
-
-
N-(6-ethoxy-1,3-benzothiazol-2-yl)-4-methoxybenzenesulfonamide
-
-
N-(6-ethoxy-1,3-benzothiazol-2-yl)-4-methylbenzenesulfonamide
-
-
N-(6-ethoxy-1,3-benzothiazol-2-yl)-4-nitrobenzene sulfonamide
-
linear mixed-type inhibition, shows in vivo antihyperglycemic activity
N-(6-ethoxy-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
N-(6-fluoro-1,3-benzothiazol-2-yl)-4-nitrobenzenesulfonamide
-
-
N-(6-methoxy-1,3-benzothiazol-2-yl)-4-methylbenzenesulfonamide
-
-
N-(6-methoxy-1,3-benzothiazol-2-yl)-4-nitrobenzenesulfonamide
-
-
N-(6-methoxy-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
N-(6-methyl-1,3-benzothiazol-2-yl)-4-nitrobenzenesulfonamide
-
linear mixed-type inhibition, shows in vivo antihyperglycemic activity
N-(6-methyl-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
N-([4-[difluoro(phosphono)methyl]phenyl]acetyl)-a-aspartyl-4-[difluoro(phosphono)methyl]phenylalaninamide
-
-
N-1-(2-[(2-oxo-4-propyl-2H-chromen-7-yl)oxy]propanoyl)-3-(trifluoromethyl)benzene-1-sulfonohydrazide
84% inhibition at 0.2 mM
N-benzoyl-L-glutamyl-[4-phosphono(difluoromethyl)]-L-phenylalanineamide
-
i.e. BzN-EJJ-amide, 50% inhibition at 4 nM
N-benzyl-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxamide
-
0.2% inhibition at 0.02 mg/ml; 7.4% inhibition at 0.02 mg/ml
N-benzyl-1-cyclopropyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxamide
-
6.1% inhibition at 0.02 mg/ml
n-dodecyl trimethylammonium bromide
-
pH 7.0, inactivation at concentration 10fold higher than critical micellar concentration
n-hexadecyl trimethylammonium bromide
-
pH 7.0, inactivation at concentration 10fold higher than critical micellar concentration
N-Methylmaleimide
-
76.3% inhibition at 0.5 mM
n-tetradecyl trimethylammonium bromide
-
pH 7.0, inactivation at concentration 10fold higher than critical micellar concentration
N-[4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenyl]-4-tert-butylbenzamide
-
-
N-[5-(dimethylamino)-2-hydroxy-3-methoxybenzyl]-N-methyl-2-(4-nitrophenyl)ethanaminium
-
N-[6-chloro-5-(2,3-dichlorophenoxy)-1-methyl-1H-benzimidazol-2-yl]acetamide
70% inhibition at 0.2 mM
N-[6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazol-2-yl]-2,2,2-trifluoroacetamide
mixed-type inhibition, 92% inhibition at 0.2 mM
N2-(2-((2-((N-((4-(difluoro(phosphono)methyl)phenyl)acetyl)-L-alpha-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalanyl)amino)ethyl)disulfanyl)ethyl)-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-argininamide
-
in presence of 5-50 nM, 11-35% decrease in cell spreading, 24% decrease in number of migratory cells, dose-dependent increase in Y527 phosphorylation of Src
Na+/K+ tartrate
-
20% residual activity in ovary and 2% residual activity in haemolymph at 10 mM
NO
-
inactivation, phosphate protects
nocardione A
inhibits Cdc25B
nocardione B
inhibits Cdc25B
NSC-87877
-
potent Shp2 and Shp1 inhibitor
p-chloromercuribenzoate
-
lung enzyme
p-hydroxymercuribenzoate
-
p-nitrocatechol sulfate
-
competitive inhibitor
PAO
complete inhibition at 0.0.5 mM
papaverine
binding structure, molecular modeling, overview
peracetic acid
-
a potent, time-dependent inactivator of the catalytic subunit of PTP1B, treatment of the enzyme with 0.015 mM for 15 sec inactivates 88% of the enzyme, inactivation of PTP1B by peracetic acid can be reversed by treatment of the enzyme with thiols
phenyl vinyl sulfonate
-
phenyl vinyl sulfonate-mediated PTP inactivation is active site-directed and irreversible
phenyl vinyl sulfone
-
phenyl vinyl sulfone-mediated PTP inactivation is active site-directed and irreversible
phenylhydrazonopyrazolone sulfonate 1
-
potent, active site-directed small molecule inhibitor which is specific for Shp2 over the closely related tyrosine phosphatases Shp1 and PTP1B
phenylhydrazonopyrazolone sulfonate 4
-
the most potent inhibitor of Shp2 which shows a specificity profile similar to phenylhydrazonopyrazolone sulfonate 1
potassium bisperoxo(1,10-phenanthroline)oxovanadate
potassium bisperoxo(1,10-phenanthroline)oxovanadate(V)
-
i.e. [bpV(phen)], the peroxovanadium compound is a stable, potent and selective protein tyrosine phosphatase inhibitor. It protects dorsal column sensory axons and white matter and rescues sensory-evoked potentials in vivo after treatement with PTP or spinal cord injury, overview
propanal
-
93% remaining activity at 0.5 mM
pterokaurene L3
no inhibition at 0.031 mM
regucalcin
-
regulatory protein in intracellular signaling
-
rilobolide-6-O-methacrylate
no inhibition at 0.026 mM
S-nitrosoglutathione
-
S-nitrosoglutathione treatment decreases the catalytic activity parameters of PtpA by half
SK7
-
a metal chalcone, complete inhibition at 0.02 mM
small t antigen
-
small t antigen of DNA tumor virus SV40 inhibits the phosphatase activity of the PP2A core enzyme
-
sodium decylsulfate
-
at concentration 10fold lower than critical micellar concentration, complete inactivation. Inactivation is independent of pH-value, irreversible and not affected by NaCl. Presence of phosphate protects
Sodium diphosphate
-
both isoforms, inhibition by millimolar concentrations
sodium dodecylsulfate
-
at concentration 10fold lower than critical micellar concentration, complete inactivation. Inactivation is independent of pH-value, irreversible and not affected by NaCl. Presence of phosphate protects
sodium octylsulfate
-
at concentration 10fold lower than critical micellar concentration, complete inactivation. Inactivation is independent of pH-value, irreversible and not affected by NaCl. Presence of phosphate protects
sodium pervanadate
-
broad-acting tyrosine phosphatase inhibitor
Sodium tetradecylsulfate
-
at concentration 10fold lower than critical micellar concentration, complete inactivation. Inactivation is independent of pH-value, irreversible and not affected by NaCl. Presence of phosphate protects
sodium tungstate
-
complete inhibition of enzyme isolated from metacyclic stage, 50% inhibition of enzyme from procyclic stage
stevastelin
inhibits VHR; inhibits VHR; inhibits VHR
sulfircin
inhibits Cdc25A
Tartrate
-
both SynPPP1 and SYnPPM3
tetramisole
-
both SynPPP1 and SYnPPM3
tetrasodium 2-(((2-(3-(((3-(5-((2,5-disulfonatophenyl)carbamoyl)-1H-benzimidazol-2-yl)phenyl)carbamoyl)amino)phenyl)-1H-benzimidazol-5-yl)carbonyl)amino)benzene-1,4-disulfonate
tetrasodium 4,4'-(benzene-1,3-diylbis(carbonylimino))dinaphthalene-2,6-disulfonate
tetrasodium 4,4'-(benzene-1,3-diylbis(carbonyliminobenzene-4,1-diylcarbonylimino))dinaphthalene-2,6-disulfonate
tetrasodium 4-(((3-(((3,5-bis((4-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)amino)-5-((4-sulfonatophenyl)carbamoyl)phenyl)carbonyl)amino)benzenesulfonate
tetrasodium 4-(((3-(((5-((4,8-disulfonatonaphthalen-1-yl)carbamoyl)-2-methylphenyl)carbamoyl)amino)-4-methylphenyl)carbonyl)amino)naphthalene-1,5-disulfonate
Trifluoperazine
-
complete inhibition of enzyme isolated from metacyclic stage, 18% inhibition of enzyme from procyclic stage
trilobolide-6-O-isobutyrate
no inhibition at 0.026 mM
VO3N3
-
oxovanadium(IV) is coordinated with one nitrogen and two oxygen atoms from the Schiff base and two nitrogen atoms from the bidentate planar ligands, in a distorted octahedral geometry, VO3N3
wedelolide D
32% inhibition at 0.020 mM
wedelolide H
no inhibition at 0.023 mM
wedelolide I
no inhibition at 0.021 mM
wedelolide J
no inhibition at 0.021 mM
[(1-benzyl-1H-indazol-5-yl)(difluoro)methyl]phosphonic acid
-
[(2-benzyl-2H-indazol-5-yl)(difluoro)methyl]phosphonic acid
-
[(4-bromophenyl)(difluoro)methyl]phosphonic acid
-
[(4-[(4E)-2-(1H-benzotriazol-1-yl)-2-[4-(methoxycarbonyl)phenyl]-5-phenylpent-4-en-1-yl]phenyl)(difluoro)methyl]phosphonic acid
-
[(4-[[3,5-bis(trifluoromethyl)phenyl]carbamoyl]phenyl)(difluoro)methyl]phosphonic acid
-
[(4-[[4-bromo-3,5-bis(trifluoromethyl)phenyl]carbamoyl]phenyl)(difluoro)methyl]phosphonic acid
selectivity with different PTPs, overview
[(4-[[4-bromo-3-(trifluoromethyl)phenyl]carbamoyl]phenyl)(difluoro)methyl]phosphonic acid
-
[(4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl]phenyl)(difluoro)methyl]phosphonic acid
-
[(BzMeIm)Au(I)Cl]
Yersinia enterolytica
-
-
[(MeIm)Au(I)Cl]
Yersinia enterolytica
-
-
[(MeMeIm)Au(I)Cl]
Yersinia enterolytica
-
-
[(p-MeBzMeIm)Au(I)Cl]
Yersinia enterolytica
-
-
[2-bromo-4-[(E)-(7,8-dimethyl-3-oxo[1,3]thiazolo[3,2-a]benzimidazol-2(3H)-ylidene)methyl]-6-ethoxyphenoxy]acetic acid
irreversible inhibition
[4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenoxy]acetic acid
-
-
[biphenyl-4-yl(difluoro)methyl]phosphonic acid
-
[difluoro(4-nitrophenyl)methyl]phosphonic acid
-
[difluoro(4-[[2-(trifluoromethyl)phenyl]carbamoyl]phenyl)methyl]phosphonic acid
-
[difluoro(4-[[3-(trifluoromethyl)phenyl]carbamoyl]phenyl)methyl]phosphonic acid
-
[difluoro(4-[[4-(trifluoromethyl)phenyl]carbamoyl]phenyl)methyl]phosphonic acid
-
[difluoro(4-[[4-fluoro-3-(trifluoromethyl)phenyl]carbamoyl]phenyl)methyl]phosphonic acid
-
[difluoro[3-(phenylcarbamoyl)phenyl]methyl]phosphonic acid
-
[difluoro[4-(1,3-thiazol-2-ylcarbamoyl)phenyl]methyl]phosphonic acid
-
[difluoro[4-(1-methyl-1H-pyrazol-4-yl)phenyl]methyl]phosphonic acid
-
[difluoro[4-(methylcarbamoyl)phenyl]methyl]phosphonic acid
-
[difluoro[4-(phenoxymethyl)phenyl]methyl]phosphonic acid
-
[difluoro[4-(phenylcarbamoyl)phenyl]methyl]phosphonic acid
-
[difluoro[4-(phenylsulfamoyl)phenyl]methyl]phosphonic acid
-
[difluoro[4-(propan-2-ylcarbamoyl)phenyl]methyl]phosphonic acid
-
[RuIII(EDTA)(OH2/OH)]1-/2-
-
RuIII-EDTA inhibits PTP, like vanadate, through an oxidant-independent pathway. It inhibits PTP at physiological pH values by a mechanism that involves binding of the Cys residue of the catalytic domain of the enzyme, overview. At pH 7.4, the Ru-EDTA complex exists as a mixture of aqua and hydroxo-species. The inhibition is reversible or inhibited by glutathione
-
[[1-(4-chlorophenyl)-2-methyl-1H-indol-5-yl]oxy]acetic acid
-
[[4'-(2-butyl-1-benzofuran-3-yl)biphenyl-4-yl]oxy]acetic acid
-
[[4-(1H-benzimidazol-2-ylcarbamoyl)phenyl](difluoro)methyl]phosphonic acid
-
[[4-(benzoylamino)phenyl](difluoro)methyl]phosphonic acid
-
[[4-(benzylcarbamoyl)phenyl](difluoro)methyl]phosphonic acid
-
[[4-([[3,5-bis(trifluoromethyl)phenyl]carbamoyl]amino)phenyl](difluoro)methyl]phosphonic acid
-
[[4-[(1-ethylpiperidin-4-yl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid
-
[[4-[(2-bromophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid
-
[[4-[(2-chlorophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid
-
[[4-[(3-bromophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid
-
[[4-[(3-chlorophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid
-
[[4-[(4-bromophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid
-
[[4-[(4-chlorophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid
-
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
-
-
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
no inhibition of LMW-PTP isozymes, but 20% inhibition of PTP-B1 at 0.02 mM
1-ethyl-6-methyl-3-phenyl-1H-pyrimido(5,4-e)(1,2,4)triazine-5,7-dione
-
covalent mode of action
1-ethyl-6-methyl-3-phenyl-1H-pyrimido(5,4-e)(1,2,4)triazine-5,7-dione
-
covalent mode of action
2,2-dioxo-2,3-dihydro-2-OMEGA-16-benzo (1,2,3)oxathiazole-6-carboxylic acid (5-phenylsulfanyl-1H-benzoimidazol-2-ylmethyl)-amide
-
competitive, noncovalent mode of action
2,2-dioxo-2,3-dihydro-2-OMEGA-16-benzo (1,2,3)oxathiazole-6-carboxylic acid (5-phenylsulfanyl-1H-benzoimidazol-2-ylmethyl)-amide
-
competitive, noncovalent mode of action
Ag+
-
16.6% inhibition at 2 mM
Ag+
-
62% inhibition at 2.5 mM
Ammonium molybdate
-
complete inhibition of enzyme isolated from metacyclic stage, 75% inhibition of enzyme from procyclic stage
Ammonium molybdate
-
4% residual activity in ovary and no activity in haemolymph at 1 mM
Ammonium molybdate
-
98% inhibition at 2 mM
Ammonium molybdate
-
strong inhibition
auranofin
-
inhibition of cysteine-dependent protein tyrosine phosphatases
auranofin
Yersinia enterolytica
-
inhibition of cysteine-dependent protein tyrosine phosphatases
BzN-EJJ-amide
50% inhibition at 3.7 nM for wild-type, at 18 nM for mutant S295F
BzN-EJJ-amide
-
50% inhibition at 8nM for wild-type PTP-1B, at 14 nM for PTP-1B mutant V113I, at 7 nM for mutant M114V, at 7 nM for mutant V113I/M114V, at 11 nM for mutant G117E, at 12 nM for mutant L119V
Ca2+
-
-
CinnGel 2ME
-
30.2% inhibition at 0.02 mM
CinnGel 2ME
-
the free cinnamic acid component of CinnGEL 2Me inhibits PTP1B
Cu2+
-
lung enzyme
Cu2+
Bracoviriform demolitoris
-
-
Cu2+
-
32.2% inhibition at 2 mM
dephostatin
-
complete inhibition of enzyme isolated from metacyclic stage, 28% inhibition of enzyme from procyclic stage
diphosphate
-
1 mM, 31% residual activity
disodium 4-(((4-methyl-3-(((3-(((3-((2-methyl-5-((4-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)benzenesulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.010 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
disodium 4-(((4-methyl-3-(((3-(((3-((2-methyl-5-((4-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)benzenesulfonate
-
suramin-derivative, 50% inhibition at 0.012mM, reversible and competitive
disodium hydrogen (3-(((4-(((4-((3-(hydroxyphosphinato)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)phosphonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.0096 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
disodium hydrogen (3-(((4-(((4-((3-(hydroxyphosphinato)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)phosphonate
-
suramin-derivative, 50% inhibition above 0.1 mM, reversible and competitive
dithiothreitol
-
dithiothreitol
complete inhibition at 1.8 mM
Fe2+
-
lung enzyme
Fe2+
-
34.5% inhibition at 2 mM
H2O2
-
inactivation, phosphate protects, mechanism, overview
H2O2
-
the enzyme can be more rapidly inactivated by H2O2 in the absence of EDTA
H3VO4
-
-
H3VO4
-
no effect on PTP-I but PTP-III inhibited
heparin
Bracoviriform demolitoris
-
-
hexasodium 8,8'-(((2E)-1,4-dioxobut-2-ene-1,4-diyl)bis(iminobenzene-3,1-diylcarbonylimino(4-methylbenzene-3,1-diyl)carbonylimino))dinaphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.005 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8,8'-(((2E)-1,4-dioxobut-2-ene-1,4-diyl)bis(iminobenzene-3,1-diylcarbonylimino(4-methylbenzene-3,1-diyl)carbonylimino))dinaphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition at 0.008mM, reversible and competitive
hexasodium 8,8'-(benzene-1,3-diylbis(carbonyliminobenzene-3,1-diylcarbonylimino(4-methylbenzene-3,1-diyl)carbonylimino))dinaphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.0023 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8,8'-(benzene-1,3-diylbis(carbonyliminobenzene-3,1-diylcarbonylimino(4-methylbenzene-3,1-diyl)carbonylimino))dinaphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition at 0.0015M, reversible and competitive
hexasodium 8-(((2'-(((3'-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)biphenyl-2-yl)carbamoyl)amino)biphenyl-4-yl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.070 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-(((2'-(((3'-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)biphenyl-2-yl)carbamoyl)amino)biphenyl-4-yl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition at 0.020 mM, reversible and competitive
hexasodium 8-(((3-methyl-4-(((3-(((3-((2-methyl-4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.0037 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-(((3-methyl-4-(((3-(((3-((2-methyl-4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition at 0.007 mM, reversible and competitive
hexasodium 8-(((3-methyl-4-(((4-(((4-((4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.0021 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-(((3-methyl-4-(((4-(((4-((4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition at 0.0028mM, reversible and competitive
hexasodium 8-(((4-(((3-(((3-((4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.0016 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-(((4-(((3-(((3-((4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition at 0.002mM, reversible and competitive
hexasodium 8-(((4-(1-methylethyl)-3-(((3-(((3-((2-(1-methylethyl)-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.009 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-(((4-(1-methylethyl)-3-(((3-(((3-((2-(1-methylethyl)-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate
-
suramin-derivative, 50% inhibition at 0.013M, reversible and competitive
hexasodium 8-(((4-ethyl-3-(((3-(((3-((2-ethyl-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.009 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-(((4-ethyl-3-(((3-(((3-((2-ethyl-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate
-
suramin-derivative, 50% inhibition at 0.011M, reversible and competitive
hexasodium 8-(((4-tert-butyl-3-(((3-(((3-((2-tert-butyl-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.007 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-(((4-tert-butyl-3-(((3-(((3-((2-tert-butyl-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.013M, reversible and competitive
hexasodium 8-([[2-(3-[[(3-[5-[(4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl]-1H-benzimidazol-2-yl]phenyl)carbamoyl]amino]phenyl)-1H-benzimidazol-5-yl]carbonyl]amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.00049 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-([[2-(3-[[(3-[5-[(4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl]-1H-benzimidazol-2-yl]phenyl)carbamoyl]amino]phenyl)-1H-benzimidazol-5-yl]carbonyl]amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition at 0.00009M, reversible and competitive
iodoacetic acid
-
-
iodoacetic acid
-
complete inhibition at 1.0 mM
ISIS 113715
-
PTP-1B antisense oligonucleotide ISIS 113715 dose-dependently inhibits PTP-1B mRNA and protein expression, although ISIS 113715 reduces PTP-1B protein levels by greater than 90%, no effects are observed on protein levels of TC-PTPase
-
ISIS 113715
-
PTP-1B antisense oligonucleotide ISIS 113715 administration reduces PTP-1B mRNA expression in both liver and adipose tissue by 40-50% but does not affect muscle PTP-1B expression
-
JTT-551
-
i.e. monosodium (([5-(1,1-dimethylethyl)thiazol-2-yl]methyl)([(4-(4-[4-(1-propylbutyl)phenoxy]methyl)phenyl)thiazol-2-yl]methyl)amino)acetate, a specific protein tyrosine phosphatase 1B inhibitor in vitro and in vivo, mixed-type inhibition mode versus PTPB1, overview
JTT-551
-
i.e. monosodium (([5-(1,1-dimethylethyl)thiazol-2-yl]methyl)([(4-(4-[4-(1-propylbutyl)phenoxy]methyl)phenyl)thiazol-2-yl]methyl)amino)acetate, a specific protein tyrosine phosphatase 1B inhibitor in vitro and in vivo, mixed-type inhibition mode versus PTPB1, overview. The inhibitor shows a hypoglycaemic effect in ob/ob mice, overview
JTT-551
-
i.e. monosodium (([5-(1,1-dimethylethyl)thiazol-2-yl]methyl) ([(4-(4-[4-(1-propylbutyl)phenoxy]methyl)phenyl)thiazol-2-yl]methyl)amino)acetate, a specific protein tyrosine phosphatase 1B inhibitor in vitro and in vivo, mixed-type inhibition mode versus PTPB1, overview. The inhibitor shows a hypoglycaemic effect in rat L6 cells, overview
L-Tartrate
-
no inhibition of lung enzyme
L-Tartrate
-
no inhibition of platelet enzyme
maslinic acid
-
poor inhibition by the isomers 3-epi-maslinic acid and augustic acid
Mg2+
-
-
Mn2+
-
-
Mn2+
-
no inhibition of platelet enzyme
molybdate
-
-
molybdate
competitive inhibition
molybdate
-
92.2% inhibition at 5 mM
molybdate
-
no effect on PTP-I, PTP-III inhibited
molybdate
-
competitive inhibition
N-(3-formylphenyl)-3-(((3-((3-formylphenyl)carbamoyl)phenyl)carbamoyl)amino)benzamide
-
suramin-derivative, 50% inhibition of PTP1B above 0.1 mM, reversible and competitive. Not inhibitory to PTPalpha, CD45 or LAR
N-(3-formylphenyl)-3-(((3-((3-formylphenyl)carbamoyl)phenyl)carbamoyl)amino)benzamide
-
suramin-derivative, 50% inhibition above 0.1 mM, reversible and competitive
N-ethylmaleimide
-
-
N-ethylmaleimide
-
both isozymes, 50% inhibition at 7 mM
Na3VO4
-
-
NaCl
-
increase in Km-value with increase of ionic strength, 10-fold increase of Km-value from 0 to 200 mM NaCl
NaCl
-
inhibits activity with 4-nitrophenyl phosphate
NaCl
inhibits the catalytic domain by 60% at 2 M
NaF
-
1 mM, 85% residual activity
NaF
-
no inhibition of lung enzyme
NaF
-
no inhibition of platelet enzyme
NaF
-
16% residual activity in ovary and no activity in haemolymph at 10 mM
NaF
-
moderate inhibition, both SynPPP1 and SYnPPM3
o-vanadate
Na3VO4, complete inhibition at 0.6 mM
o-vanadate
-
both SynPPP1 and SYnPPM3
okadaic acid
-
complete inhibition of enzyme isolated from metacyclic stage, 35% inhibition of enzyme from procyclic stage
okadaic acid
-
7.5% inhibition at 0.01 mM
okadaic acid
-
both SynPPP1 and SYnPPM3
oleanolic acid
-
orthovanadate
-
-
orthovanadate
competitive inhibitor
orthovanadate
-
inhibition of protein tyrosine phosphatase activity
orthovanadate
-
24.5% inhibition at 5 mM
orthovanadate
Q6JHV2
50% inhibition at 0.075 mM
pervanadate
-
-
pervanadate
-
pervanadate inhibits PTP by irreversibly oxidizing the catalytic cysteine of PTP
Phenylarsine oxide
-
specific inhibitor of protein Tyr phosphatase activity
Phenylarsine oxide
-
55.8% inhibition at 0.01 mM
Phenylarsine oxide
-
a specific PTP inhibitor, 79% inhibition at 1.0 nM
phosphate
-
-
phosphate
inhibits the phosphatase activity, but not the sugar hydrolase activity; inhibits the phosphatase activity, but not the sugar hydrolase activity
phosphate
-
38% residual activity in ovary and 3% residual activity in haemolymph at 10 mM
phosphotyrosine
-
-
PO43-
-
treatment of the enzyme with 0.05 mM PO43- for 15 sec inactivates 49% of the enzyme
potassium bisperoxo(1,10-phenanthroline)oxovanadate
-
-
potassium bisperoxo(1,10-phenanthroline)oxovanadate
-
complete inhibition at 0.01 mM
potassium bisperoxo(1,10-phenanthroline)oxovanadate
-
-
potassium bisperoxo(1,10-phenanthroline)oxovanadate
-
potent PTP inhibitor
RK-682
-
-
RK-682
-
98.5% PTP1B inhibitory activity with 0.0012 mg/ml
Sodium fluoride
NaF, 30% inhibition at 5 mM, no inhibition at 1-3 mM
Sodium fluoride
-
96% inhibition at 2 mM
sodium orthovanadate
-
17.5% inhibition at 1 mM
sodium orthovanadate
-
a broad-range PTP inhibitor, abrogated Cr(VI)-induced clonogenic lethality
sodium orthovanadate
-
complete inhibition of enzyme isolated from metacyclic stage, 30% inhibition of enzyme from procyclic stage
sodium orthovanadate
-
20% residual activity in ovary and 13% residual activity in haemolymph at 0.1 mM
sodium orthovanadate
-
shows dose-dependent inhibition of PRL activity
sodium orthovanadate
-
99.5% inhibition at 0.05 mM
sodium orthovanadate
-
both isozymes, 50% inhibition at 3 mM
sodium orthovanadate
-
strong inhibition
Sodium vanadate
-
1 mM, 60-80% inhibition
Sodium vanadate
a PTP inhibitor targeting the catalytic site pocket. Vanadate is anchored in the active site of Tk-PTP(form II), stabilized by electrostatic interaction with the guanidinium group of Arg109 and by its oxygen atom-mediated hydrogen bonds with the main chain amides of Met94, Gly95, Leu97, Gly98, and Arg99. The Tk-PTP(form II) P-loop is structurally similar to those of catalytically active DUSP proteins
suramin
-
50% inhibition of PTP1B at 0.011 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
suramin
-
50% inhibition at 0.007M, reversible and competitive
tetrasodium 2-(((2-(3-(((3-(5-((2,5-disulfonatophenyl)carbamoyl)-1H-benzimidazol-2-yl)phenyl)carbamoyl)amino)phenyl)-1H-benzimidazol-5-yl)carbonyl)amino)benzene-1,4-disulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.00025 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
tetrasodium 2-(((2-(3-(((3-(5-((2,5-disulfonatophenyl)carbamoyl)-1H-benzimidazol-2-yl)phenyl)carbamoyl)amino)phenyl)-1H-benzimidazol-5-yl)carbonyl)amino)benzene-1,4-disulfonate
-
suramin-derivative, 50% inhibition at 0.0007mM, reversible and competitive
tetrasodium 4,4'-(benzene-1,3-diylbis(carbonylimino))dinaphthalene-2,6-disulfonate
-
suramin-derivative, 50% inhibition of PTP1B above 0.1 mM, reversible and competitive. Not inhibitory to PTPalpha, CD45 or LAR
tetrasodium 4,4'-(benzene-1,3-diylbis(carbonylimino))dinaphthalene-2,6-disulfonate
-
suramin-derivative, 50% inhibition above 0.1 mM, reversible and competitive
tetrasodium 4,4'-(benzene-1,3-diylbis(carbonyliminobenzene-4,1-diylcarbonylimino))dinaphthalene-2,6-disulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.08 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
tetrasodium 4,4'-(benzene-1,3-diylbis(carbonyliminobenzene-4,1-diylcarbonylimino))dinaphthalene-2,6-disulfonate
-
suramin-derivative, 50% inhibition at 0.045 mM, reversible and competitive
tetrasodium 4-(((3-(((3,5-bis((4-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)amino)-5-((4-sulfonatophenyl)carbamoyl)phenyl)carbonyl)amino)benzenesulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.0045 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
tetrasodium 4-(((3-(((3,5-bis((4-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)amino)-5-((4-sulfonatophenyl)carbamoyl)phenyl)carbonyl)amino)benzenesulfonate
-
suramin-derivative, 50% inhibition at 0.005mM, reversible and competitive
tetrasodium 4-(((3-(((5-((4,8-disulfonatonaphthalen-1-yl)carbamoyl)-2-methylphenyl)carbamoyl)amino)-4-methylphenyl)carbonyl)amino)naphthalene-1,5-disulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.070 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
tetrasodium 4-(((3-(((5-((4,8-disulfonatonaphthalen-1-yl)carbamoyl)-2-methylphenyl)carbamoyl)amino)-4-methylphenyl)carbonyl)amino)naphthalene-1,5-disulfonate
-
suramin-derivative, 50% inhibition at 0.0042 mM, reversible and competitive
tungstate
competitive inhibition
tungstate
-
16.3% inhibition at 20 mM
tungstate
-
competitive inhibition
ursolic acid
-
50% inhibition at 0.0038 mM, competitive inhibition
ursolic acid
-
99% PTP1B inhibitory activity with 0.0007 mg/ml
vanadate
-
competitive, 1 mM, 11% residual activity
vanadate
Bracoviriform demolitoris
-
-
vanadate
the equatorial vanadate oxygen atoms bind to the P-loop and assumes a trigonal bipyramidal geometry in both transition state analogue structures, with very similar apical O-O distances, binding structure, overview
vanadate
-
enzyme inhibition by vanadate takes place through an oxidant-independent pathway, the inhibition is reversible with EDTA
Zn2+
-
-
Zn2+
low nanomolar Zn2+ concentrations inhibit isoform PTB1Bll
Zn2+
-
75.2% inhibition at 5 mM
Zn2+
-
65.5% inhibition at 2.5 mM
Zn2+
-
Zn2+ inhibits the enzyme irreversibly in a concentration-dependent manner
additional information
Bracoviriform demolitoris
-
the enzyme activity is diminished by increasing acetate buffer ionic strength, but PTP-H2 is unaffected by tetramisole and levamisole, as well as by okadaic acid, sodium fluoride and sodium citrate
-
additional information
-
hyperosmotic stress inhibits PTP3. Overexpression of a dominant inhibitor of PTP3 leads to constitutive tyrosine phosphorylation and ectopic nuclear localisation of STATc
-
additional information
-
overview on recently developed inhibitors
-
additional information
-
inhibition data for isoforms CD45, Cdc25A, VHR; not inhibitory to PTP1B, CD45: disodium 3-(((4-methyl-3-(((2-methyl-5-((3-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)benzenesulfonate
-
additional information
-
enzyme is active in unstimulated or thrombin-stimulated platelets. Enzyme is not active in lysate of platelets adherent to fibrinogen
-
additional information
-
down-regulation of enzyme activity with small molecule inhibitors suppresses cell spreading and migration to fibronectin, increases Y527 phosphorylation in Src, and decreases phosphorylation of focal adhesion kinase, p130 Crk-associated substrate, and extracellular signal-regulated kinase 1/2
-
additional information
-
the presence of the superoxide- and hydrogen peroxide-destroying enzymes superoxide dismutase and catalase has no effect on the rate of the inactivation reaction
-
additional information
-
tert-butyl hydroperoxide cumene hydroperoxide do not inactivate PTP1B, 150 nM H2O2 has no measurable effect on enzyme activity
-
additional information
-
3alpha,24,29-trihydroxyolean-12-en-28-oic acid, 3alpha,19alpha-dihydroxyurs-12,20(30)-dien-24,28-dioic acid, and 3alpha,19alpha-dihydroxyurs-12-en-24,28-dioic acid show very weak inhibitory effect towards PTP1B
-
additional information
-
not inhibited by costunolide, 11beta,13-dihydrocostunolide, reynosin, 1beta-hydroxy arbusculin A, santamarine, alpha-costol, beta-sitosterol, aplotaxene, and alpha-amyrin stearate
-
additional information
no inhibition by EDTA at 1 mM
-
additional information
structure derivatives, derived from papaverine, e.g. Pnu177496, in docking simulations, simulated molecular docking method, overview
-
additional information
-
structure derivatives, derived from papaverine, e.g. Pnu177496, in docking simulations, simulated molecular docking method, overview
-
additional information
-
inhibitor synthesis, inhibitor selectivity for PTP1B over TCPTP, overview
-
additional information
structure-based optimization of benzoic acids as inhibitors of PTPB1 and LMW-PTP, molecular docking study using crystal structures of PTPB1, PDB ID 1G7G and 1XBO, as templates, overview
-
additional information
-
synthesis of series of oxovanadium complexes with mixed ligands, a tridentate ONO-donor Schiff base ligand with salicylidene anthranilic acid, and a bidentate NN ligand, e.g., 2,2'-bipyridine, 1,10-phenanthroline, dipyrido[3,2-d:2',3'-f]quinoxaline, dipyrido[3,2-a:2',3'-c]phenazine, or 7-methyldipyrido[3,2-a:2',3'-c]phenazine, spectroscopical analysis, and crystal structures of complexes bound to PTPB1, molecular modeling, overview
-
additional information
-
mechanism of substrate selectivity of five bidentate inhibitors, NNY, B07, F6Z, Q1M, and PYN, for PTP1B, compared to SHP-2 and TCPTP, using molecular dynamics simulations and free energy calculations, and crystal structures with PDB IDs 1NNY, 2B07, 2F6Z, 1Q1M, and 1PYN, 1L8k, and 2SHP, overview. Residues Arg24, Arg254, and Gln262 in the second binding site of PTP1B are essential for the high selectivity of inhibitors
-
additional information
-
inhibitory potency of gold(I) complexes containing N-heterocyclic carbene ligands versus cysteine-dependent protein tyrosine phosphatases, reversible inhibition, overview
-
additional information
-
bis(thiosemicarbazonato) metal complexes, e.g. with Cu2+ or Zn2+, inhibit PTP and its dephophorylating and inhibitory activity on the epidermal growth factor receptor, EGFR
-
additional information
-
the substitution of prenyl groups on pterocarpans might be important for in vitro PTP1B inhibitory activity, and hydroxyl group attached to C-6a or an aldehyde group attached to C-8 may decrease this activity. No inhibition by erylysins C, i.e. 8-formyl-3,9-dihydroxy-4,10-diprenylpterocarpan, by cristacarpin, and by erystagallin C
-
additional information
-
development of a rapid high-throughput screening method for PTP inhibitors, overview
-
additional information
-
design, synthesis and evaluation of a series of bromo-retrochalcones as PTP1B inhibitors based on licochalcone A and E, overview
-
additional information
not inhibited by H2O2 treatment
-
additional information
-
not inhibited by H2O2 treatment
-
additional information
-
not inhibited by camelliaolean A and camelliaolean B
-
additional information
structure-based drug design
-
additional information
-
structure-based drug design
-
additional information
IPTG and lactose inhibit the sugar hydrolase activity of the enzyme PTPRdelta
-
additional information
IPTG and lactose inhibit the sugar hydrolase activity of the enzyme PTPRdelta
-
additional information
no autoinhibition
-
additional information
abietane-type diterpenoids inhibit protein tyrosine phosphatases by stabilizing an inactive enzyme conformation. Abietane-type diterpenoids, a biologically active class of phytometabolites with largely nonpolar structures, are used for the development of pharmaceutically relevant PTP inhibitors. Minor changes in the structures of abietane-type diterpenoids (e.g. the addition of hydrogens) can improve potency (i.e. lower IC50) by several fold. Trodusquemine and benzofuran derivatives bind to C-terminal allosteric sites that attenuate WPD loop dynamics. Mechanisms of inhibition, dynamic docking, modelling, overview
-
additional information
design and synthesis of azolyl flavonoids as enzyme inhibitors of protein tyrosine phosphatase 1B, molecular modeling and dynamics studies, using the crystal structure of PTP1B (PDB ID 1G1H) reveals the selectivity of triazolyl flavonoid inhibitor 7-(2-(1H-1,2,4-triazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one for PTP1B over the closely related T-cell protein tyrosine phosphatase (TCPTP), detailed overview. The inhibitory effects and kinetics analysis of the azoyl flavonoids against PTPs are measured, using 4-nitrophenol phosphate as the substrate
-
additional information
the active sites of PTPs are exceptionally conserved and charged, making it nearly impossible to develop PTP inhibitors that are selective. But targeting PTP protein (substrate/regulatory) interaction sites, which are distal from the active sites, are highly viable and suitable drug targets. Domains outside PTP catalytic domains have also been demonstrated to directly alter PTP activity. Development of drugs that bind to intrinsically disordered regions of the enzyme, overview
-
additional information
design of non-natural allosteric-inhibition sites in PTPs, in which a tricysteine moiety is engineered within the PTP catalytic domain at a conserved location outside of the active site. Introduction of the tricysteine motif, which does not exist in any wild-type PTP, serves to sensitize target PTPs to inhibition by a biarsenical compound, providing a generalizable strategy for the generation of allosterically sensitized (as) PTPs. Biarsenical reagents as enzyme inhibitors, overview. Enzyme asPTP catalytic domains have differing biarsenical sensitivities, with some being most potently inhibited by biarsenical compounds with large interarsenical distances, whereas others prefer compounds with relatively small interarsenical distances. AsCy3 is an optimized inhibitor of of engineered enzyme asPTP1B
-
additional information
identification of a benzo imidazole thiazole derivative as the specific irreversible inhibitor of protein tyrosine phosphatase, overview
-
additional information
-
identification of a benzo imidazole thiazole derivative as the specific irreversible inhibitor of protein tyrosine phosphatase, overview
-
additional information
wedelolide derivatives and structure-activity relationships of protein tyrosine phosphatase 1B inhibitory ent-kaurene diterpenes, determination and analysis of inhibitors isolated from aerial parts of Wedelia prostrata collected in Manado (Indonesia) and Wedelia chinensis collected on Iriomote Island (Okinawa, Japan). For inhibitory assays, 4-nitrophenyl phosphate is used as enzyme substrate
-
additional information
-
wedelolide derivatives and structure-activity relationships of protein tyrosine phosphatase 1B inhibitory ent-kaurene diterpenes, determination and analysis of inhibitors isolated from aerial parts of Wedelia prostrata collected in Manado (Indonesia) and Wedelia chinensis collected on Iriomote Island (Okinawa, Japan). For inhibitory assays, 4-nitrophenyl phosphate is used as enzyme substrate
-
additional information
4-[(5-arylidene-4-oxothiazolidin-3-yl)methyl]benzoic acid derivatives determined as active potent allosteric inhibitors of protein tyrosine phosphatase 1B, in silico studies and in vitro evaluation as insulinomimetic and anti-inflammatory agents, binding modes and inhibitory mechanism, docking studies, detailed overview
-
additional information
phosphorylation of PTPN12 at Ser19 changes its substrate interface, and by doing so, selectively decreases its activity toward the human epidermal growth factor receptor 2 (HER2)-pY1196 site, but not other HER2 phosphorylation sites or other known PTPN12 substrates, such as SRC, paxillin, PAK1,VAV2, p130Cas, FAK, and p190RhoGAP
-
additional information
-
phosphorylation of PTPN12 at Ser19 changes its substrate interface, and by doing so, selectively decreases its activity toward the human epidermal growth factor receptor 2 (HER2)-pY1196 site, but not other HER2 phosphorylation sites or other known PTPN12 substrates, such as SRC, paxillin, PAK1,VAV2, p130Cas, FAK, and p190RhoGAP
-
additional information
inhibition of protein tyrosine phosphatase-1B by vanadyl (VO2+) chelates, competitive and noncompetitive inhibition modes, overview
-
additional information
chemical library screening, kinetic and computational studies of mixed-type inhibitors of protein tyrosine phosphatase 1B, docking and molecular dynamic simulations studies, and enzyme interaction analysis, overview. For the inhibition assays, 4-nitrophenyl phosphate is used as enzyme substrate
-
additional information
-
unaffected by EDTA
-
additional information
-
EDTA, sodium tartrate, sodium fluoride, or okadaic acid have no effect on activity
-
additional information
-
inhibition of PTP-PEST by RNAi reduces formation of podosomal structures at the cell periphery and reduces bone resorption indicating a positive functional role for this PTP in promoting osteoclast activity
-
additional information
-
beta2AR stimulation on a B cell phosphorylates and inactivates HePTP in a Gs/cAMP/PKA-dependent manner
-
additional information
-
interaction between the alpha-cytoplasmic tail of a1beta1 integrin and TCPTP activates TCPTP by disrupting an inhibitory intramolecular bond in TCPTP, screening of screened 64280 small molecules for TCPTP inhibition, overview
-
additional information
-
not inhibitory: okadaic acid
-
additional information
-
synthesis and inhibitory activity of 38 synthetic chalcones towards PtpA, the predominant factor for the activity is the molecule planarity/hydrophobicity and the nature of the substituents, structure-activity analysis, overview. No inhibition by 3a, 3b, 3c, 4h, 5l, 6d, 6g, and 6j
-
additional information
inhibitor synthesis, structure-activity relationships, overview
-
additional information
-
inhibitor synthesis, structure-activity relationships, overview
-
additional information
-
PTP bidentate inhibitor library synthesis and screening, overview. The bidentate inhibitors have three components: 1. the warheads, alkyne-containing N-phenyloxamic acids that are cell-permeable, potent bioisosteric phosphotyrosine mimics, 2. a variety of different types of building blocks that act as the secondary-site binders, and 3. azide-containing linkers of different lengths joining the warhead and the building blocks, overview
-
additional information
-
design of structure based cyclic peptide inhibitors, synthesis involves a crucial intramolecular transamidation via a ring opening reaction. All the compounds show moderate to good inhibitory activities against MPtpA in micromolar concentrations, enzyme docking study, overview
-
additional information
-
unaffected by EDTA
-
additional information
-
in absence of externally added Ca2+, no effect of ethylene glycol bis(2-amino-ethylether) N,N,N,N-tetracetic acid or trifluoperazine. Not inhibitory: okadaic acid
-
additional information
-
inhibitor docking studies with PTP-1B, overview
-
additional information
-
inhibitor design using the crystal structure of PtpA, overview
-
additional information
-
unaffected by okadaic acid
-
additional information
Q6JHV2
not inhibitory: pentamidine, okadaic acid, sodium fluoride up to 5 mM, EDTA up to 10 mM
-
additional information
-
not inhibitory: pentamidine, okadaic acid, sodium fluoride up to 5 mM, EDTA up to 10 mM
-
additional information
-
overview, development of inhibitors
-
additional information
-
the inhibition mechanism of [RuIII(EDTA)(OH2/OH)]1-/2- shows similar interactions, that may be important in the anti-cancer properties of the active forms of many Ru pro-drugs
-
additional information
Yersinia enterolytica
-
inhibitory potency of gold(I) complexes containing N-heterocyclic carbene ligands versus cysteine-dependent protein tyrosine phosphatases, reversible inhibhition, overview
-
additional information
shows no sensitivity to H2O2
-
additional information
-
shows no sensitivity to H2O2
-
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0.0068
(2E)-1-(3-aminophenyl)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0062
(2E)-1-(4-aminophenyl)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0029
(2E)-1-[3-(benzyloxy)phenyl]-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0026
(2E)-3-(5-bromo-2,4-dihydroxyphenyl)-1-[4-methoxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0111
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(3-methoxyphenyl)prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0113
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(3-[[(methoxycarbonyl)sulfanyl]amino]phenyl)prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0042
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(4-butoxyphenyl)prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0137
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(4-hydroxyphenyl)prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0099
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(4-methoxyphenyl)prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0139
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[2-(dimethylamino)phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0068
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[2-(piperidin-1-yl)phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0035
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[2-[di(prop-2-en-1-yl)amino]phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.007
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[3-(3-methylbut-3-en-2-yl)-4-[(3-methylbut-2-en-1-yl)oxy]phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0264
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[3-(dimethylamino)phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0049
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[3-(piperidin-1-yl)phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0045
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[3-[di(prop-2-en-1-yl)amino]phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.006
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(1H-pyrazol-1-yl)phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.03
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(dimethylamino)phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0184
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(methylsulfonyl)phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.008
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(morpholin-4-yl)phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0026
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(piperidin-1-yl)phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0044
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-hydroxy-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0053
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-hydroxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0044
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-hydroxy-3-(prop-2-en-1-yl)phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0029
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-methoxy-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0019
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-methoxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0053
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-methoxy-3-(prop-2-en-1-yl)phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0035
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-[(3-methylbut-2-en-1-yl)oxy]phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0027
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-[(4-methylphenyl)sulfonyl]phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0034
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-[di(prop-2-en-1-yl)amino]phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0063
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[6-(dimethylamino)-1,3-benzodioxol-5-yl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0029
(2E)-3-[5-bromo-2-hydroxy-4-(tetrahydro-2H-pyran-2-yloxy)phenyl]-1-[4-methoxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.0103
(2E)-3-[5-bromo-2-methoxy-4-(tetrahydro-2H-pyran-2-yloxy)phenyl]-1-[4-hydroxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one
-
pH not specified in the publication, temperature not specified in the publication
0.22
(3S,6S,9R)-3,6-dimethyl-9-[(R)-phenyl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione
-
pH 7.5, 25°C
0.199
(3S,6S,9R,12R)-3,6,9-trimethyl-12-[(R)-phenyl(phenylamino)methyl]-1,4,7,10-tetraazacyclotridecane-2,5,8,11-tetrone
-
pH 7.5, 25°C
0.008
(3S,9R)-3-(4-hydroxybenzyl)-9-[(R)-phenyl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione
-
pH 7.5, 25°C
0.023 - 0.1
(5R)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
0.0003 - 0.113
(5S)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
0.14
(6R)-6-[(R)-phenyl(phenylamino)methyl]-1,4-diazepane-2,5-dione
-
pH 7.5, 25°C
0.215
(9R)-9-[(R)-furan-2-yl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione
-
pH 7.5, 25°C
0.0855
(9R)-9-[(R)-phenyl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione
-
pH 7.5, 25°C
0.0497
(difluoro[4-[(2,2,2-trifluoroethyl)carbamoyl]phenyl]methyl)phosphonic acid
pH 6.2, 37°C
0.1
(difluoro[4-[(2-fluorophenyl)carbamoyl]phenyl]methyl)phosphonic acid
above, pH 6.2, 37°C
0.0616
(difluoro[4-[(2-phenylethyl)carbamoyl]phenyl]methyl)phosphonic acid
pH 6.2, 37°C
0.0418
(difluoro[4-[(3-fluorophenyl)carbamoyl]phenyl]methyl)phosphonic acid
pH 6.2, 37°C
0.0227
(difluoro[4-[(4-fluorophenyl)carbamoyl]phenyl]methyl)phosphonic acid
pH 6.2, 37°C
0.1
(difluoro[4-[(phenylamino)methyl]phenyl]methyl)phosphonic acid
above, pH 6.2, 37°C
0.1
(difluoro[4-[2-oxo-2-(phenylamino)ethyl]phenyl]methyl)phosphonic acid
above, pH 6.2, 37°C
0.1
(difluoro[4-[methyl(phenyl)carbamoyl]phenyl]methyl)phosphonic acid
above, pH 6.2, 37°C
0.01
16alphaH,17-isovaleryloxy-ent-kauran-19-oic acid
-
pH 6.0, 30°C
0.019 - 0.109
2-((carboxycarbonyl)amino)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
0.00091 - 0.115
2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
0.00061 - 0.147
2-((carboxycarbonyl)amino)-5-((4-fluoro-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
0.00019 - 0.0038
2-((carboxycarbonyl)amino)-5-((4-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
0.00017 - 0.088
2-((carboxycarbonyl)amino)-5-((5-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
2 - 81
2-(oxalyl-amino)-4,7-dihydro-5H-thieno[2,3-c]thiopyran-3-carboxylic acid
0.0042
2-[6-chloro-5-(1-naphthalyloxy)-1H-benzimidazol-2-yl]thio-N-(thiazol-2-yl)acetamide
pH 7.0, 37°C
2.5
3-(1-carboxy-ethoxy)-6-chloro-benzo(b)-thiophene-2-carboxylic acid
-
pH 7.0, 22°C
0.052
3-(carboxy-fluoro-methoxy)-6-chloro-benzo(b)thiophene-2-carboxylic acid
-
pH 7.0, 22°C
0.86
3-(carboxymethoxy)-2-naphthoic acid
-
pH 7.0, 22°C
0.00092
3-(carboxymethoxy)-5-((cyclohexylmethyl)-amino)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
pH 7.0, 22°C
0.0017
3-(carboxymethoxy)-5-(cyclohexylamino)-thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
pH 7.0, 22°C
0.01
3-(carboxymethoxy)-5-chlorothieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
pH 7.0, 22°C
0.0016
3-(carboxymethoxy)-6-((1-(ethylsulfonyl)-piperidin-4-yl)amino)thieno(3,2-b)(1)benzo-thiophene-2-carboxylic acid
-
pH 7.0, 22°C
0.00068
3-(carboxymethoxy)-6-((cyclohexylmethyl)-amino)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
pH 7.0, 22°C
0.00074
3-(carboxymethoxy)-6-(cyclohexylamino)-thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
pH 7.0, 22°C
0.0024
3-(carboxymethoxy)-6-(tetrahydro-2H-pyran-4-ylamino)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
pH 7.0, 22°C
0.035
3-(carboxymethoxy)-6-chlorothieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
pH 7.0, 22°C
2.5
3-(carboxymethoxy)-6-methylthieno(3,2-c)pyridine-2-carboxylic acid
-
pH 7.0, 22°C
0.16
3-(carboxymethoxy)benzo(b)thiophene-2-carboxylic acid
-
pH 7.0, 22°C
2.5
3-(carboxymethoxy)furo(2,3-b)pyridine-2-carboxylic acid
-
pH 7.0, 22°C
0.2 - 0.23
3-(carboxymethoxy)thieno(2,3-b)pyridine-2-carboxylic acid
0.0092
3-(carboxymethoxy)thieno(3,2-b)(1)benzo-thiophene-2-carboxylic acid
-
pH 7.0, 22°C
0.077
3-(carboxymethoxy)thieno(3,2-b)pyridine-2-carboxylic acid
-
pH 7.0, 22°C
0.28
3-(carboxymethoxy)thieno(3,2-b)thiophene-2-carboxylic acid
-
pH 7.0, 22°C
0.026
3-carboxymethoxy-6-(4-hydroxyphenyl)-benzo(b)-thiophene-2-carboxylic acid
-
pH 7.0, 22°C
0.02
3-carboxymethoxy-6-(5-methyl-1-phenyl-1H-pyrazol-3-ylcarbamoyl)-benzo(b)thiophene-2-carboxylic acid
-
pH 7.0, 22°C
0.061
3-carboxymethoxy-6-chloro-benzo(b)-thiophene-2-carboxylic acid
-
pH 7.0, 22°C
0.128
3-carboxymethoxy-6-phenylbenzo(b)-thiophene-2-carboxylic acid
-
pH 7.0, 22°C
0.03
3-carboxymethoxy-6-thiophen-2-yl-benzo(b)-thiophene-2-carboxylic acid
-
pH 7.0, 22°C
0.119
3-carboxymethoxy-7-chloro-benzo(b)-thiophene-2-carboxylic acid
-
pH 7.0, 22°C
0.037
3-carboxymethoxy-7-methyl-benzo(b)-thiophene-2-carboxylic acid
-
pH 7.0, 22°C
0.011
3-carboxymethoxy-naphtho(1,2-b)thiophene-2-carboxylic acid
-
pH 7.0, 22°C
0.5
3-carboxymethoxy-thieno(3,2-c)quinoline-2-carboxylic acid
-
pH 7.0, 22°C
0.0216
3-[2,5-dimethyl-3-[(3-oxo-2,3-dihydro[1,3]thiazolo[3,2-a]benzimidazol-2-yl)methyl]-1H-pyrrol-1-yl]benzoic acid
pH 7.0, 25°C
0.000026
4-(difluoro(phosphono)methyl)-N-pentadecanoyl-L-phenylalanyl-L-a-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide
-
-
0.0023
4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenyl 4-bromobenzoate
-
pH not specified in the publication, temperature not specified in the publication
0.0024
4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenyl 4-tert-butylbenzoate
-
pH not specified in the publication, temperature not specified in the publication
0.0049
4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenyl benzoate
-
pH not specified in the publication, temperature not specified in the publication
0.03
4-[4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenoxy]butanoic acid
-
pH not specified in the publication, temperature not specified in the publication
0.1
4-[difluoro(phosphono)methyl]benzoic acid
above, pH 6.2, 37°C
0.0052
5-chloro-N-[6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazol-2-yl]-1-methyl-2-(methylthio)-1H-benz-imidazole-6-carboxamide
pH 7.0, 37°C
0.00037
6-((1-(benzylsulfonyl)piperidin-4-yl)amino)-3-(carboxymethoxy)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
pH 7.0, 22°C
0.042
6-bromo-3-carboxymethoxy-benzo(b)-thiophene-2-carboxylic acid
-
pH 7.0, 22°C
0.000044
6-hydroxy-2-phenyl-3-((3-trifluoromethyl)phenyl)benzofuran-5-carboxylic acid
-
at 25°C in 50 mM 3,3-dimethylglutarate buffer, pH 7.0
0.00023
acrolein
-
in sodium acetate (100 mM), bis-Tris (50 mM), Tris (50 mM), diethylenetriaminepentaacetic acid (5 mM), and 2,5-dimethylfuran (5% v/v), at pH 7 and 25°C
0.0363
benzyl (3R,6S)-4,9-dioxo-3-[(R)-phenyl(phenylamino)methyl]-1,5-diazonane-6-carboxylate
-
pH 7.5, 25°C
0.00014 - 0.0148
bis(2-ethyl-maltolato)oxidovanadium(IV)
0.0382
bis(3-hydroxy-2-methyl-4(1H)pyridinonato)oxidovanadium(IV)
pH 5.0, 22°C, recombinant enzyme, versus 4-nitrophenyl phosphate
0.00016 - 0.0065
bis(acetylacetonato)oxidovanadium(IV)
0.0108
ethyl 4-[4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenoxy]butanoate
-
pH not specified in the publication, temperature not specified in the publication
0.0152
ethyl [4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenoxy]acetate
-
pH not specified in the publication, temperature not specified in the publication
0.000017 - 0.00037
fluorescein arsenical hairpin binder
-
0.0118
lupenone
-
pH 6.0, 37°C
0.0034
lupeol
-
pH 6.0, 37°C
0.00134
methyl (6S,10S)-12-[(4-chloro-6-fluoro-2H-chromen-3-yl)methyl]-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
inhibition of MptpB
0.0000024
N-((4-(difluoro(phosphono)methyl)phenyl)acetyl)-L-alpha-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide
-
-
0.0204
N-(6-ethoxy-1,3-benzothiazol-2-yl)-4-nitrobenzene sulfonamide
-
-
0.0071
N-(6-methyl-1,3-benzothiazol-2-yl)-4-nitrobenzenesulfonamide
-
-
0.0034
N-[4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenyl]-4-tert-butylbenzamide
-
pH not specified in the publication, temperature not specified in the publication
0.0413
N-[6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazol-2-yl]-2,2,2-trifluoroacetamide
pH 7.0, 37°C
0.0003 - 0.0007
orthovanadate
0.00073 - 0.0107
phenylhydrazonopyrazolone sulfonate 1
0.017
PO43-
-
active site-directed inhibitor
0.002 - 0.0031
ursolic acid
0.0000056
Zn2+
at pH 7.4 and 25°C
0.1
[(1-benzyl-1H-indazol-5-yl)(difluoro)methyl]phosphonic acid
above, pH 6.2, 37°C
0.0844
[(2-benzyl-2H-indazol-5-yl)(difluoro)methyl]phosphonic acid
pH 6.2, 37°C
0.0923
[(4-bromophenyl)(difluoro)methyl]phosphonic acid
pH 6.2, 37°C
0.0033
[(4-[[3,5-bis(trifluoromethyl)phenyl]carbamoyl]phenyl)(difluoro)methyl]phosphonic acid
pH 6.2, 37°C
0.0014
[(4-[[4-bromo-3,5-bis(trifluoromethyl)phenyl]carbamoyl]phenyl)(difluoro)methyl]phosphonic acid
pH 6.2, 37°C
0.0049
[(4-[[4-bromo-3-(trifluoromethyl)phenyl]carbamoyl]phenyl)(difluoro)methyl]phosphonic acid
pH 6.2, 37°C
0.006
[(4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl]phenyl)(difluoro)methyl]phosphonic acid
pH 6.2, 37°C
0.03
[4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenoxy]acetic acid
-
pH not specified in the publication, temperature not specified in the publication
0.1
[biphenyl-4-yl(difluoro)methyl]phosphonic acid
above, pH 6.2, 37°C
0.0754
[difluoro(4-nitrophenyl)methyl]phosphonic acid
pH 6.2, 37°C
0.0548
[difluoro(4-[[2-(trifluoromethyl)phenyl]carbamoyl]phenyl)methyl]phosphonic acid
pH 6.2, 37°C
0.0107
[difluoro(4-[[3-(trifluoromethyl)phenyl]carbamoyl]phenyl)methyl]phosphonic acid
pH 6.2, 37°C
0.0185
[difluoro(4-[[4-(trifluoromethyl)phenyl]carbamoyl]phenyl)methyl]phosphonic acid
pH 6.2, 37°C
0.0114
[difluoro(4-[[4-fluoro-3-(trifluoromethyl)phenyl]carbamoyl]phenyl)methyl]phosphonic acid
pH 6.2, 37°C
0.1
[difluoro[3-(phenylcarbamoyl)phenyl]methyl]phosphonic acid
above, pH 6.2, 37°C
0.033
[difluoro[4-(1,3-thiazol-2-ylcarbamoyl)phenyl]methyl]phosphonic acid
pH 6.2, 37°C
0.1
[difluoro[4-(1-methyl-1H-pyrazol-4-yl)phenyl]methyl]phosphonic acid
above, pH 6.2, 37°C
0.1
[difluoro[4-(methylcarbamoyl)phenyl]methyl]phosphonic acid
above, pH 6.2, 37°C
0.1
[difluoro[4-(phenoxymethyl)phenyl]methyl]phosphonic acid
above, pH 6.2, 37°C
0.024
[difluoro[4-(phenylcarbamoyl)phenyl]methyl]phosphonic acid
pH 6.2, 37°C
0.1
[difluoro[4-(phenylsulfamoyl)phenyl]methyl]phosphonic acid
above, pH 6.2, 37°C
0.1
[difluoro[4-(propan-2-ylcarbamoyl)phenyl]methyl]phosphonic acid
above, pH 6.2, 37°C
0.0655
[[4-(benzoylamino)phenyl](difluoro)methyl]phosphonic acid
pH 6.2, 37°C
0.0431
[[4-(benzylcarbamoyl)phenyl](difluoro)methyl]phosphonic acid
pH 6.2, 37°C
0.0031
[[4-([[3,5-bis(trifluoromethyl)phenyl]carbamoyl]amino)phenyl](difluoro)methyl]phosphonic acid
pH 6.2, 37°C
0.1
[[4-[(1-ethylpiperidin-4-yl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid
above, pH 6.2, 37°C
0.0446
[[4-[(2-bromophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid
pH 6.2, 37°C
0.068
[[4-[(2-chlorophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid
pH 6.2, 37°C
0.0182
[[4-[(3-bromophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid
pH 6.2, 37°C
0.0349
[[4-[(3-chlorophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid
pH 6.2, 37°C
0.0103
[[4-[(4-bromophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid
pH 6.2, 37°C
0.0168
[[4-[(4-chlorophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid
pH 6.2, 37°C
additional information
additional information
-
0.023
(5R)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTP1B, mutant D48N, pH 7.0, 25°C
0.027
(5R)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTPbeta, pH 7.0, 25°C
0.03
(5R)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTP1B, mutant R47N/D48N, pH 7.0, 25°C
0.1
(5R)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTP1B, pH 7.0, 25°C
0.1
(5R)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTPbeta, mutant N47R/D48N, pH 7.0, 25°C
0.0003
(5S)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTP1B, mutant D48N, pH 7.0, 25°C
0.00033
(5S)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTP1B, mutant R47N/D48N, pH 7.0, 25°C
0.00055
(5S)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTPbeta, pH 7.0, 25°C
0.057
(5S)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTPbeta, mutant N47R/N48D, pH 7.0, 25°C
0.113
(5S)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTP1B, pH 7.0, 25°C
0.019
2-((carboxycarbonyl)amino)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTP1B, mutant R47N/D48N, pH 7.0, 25°C
0.02
2-((carboxycarbonyl)amino)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTP1B, mutant D48N, pH 7.0, 25°C
0.048
2-((carboxycarbonyl)amino)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTPbeta, pH 7.0, 25°C
0.1
2-((carboxycarbonyl)amino)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTP1B, pH 7.0, 25°C
0.109
2-((carboxycarbonyl)amino)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTPbeta, mutant N47R/N48D, pH 7.0, 25°C
0.00091
2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTP1B, mutant D48N, pH 7.0, 25°C
0.00094
2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTP1B, mutant R47N/D48N, pH 7.0, 25°C
0.00128
2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTPbeta, pH 7.0, 25°C
0.08
2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTP1B, pH 7.0, 25°C
0.115
2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTPbeta, mutant N47R/N48D, pH 7.0, 25°C
0.00061
2-((carboxycarbonyl)amino)-5-((4-fluoro-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTP1B, mutant D48N, pH 7.0, 25°C
0.00067
2-((carboxycarbonyl)amino)-5-((4-fluoro-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTP1B, mutant R47N/D48N, pH 7.0, 25°C
0.00073
2-((carboxycarbonyl)amino)-5-((4-fluoro-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTPbeta, pH 7.0, 25°C
0.084
2-((carboxycarbonyl)amino)-5-((4-fluoro-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTPbeta, mutant N47R/N48D, pH 7.0, 25°C
0.147
2-((carboxycarbonyl)amino)-5-((4-fluoro-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTP1B, pH 7.0, 25°C
0.00019
2-((carboxycarbonyl)amino)-5-((4-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTP1B, mutant D48N, pH 7.0, 25°C
0.00031
2-((carboxycarbonyl)amino)-5-((4-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTP1B, mutant R47N/D48N, pH 7.0, 25°C
0.00061
2-((carboxycarbonyl)amino)-5-((4-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTP1B, pH 7.0, 25°C
0.00061
2-((carboxycarbonyl)amino)-5-((4-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTPbeta, pH 7.0, 25°C
0.0038
2-((carboxycarbonyl)amino)-5-((4-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTPbeta, mutant N47R/N48D, pH 7.0, 25°C
0.00017
2-((carboxycarbonyl)amino)-5-((5-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTP1B, mutant D48N, H 7.0, 25°C
0.00019
2-((carboxycarbonyl)amino)-5-((5-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTP1B, mutant R47N/D48N, pH 7.0, 25°C
0.00049
2-((carboxycarbonyl)amino)-5-((5-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTPbeta, pH 7.0, 25°C
0.064
2-((carboxycarbonyl)amino)-5-((5-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTP1B, pH 7.0, 25°C
0.088
2-((carboxycarbonyl)amino)-5-((5-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
isoform PTPbeta, mutant N47R/N48D, pH 7.0, 25°C
2
2-(oxalyl-amino)-4,7-dihydro-5H-thieno[2,3-c]thiopyran-3-carboxylic acid
-
pH 5.5, 25°C, isozyme PTP1B
19
2-(oxalyl-amino)-4,7-dihydro-5H-thieno[2,3-c]thiopyran-3-carboxylic acid
-
pH 5.5, 25°C, isozyme PTPalpha, mutant Q259G
33
2-(oxalyl-amino)-4,7-dihydro-5H-thieno[2,3-c]thiopyran-3-carboxylic acid
-
pH 5.5, 25°C, isozyme PTP1B, mutant G259Q
81
2-(oxalyl-amino)-4,7-dihydro-5H-thieno[2,3-c]thiopyran-3-carboxylic acid
-
pH 5.5, 25°C, isozyme PTPalpha
0.2
3-(carboxymethoxy)thieno(2,3-b)pyridine-2-carboxylic acid
-
pH 5.5, 22°C
0.23
3-(carboxymethoxy)thieno(2,3-b)pyridine-2-carboxylic acid
-
pH 7.4, 22°C
0.00014
bis(2-ethyl-maltolato)oxidovanadium(IV)
pH 5.0, 22°C, recombinant enzyme, versus DADE(pY)LIPQQG
0.0148
bis(2-ethyl-maltolato)oxidovanadium(IV)
pH 5.0, 22°C, recombinant enzyme, versus 4-nitrophenyl phosphate
0.00016
bis(acetylacetonato)oxidovanadium(IV)
pH 5.0, 22°C, recombinant enzyme, versus DADE(pY)LIPQQG
0.0065
bis(acetylacetonato)oxidovanadium(IV)
pH 5.0, 22°C, recombinant enzyme, versus 4-nitrophenyl phosphate
0.000017
fluorescein arsenical hairpin binder
CCPGCC-insertion mutant TCPTP-187
-
0.000038
fluorescein arsenical hairpin binder
CCPGCC-insertion mutant PTPH1-816
-
0.000039
fluorescein arsenical hairpin binder
CCPGCC-insertion mutant PTPHalpha-406
-
0.000046
fluorescein arsenical hairpin binder
CCPGCC-insertion mutant PTP1B-186
-
0.000053
fluorescein arsenical hairpin binder
CCPGCC-insertion mutant PTP-PEST-204
-
0.000089
fluorescein arsenical hairpin binder
CCPGCC-insertion mutant HePTPH-211
-
0.00037
fluorescein arsenical hairpin binder
CCPGCC-insertion mutant FAP-1-2364
-
0.006
H2O2
-
PTP1B, in 50 mM 3,3-dimethylglutarate (pH 6.0), at 25°C
0.0074
H2O2
-
CD45, in 50 mM 3,3-dimethylglutarate (pH 6.0), at 25°C
0.0075
H2O2
-
HePTP, in 50 mM 3,3-dimethylglutarate (pH 6.0), at 25°C
0.0294
H2O2
-
VHR, in 50 mM 3,3-dimethylglutarate (pH 6.0), at 25°C
0.196
H2O2
-
PTPalpha, in 50 mM 3,3-dimethylglutarate (pH 6.0), at 25°C
0.00022
JTT-551
-
pH 7.5, 22°C, PTPB1
0.0093
JTT-551
-
pH 7.5, 22°C, TCPTP
0.03
JTT-551
-
above, pH 7.5, 22°C, CD45 and LAR
0.0003
orthovanadate
pH 5.0, 22°C, recombinant enzyme
0.0007
orthovanadate
-
Ki value for inhibition of wild type Shp2
0.00073
phenylhydrazonopyrazolone sulfonate 1
-
Ki value for inhibition of wild type Shp2
0.0058
phenylhydrazonopyrazolone sulfonate 1
-
Ki value for inhibition of mutant Shp2 R362K
0.0058
phenylhydrazonopyrazolone sulfonate 1
-
Ki value for inhibition of wild type PTP1B
0.0107
phenylhydrazonopyrazolone sulfonate 1
-
Ki value for inhibition of wild type Shp1
0.0053
suramin
-
Ki value for inhibition of wild type PTP1B
0.0057
suramin
-
Ki value for inhibition of wild type Shp2
0.002
ursolic acid
-
pH 6.0, 37°C
0.0031
ursolic acid
-
pH not specified in the publication, temperature not specified in the publication
additional information
additional information
-
inhibition kinetics
-
additional information
additional information
inhibition kinetics of WPD loop insertion cysteine mutants with FlAsH, overview
-
additional information
additional information
-
PTPB1 inhibition kinetics, overview
-
additional information
additional information
-
Ru(III) complexes with thiolato groups, stopped-flow kinetic studies with both RuIII-EDTA and RuIII-hEDTRA with the thiol-containing biomolecules, GSH or Cys, in the buffer
-
additional information
additional information
inhibition kinetic analysis of (VO2+) chelates with PTP1B, Lineweaver-Burk plots, overview
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
0.00927
(1R,3aS,3bS,10aR,10bS,12aR)-1-[(2R)-4-carboxybutan-2-yl]-6,6,10a,12a-tetramethyl-1,2,3,3a,3b,4,6,7,10,10a,10b,11,12,12a-tetradecahydrocyclopenta[5,6]naphtho[1,2-f]indazole-9-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.01433
(2alpha,3alpha)-2,3-dihydroxyolean-12-en-28-oic acid
Homo sapiens
-
PTPB1
0.00493
(2beta,3beta)-2,3-dihydroxyolean-12-en-28-oic acid
Homo sapiens
-
PTPB1
0.0502
(2E)-1-(2'-hydroxyphenyl)-3-(1-naphthyl)-2-propen-1-one
Mycobacterium tuberculosis
-
pH 8.0, 37°C
0.05
(2E)-1-(2,4-dihydroxyphenyl)-3-(4-hydroxyphenyl)prop-2-en-1-one
Homo sapiens
-
above, pH 6.0, 37°C
0.0084
(2E)-1-(2,5-dimethoxyphenyl)-3-(2-naphthyl)-2-propen-1-one
Mycobacterium tuberculosis
-
pH 8.0, 37°C
0.0395
(2E)-1-(2,5-dimethoxyphenyl)-3-(naphth-1-yl)-2-propen-1-one
Mycobacterium tuberculosis
-
pH 8.0, 37°C
0.0231
(2E)-1-(3,4-dimethoxyphenyl)-3-(2-naphthyl)-2-propen-1-one
Mycobacterium tuberculosis
-
pH 8.0, 37°C
0.0537
(2E)-1-(3-methoxy-4-hydroxyphenyl)-3-(2-naphthyl)-2-propen-1-one
Mycobacterium tuberculosis
-
pH 8.0, 37°C
0.00461
(2E)-2-[1-carbamothioyl-3-(4-nitrophenyl)-5-oxo-1,5-dihydro-4H-pyrazol-4-ylidene]-1-(4-sulfophenyl)diazanide
Yersinia pestis
-
pH and temperature not specified in the publication
0.00038
(2E)-2-[[5-(3-carboxy-4-hydroxycyclohexa-1,5-dien-1-yl)furan-2-yl]methylidene]-1-[6-[(4-fluorophenyl)amino][1,2,5]oxadiazolo[3,4-b]pyrazin-5-yl]diazanide
Yersinia pestis
-
pH and temperature not specified in the publication
0.05
(2E)-3-(4-hydroxy-2-methoxyphenyl)-1-(4-hydroxyphenyl)prop-2-en-1-one
Homo sapiens
-
above, pH 6.0, 37°C
0.0183
(2E)-3-[2,4-dimethoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
Homo sapiens
-
pH 6.0, 37°C
0.0198
(2E)-3-[2,4-dimethoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-methoxyphenyl)prop-2-en-1-one
Homo sapiens
-
pH 6.0, 37°C
0.0309
(2E)-3-[4-hydroxy-2-methoxy-3-(3-methylbut-2-en-1-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
Homo sapiens
-
pH 6.0, 37°C
0.0191
(2E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
Homo sapiens
-
pH 6.0, 37°C
0.0117
(2E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-methoxyphenyl)prop-2-en-1-one
Homo sapiens
-
pH 6.0, 37°C
0.0207
(2E)-3-[4-hydroxy-2-methoxy-5-(3-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
Homo sapiens
-
pH 6.0, 37°C
0.00017
(2R)-2-benzyl-3-[2,6-dibromo-4-(6-bromo-5a,11a-dihydrobenzo[b]naphtho[2,3-d]furan-11-yl)phenyl]propanoic acid
Homo sapiens
-
0.0632
(2Z)-2-([5-[4-(1H-tetrazol-1-yl)phenyl]furan-2-yl]methylidene)[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
Homo sapiens
pH 7.0, 25°C
0.3
(2Z)-2-[[5-(2-methyl-5-nitrophenyl)furan-2-yl]methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
Homo sapiens
above, pH 7.0, 25°C
0.0083
(3alpha,5beta,8alpha,9beta,10alpha,13alpha)-3-[[(2E)-4-phenylbut-2-enoyl]oxy]kaur-16-en-18-oic acid
Homo sapiens
pH 6.0, 37°C
0.00479
(3beta)-3-(acetyloxy)olean-12-en-28-oic acid
Homo sapiens
-
in 50 mM citrate (pH 6.0), 1 mM dithiothreitol, 1 mM EDTA, and 0.1 M NaCl, at 37°C
0.00534
(3beta)-3-hydroxyolean-12-en-28-oic acid
Homo sapiens
-
in 50 mM citrate (pH 6.0), 1 mM dithiothreitol, 1 mM EDTA, and 0.1 M NaCl, at 37°C
0.0064
(3beta)-3-hydroxyoleana-11,13(18)-dien-28-oic acid
Homo sapiens
-
in 50 mM citrate (pH 6.0), 1 mM dithiothreitol, 1 mM EDTA, and 0.1 M NaCl, at 37°C
0.00122
(3Z)-5-bromo-3-[4-oxo-2-thioxo-3-[3-(trifluoromethyl)phenyl]-1,3-thiazolidin-5-ylidene]-1,3-dihydro-2H-indol-2-one
Yersinia pestis
-
pH and temperature not specified in the publication
0.00235
(4-fluorophenyl)[[(Z)-(2,2,2-trifluoro-1-[1-(4-fluorophenyl)-2-methyl-5-[4-(methylsulfonyl)phenyl]-1H-pyrrol-3-yl]ethylidene)amino]oxy]methanone
Yersinia pestis
-
pH and temperature not specified in the publication
0.03
(4aR,6aR,6bS,8aR,12aS,14aR,14bR)-8a-hydroxy-4,4,6a,6b,11,11,14b-heptamethyl-1,4a,5,6,6a,6b,7,8a,9,10,11,12,12a,14,14a,14b-hexadecahydropicene-3,8(2H,4H)-dione
Homo sapiens
-
in 50 mM citrate (pH 6.0), 1 mM dithiothreitol, 1 mM EDTA, and 0.1 M NaCl, at 37°C
0.00377
(4aR,6aS,6bR,8aR,10S,12aR,12bR,14bS)-4a,10-dihydroxy-2,2,6a,6b,9,9,12a-heptamethyl-2,3,4,4a,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,13,14b-octadecahydropicen-5(1H)-one
Homo sapiens
-
in 50 mM citrate (pH 6.0), 1 mM dithiothreitol, 1 mM EDTA, and 0.1 M NaCl, at 37°C
0.00148 - 0.00493
(4aS,6aS,6bR,13aR)-10-acetyl-2,2,6a,6b,9,9,13a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
0.00175 - 0.00566
(4aS,6aS,6bR,13aR)-10-hexanoyl-2,2,6a,6b,9,9,13a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
0.00192 - 0.00644
(4aS,6aS,6bR,13aR)-11-amino-2,2,6a,6b,9,9,13a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,13,13a,13b,14,15b-hexadecahydropiceno[3,2-d][1,3]thiazole-4a(2H)-carboxylic acid
0.00165 - 0.00599
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
0.0026 - 0.00844
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,13,13a,13b,14,15b-hexadecahydropiceno[2,3-d][1,2]oxazole-4a(2H)-carboxylic acid
0.00064 - 0.00439
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-10-(pyridin-3-ylcarbonyl)-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
0.00081 - 0.00362
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-10-(pyridin-4-ylcarbonyl)-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
0.00139 - 0.0038
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-10-phenyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
0.00178 - 0.00551
(4aS,6aS,6bR,14aR)-11-amino-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
0.00261 - 0.0065
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,11,14a-octamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
0.00273 - 0.00819
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
0.00179 - 0.00831
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinoxaline-4a(2H)-carboxylic acid
0.00544
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-11-(methylamino)-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
Homo sapiens
-
PTPB1
0.00061 - 0.0016
(4aS,6aS,6bR,15aR)-2,2,6a,6b,9,9,15a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,15,15a,15b,16,17b-octadecahydro-4aH-chryseno[2,1-b]carbazole-4a-carboxylic acid
0.00143 - 0.00588
(4aS,6aS,6bR,16aR)-2,2,6a,6b,9,9,16a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,16,16a,16b,17,18b-hexadecahydrochryseno[1,2-b]phenazine-4a(2H)-carboxylic acid
0.00448
(4E)-2-(3,4-dichlorophenyl)-4-(3,4,5-trimethoxybenzylidene)-1,3-oxazol-5(4H)-one
Yersinia pestis
-
pH and temperature not specified in the publication
0.00411
(4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-1,2,3,3a,3b,4,6,6a,7,9a,10,10a,10b,11,12,12a-hexadecahydrocyclopenta[5,6]naphtho[1,2-f]indazol-1-yl]pentanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.03944
(4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-2,3,3a,3b,4,6,10,10a,10b,11,12,12a-dodecahydro-1H-cyclopenta[7,8]phenanthro[2,3-d][1,2,3]thiadiazol-1-yl]pentanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00913
(4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-2,3,3a,3b,4,6,6a,9a,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2-d][1,2]oxazol-1-yl]pentanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00162
(4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-7-phenyl-1,2,3,3a,3b,4,6,6a,7,9a,10,10a,10b,11,12,12a-hexadecahydrocyclopenta[5,6]naphtho[1,2-f]indazol-1-yl]pentanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00557
(4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-8-amino-6,6,10a,12a-tetramethyl-2,3,3a,3b,4,6,10,10a,10b,11,12,12a-dodecahydro-1H-cyclopenta[7,8]phenanthro[2,3-d][1,3]thiazol-1-yl]pentanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.01165
(4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinazolin-1-yl]pentanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00862
(4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinoxalin-1-yl]pentanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00911
(4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-6,6,8,11a,13a-pentamethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinazolin-1-yl]pentanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00361
(4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-8-amino-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinazolin-1-yl]pentanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.028
(5beta,8alpha,9beta,10alpha,13alpha)-kaur-16-en-18-oic acid
Homo sapiens
pH 6.0, 37°C
0.0066
(5Z)-3-benzyl-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.03
(5Z)-3-benzyl-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
Homo sapiens
IC50 above 0.03 mM, in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0072
(5Z)-3-benzyl-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0206
(5Z)-3-butyl-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0096
(5Z)-3-butyl-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0298
(5Z)-5-(4-hydroxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0142
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0082
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0121
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-3-butyl-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0223
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-3-methyl-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0049
(5Z)-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0123
(5Z)-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.03
(5Z)-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-3-butyl-1,3-thiazolidine-2,4-dione
Homo sapiens
IC50 above 0.03 mM, in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0113
(5Z)-5-(5-bromo-4-hydroxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0122
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0227
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-(3-methylbut-2-en-1-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.03
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-(prop-2-en-1-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
IC50 above 0.03 mM, in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.03
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-(propan-2-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
IC50 above 0.03 mM, in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.03
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-methyl-1,3-thiazolidine-2,4-dione
Homo sapiens
IC50 above 0.03 mM, in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0076
(5Z)-5-[4-(benzyloxy)-5-bromo-2-methoxybenzylidene]-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0103
(5Z)-5-[4-(benzyloxy)-5-bromo-2-methoxybenzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0081
(5Z)-5-[4-(benzyloxy)-5-bromo-2-methoxybenzylidene]-3-methyl-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0293
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.012
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-(3-methylbut-2-en-1-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.03
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-(prop-2-en-1-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
IC50 above 0.03 mM, in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0064
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-(propan-2-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.03
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-methyl-1,3-thiazolidine-2,4-dione
Homo sapiens
IC50 above 0.03 mM, in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0081
(5Z)-5-[5-bromo-2-methoxy-4-(prop-2-en-1-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.017
(5Z)-5-[5-bromo-2-methoxy-4-(prop-2-en-1-yloxy)benzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0079
(5Z)-5-[5-bromo-2-methoxy-4-(prop-2-en-1-yloxy)benzylidene]-3-butyl-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0046
(5Z)-5-[5-bromo-2-methoxy-4-(propan-2-yloxy)benzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0097
(5Z)-5-[5-bromo-2-methoxy-4-(propan-2-yloxy)benzylidene]-3-butyl-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.0053
(5Z)-5-[5-bromo-2-methoxy-4-[(3-methylbut-2-en-1-yl)oxy]benzylidene]-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.01
(5Z)-5-[5-bromo-2-methoxy-4-[(4-methylpent-3-en-1-yl)oxy]benzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
0.00466
(6aS,6bR,8aR,10S,12aS,12bR)-10-hydroxy-2,2,6a,6b,9,9,12a-heptamethyl-2,3,4,4a,6,6a,6b,7,8,8a,9,10,11,12,12a,12b-hexadecahydropicen-5(1H)-one
Homo sapiens
-
in 50 mM citrate (pH 6.0), 1 mM dithiothreitol, 1 mM EDTA, and 0.1 M NaCl, at 37°C
0.022
(E)-N-(4,5-diphenyl-1,3-thiazol-2-yl)-2-naphthalen-2-ylethenesulfonamide
Homo sapiens
-
0.021
(E)-N-[4-(4-chlorophenyl)-5-propyl-1,3-thiazol-2-yl]-2-(3,4-dichlorophenyl)ethenesulfonamide
Homo sapiens
-
0.0229 - 0.0324
(Z)-2-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
0.0008 - 0.0154
(Z)-3-(2-(2-carboxyphenyl)hydrazono)-2-oxoindoline-5-carboxylic acid
0.0468 - 0.0967
(Z)-3-(2-(2-nitrophenyl)hydrazono)-2-oxoindoline-5-sulfonic acid
0.0158 - 0.0724
(Z)-3-(2-(3-carboxyphenyl)hydrazono)-2-oxoindoline-5-carboxylic acid
0.0194 - 0.3
(Z)-3-(2-(5-(4-chlorobenzylcarbamoyl)-2-oxoindolin-3-ylidene)-hydrazinyl)benzoic acid
0.0052 - 0.0734
(Z)-3-(2-(5-(N-(2,4-dichlorophenethyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
0.0055 - 0.0194
(Z)-3-(2-(5-(N-(2-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
0.0048 - 0.1228
(Z)-3-(2-(5-(N-(3-chloro-4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
0.0038 - 0.0425
(Z)-3-(2-(5-(N-(3-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
0.0106 - 0.0742
(Z)-3-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
0.0014 - 0.0188
(Z)-3-(2-(5-(N-(4-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
0.001 - 0.0183
(Z)-3-(2-(5-(N-(4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
0.005 - 0.0326
(Z)-3-(2-(5-(N-(4-methylbenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
0.0074 - 0.0608
(Z)-4-(2-(5-(N-(2-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
0.0083 - 0.0431
(Z)-4-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
0.0059 - 0.0181
(Z)-4-(2-(5-(N-(4-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
0.0063 - 0.0114
(Z)-4-(2-(5-(N-(4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
0.0013 - 0.0071
(Z)-4-(2-(5-(N-benzylsulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl) benzoic acid
0.0028
1,1'-(piperazine-1,4-diyl)bis(4-(3-(dibenzylamino)phenyl)butane-1,2,4-trione)
Homo sapiens
-
in 50 mM MOPS, pH 6.5, at 30°C
0.00088
1,6-dimethyl-3-(thiophen-2-yl)pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
Yersinia pestis
-
pH and temperature not specified in the publication
0.2
1-(2,6-dihydroxy-4-methoxy-3-methylphenyl)ethanone
Homo sapiens
-
above
0.00168
1-[(5Z)-5-(1-butyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperidine-4-carboxamide
Yersinia pestis
-
pH and temperature not specified in the publication
0.00098
1-[4-[(2-nitrophenyl)sulfonyl]piperazin-1-yl]-2-phenoxyethanone
Yersinia pestis
-
pH and temperature not specified in the publication
0.013
15-hydroxykaur-9(11),16-dien-19-oic acid
Homo sapiens
pH 6.0, 37°C
0.0081
19alpha,24-dihydroxyurs-12-en-3-on-28-oic acid
Homo sapiens
-
-
0.00074
2',4'-dihydroxy-1,1'-biphenyl
Homo sapiens
pH 7.0, 37°C, PTP-B1
0.00389
2,2'-[benzene-1,4-diylbis(methanediyloxybenzene-4,1-diyl)]bis(oxoacetic acid)
Homo sapiens
-
pH and temperature not specified in the publication
0.001
2,5-dihydroxy-3-[7-(2-methylbenzyl)-1H-indol-3-yl]cyclohexa-2,5-diene-1,4-dione
Homo sapiens
-
0.0056
2,5-dihydroxy-3-[7-(3-methylbut-2-en-1-yl)-1H-indol-3-yl]cyclohexa-2,5-diene-1,4-dione
Homo sapiens
-
0.005 - 0.0143
2-(4-hydroxyphenyl)-3-[(3,4-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0007 - 0.0057
2-(4-hydroxyphenyl)-3-[(4-carboxy-3-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.00401
2-[(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)imino]-1H-indene-1,3(2H)-dione
Yersinia pestis
-
pH and temperature not specified in the publication
0.0084
2-[6-chloro-5-(1-naphthalyloxy)-1H-benzimidazol-2-yl]thio-N-(thiazol-2-yl)acetamide
Homo sapiens
pH 7.0, 37°C
0.0128
24-hydroxyursolic acid
Homo sapiens
-
-
0.00072
28-(10-decanoic)-oleanolic acid
Homo sapiens
-
0.00059
28-(12-dodecanoic)-oleanolic acid
Homo sapiens
-
0.0021
28-(2-acetic)-oleanolic acid
Homo sapiens
-
0.00133
28-(4-butyric)-oleanolic acid
Homo sapiens
-
0.00088
28-(6-hexanoic)-oleanolic acid
Homo sapiens
-
0.00078
28-(8-octanoic)-oleanolic acid
Homo sapiens
-
0.01544
28-(glycine)-oleanolic acid amide
Homo sapiens
-
0.01635
28-(L-glutamic acid)-oleanolic acid amide
Homo sapiens
-
0.00331
28-(L-phenylalanine)-oleanolic acid amide
Homo sapiens
-
0.00319
28-(p-carboxyphenyl)-oleanolic acid amide
Homo sapiens
-
0.00074
28-[4-butyric((R)-1-carboxy-phenylethyl)-amide]-DELTA12-oleanene
Homo sapiens
-
0.00059
28-[4-butyric((S)-1-carboxy-3-indole-ethyl)-amide]-DELTA12-oleanene
Homo sapiens
-
0.00462
28-[4-butyric((S)-1-carboxy-5-imidazole-ethyl)-amide]-DELTA12-oleanene
Homo sapiens
-
0.00055
28-[4-butyric((S)-1-carboxy-methylthioethyl)-amide]-DELTA12-oleanene
Homo sapiens
-
0.00057
28-[4-butyric((S)-1-carboxy-phenylethyl)-amide]-DELTA12-oleanene
Homo sapiens
-
0.00066
28-[4-butyric(1-carboxy-2,3-dimethoxyphenylethyl)-amide]-DELTA12-oleanene
Homo sapiens
-
0.00082
28-[4-butyric(1-carboxy-3,4-dimethoxyphenylethyl)-amide]-DELTA12-oleanene
Homo sapiens
-
0.00044
28-[4-butyric(1-carboxy-3,4-oxymethyleneoxyphenylethyl)-amide]-DELTA12-oleanene
Homo sapiens
-
0.00063
28-[4-butyric(1-carboxy-3,5-dimethoxyphenylethyl)-amide]-DELTA12-oleanene
Homo sapiens
-
0.00051
28-[4-butyric(1-carboxy-m-chlorophenylethyl)-amide]-DELTA12-oleanene
Homo sapiens
-
0.00052
28-[4-butyric(1-carboxy-m-methoxyphenylethyl)-amide]-DELTA12-oleanene
Homo sapiens
-
0.00056
28-[4-butyric(1-carboxy-o-chlorophenylethyl)-amide]-DELTA12-oleanene
Homo sapiens
-
0.00053
28-[4-butyric(1-carboxy-o-methoxyphenylethyl)-amide]-DELTA12-oleanene
Homo sapiens
-
0.00055
28-[4-butyric(1-carboxy-o-methylphenylethyl)-amide]-DELTA12-oleanene
Homo sapiens
-
0.00061
28-[4-butyric(1-carboxy-p-chlorophenylethyl)-amide]-DELTA12-oleanene
Homo sapiens
-
0.00057
28-[4-butyric(1-carboxy-p-fluorophenylethyl)-amide]-DELTA12-oleanene
Homo sapiens
-
0.0006
28-[4-butyric(1-carboxy-p-methoxyphenylethyl)-amide]-DELTA12-oleanene
Homo sapiens
-
0.00065
28-[4-butyric(1-carboxy-p-methylphenylethyl)-amide]-DELTA12-oleanene
Homo sapiens
-
0.00045
28-[4-butyric(1-carboxy-p-nitrophenylethyl)-amide]-DELTA12-oleanene
Homo sapiens
-
0.00593
2beta,3beta-2,3-dihydroxyolean-12-en-28-oic acid
Homo sapiens
-
PTPB1
0.01623
3,16-dioxo-olean-12(13),17(18)-diene
Homo sapiens
-
in 50 mM citrate (pH 6.0), 1 mM dithiothreitol, 1 mM EDTA, and 0.1 M NaCl, at 37°C
0.00233
3-(2,2'-dimethyl-carboxypropanoyloxy)-oleanolic acid
Homo sapiens
-
0.00272
3-(2-carboxy-benzyloxy)-oleanolic acid
Homo sapiens
-
0.00458
3-(2-carboxybenzoyloxy)-oleanolic acid
Homo sapiens
-
0.008
3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethyl-N-[4-(1,3-thiazol-2-ylsulfamoyl)phenyl]-1-benzofuran-6-sulfonamide
Homo sapiens
pH and temperature not specified in the publication
0.00062
3-(3-carboxy-benzyloxy)-oleanolic acid
Homo sapiens
-
0.00015
3-(4-carboxy-benzyloxy)-28-[4-butyric((s)-1-carboxyphenylethyl)-amide]-DELTA12-oleanene
Homo sapiens
-
0.00054
3-(4-carboxy-benzyloxy)-oleanolic acid
Homo sapiens
-
0.00128
3-(4-chlorophenyl)-1,6-dimethylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
Yersinia pestis
-
pH and temperature not specified in the publication
0.3
3-([2-chloro-6-methoxy-4-[(E)-(3-oxo[1,3]thiazolo[3,2-a]benzimidazol-2(3H)-ylidene)methyl]phenoxy]methyl)benzoic acid
Homo sapiens
above, pH 7.0, 25°C
0.00267
3-benzyloxy-oleanolic acid
Homo sapiens
-
0.00686
3-butyl-7-(2,4-dihydroxy-6-pentylphenoxy)-3,5-dimethoxy-2-benzofuran-1(3H)-one
Homo sapiens
-
-
0.00597
3-carboxypropanoyloxy-oleanolic acid
Homo sapiens
-
0.00261
3-dehydroxy-oleanolic acid
Homo sapiens
-
0.00289
3-ethyl oxalyl-oleanolic acid
Homo sapiens
-
0.0635
3-hydroxy-4-(methoxycarbonyl)-2,5-dimethylphenyl 3-acetyl-2,4-dihydroxy-6-methylbenzoate
Homo sapiens
-
-
0.017
3-hydroxy-4-(methoxycarbonyl)-5-methylphenyl 4-(beta-D-galactopyranosyloxy)-2-hydroxy-6-pentadecylbenzoate
Homo sapiens
-
-
0.00285
3-methylene-oleanolic acid
Homo sapiens
-
0.00286
3-oxalyl-oleanolic acid
Homo sapiens
-
0.00532
3-oxo-oleanolic acid
Homo sapiens
-
0.00248
3-[(1-butyl-1,6-dimethoxy-3-oxo-1,3-dihydro-2-benzofuran-4-yl)oxy]-4,6-dihydroxy-2-pentylbenzoic acid
Homo sapiens
-
-
0.0119 - 0.1566
3-[(2-nitrophenyl)hydrazono]-2-oxo-2,3-dihydro-1H-indole-5-sulfonamide
0.0044 - 0.0409
3-[(2-nitrophenyl)hydrazono]-2-oxo-2,3-dihydro-1H-indole-5-sulfonic acid 4-chlorobenzylamide
0.3
3-[(E)-(3-oxo[1,3]thiazolo[3,2-a]benzimidazol-2(3H)-ylidene)methyl]benzoic acid
Homo sapiens
above, pH 7.0, 25°C
0.0083
3-[2,5-dimethyl-3-[(3-oxo-2,3-dihydro[1,3]thiazolo[3,2-a]benzimidazol-2-yl)methyl]-1H-pyrrol-1-yl]benzoic acid
Homo sapiens
pH 7.0, 25°C
0.0329
3-[3-(2,4-dichlorophenyl)propanoyl]-2-hydroxycyclohepta-2,4,6-trien-1-one
Homo sapiens
pH 7.0, 25°C
0.0045 - 0.0371
3-[N'-(5-isopropylsulfamoyl-2-oxo-1,2-dihydroindol-3-ylidene)-hydrazino]benzoic acid
0.0077
3alpha-cinnamoyloxypterokaurene L3
Homo sapiens
pH 6.0, 37°C
0.00505
3alpha-oleanolic acid
Homo sapiens
-
0.00394
3beta,16a,17-trihydroxy-olean-12-ene
Homo sapiens
-
in 50 mM citrate (pH 6.0), 1 mM dithiothreitol, 1 mM EDTA, and 0.1 M NaCl, at 37°C
0.05
3beta-acetoxy-17beta-hydroxy-28-norolean-12-ene
Homo sapiens
-
IC50 above 0.05 mM, in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA, and 1 mM dithiothreitol, at 37°C
0.044
3beta-acetoxy-28-hydroxyolean-12-ene
Homo sapiens
-
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA, and 1 mM dithiothreitol, at 37°C
0.0078
3beta-acetoxyolean-12-en-28-acid
Homo sapiens
-
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA, and 1 mM dithiothreitol, at 37°C
0.0093
3beta-acetoxyolean-12-en-28-aldehyde
Homo sapiens
-
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA, and 1 mM dithiothreitol, at 37°C
0.0052
3beta-hydroxyolean-12-en-28-oic acid
Homo sapiens
-
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA, and 1 mM dithiothreitol, at 37°C
0.00119
4'-[(2-butyl-1-benzofuran-3-yl)methyl]biphenyl-4-ol
Homo sapiens
pH 7.0, 37°C, PTP-B3
0.00108
4'-[2-(4-hydroxybutyl)-1-benzofuran-3-yl]biphenyl-4-ol
Homo sapiens
pH 7.0, 37°C, PTP-B2
0.00573
4,4'-[benzene-1,4-diylbis(methanediyloxy)]dibenzoic acid
Homo sapiens
-
0.01
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(3-phenoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0042
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(3-phenylmethoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0051
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(4-phenoxyphenyl)methylidene]thiazolidin-3-yl) methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0019
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(4-phenylmethoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0071
4-(((5Z)-4-oxo-5-[(3-phenoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0057
4-(((5Z)-4-oxo-5-[(3-phenylmethoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0106
4-(((5Z)-4-oxo-5-[(4-phenoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.005
4-(((5Z)-4-oxo-5-[(4-phenylmethoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.02
4-(3-(dibenzylamino)phenyl)-2,4-dioxobutanoic acid
Homo sapiens
-
in 50 mM MOPS, pH 6.5, at 30°C
0.2732
4-(5-bromo-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-2-hydroxybenzoic acid
Homo sapiens
pH 7.0, 25°C
0.00059
4-(beta-D-galactopyranosyloxy)-2-hydroxy-6-pentadecylbenzoic acid
Homo sapiens
-
-
0.0109
4-([(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0025
4-([(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0104
4-([(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0022
4-([(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0051
4-([(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2-[(4-methoxyphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0056
4-([(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2-[(4-tert-butylphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.003
4-([(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2-[(4-methoxyphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0014
4-([(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2-[(4-tert-butylphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.018
4-([(5Z)-2,4-dioxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0028
4-([(5Z)-2,4-dioxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0145
4-([(5Z)-2-(4-fluorophenylimino)-4-oxo-5-([3-(2-phenylethoxy)phenyl]methylidene)thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0015
4-([(5Z)-2-(4-fluorophenylimino)-4-oxo-5-([4-(2-phenylethoxy)phenyl]methylidene)thiazolidin-3-yl]methyl)benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0019
4-([(5Z)-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene)-2-thioxothiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0035
4-([(5Z)-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene)-2-thioxothiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0796
4-methoxy-3-(5-methoxy-1-benzofuran-6-yl)-5-(4-methoxyphenyl)isoxazole
Homo sapiens
-
0.0804
4-methoxy-3-(5-methoxy-1-benzofuran-6-yl)-5-phenylisoxazole
Homo sapiens
-
0.005
4-oxo-8-(phenylsulfanyl)-1,4-dihydro-1,7-naphthyridine-3-carboxylic acid
Homo sapiens
-
0.0173
4-[(1E)-3-(4-hydroxyphenyl)-3-oxoprop-1-en-1-yl]-5-methoxy-2-(2-methylbut-3-en-2-yl)phenyl acetate
Homo sapiens
-
pH 6.0, 37°C
0.00022
4-[(2,4-dihydroxy-6-pentadecylbenzoyl)oxy]-2-hydroxy-6-methylbenzoic acid
Homo sapiens
-
-
0.0292
4-[(2E)-3-[2,4-dimethoxy-5-(2-methylbut-3-en-2-yl)phenyl]prop-2-enoyl]phenyl acetate
Homo sapiens
-
pH 6.0, 37°C
0.05
4-[(2E)-3-[4-(acetyloxy)-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]prop-2-enoyl]phenyl acetate
Homo sapiens
-
above, pH 6.0, 37°C
0.0192
4-[(2E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]prop-2-enoyl]phenyl acetate
Homo sapiens
-
pH 6.0, 37°C
0.00192
4-[1,3-dioxo-5-(4-oxo-4H-3,1-benzoxazin-2-yl)-1,3-dihydro-2H-isoindol-2-yl]benzoate
Yersinia pestis
-
pH and temperature not specified in the publication
0.3
4-[2-[(5-chloro-1,3-benzoxazol-2-yl)sulfanyl]acetamido]benzoic acid
Homo sapiens
above, pH 7.0, 25°C
0.00215
4-[4,5-di(biphenyl-4-yl)-1H-imidazol-2-yl]benzoic acid
Yersinia pestis
-
pH and temperature not specified in the publication
0.0045 - 0.0277
4-[N'-(5-isopropylsulfamoyl-2-oxo-1,2-dihydroindol-3-ylidene)-hydrazino]benzoic acid
0.0019
4-[[(2E,5Z)-4-oxo-5-[(3-phenoxyphenyl)methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0011
4-[[(2E,5Z)-4-oxo-5-[(4-phenoxyphenyl)methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0046
4-[[(2E,5Z)-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0015
4-[[(2E,5Z)-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0038
4-[[(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0011
4-[[(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0095
4-[[(5Z)-2,4-dioxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0026
4-[[(5Z)-2,4-dioxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0011
4-[[(5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.0016
4-[[(5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid
Homo sapiens
pH 7.0, 37°C
0.00444
5,7-bis[(E)-2-[4-(dimethylamino)phenyl]ethenyl]-2-methyltetrazolo[1,5-a]pyrimidin-2-ium
Yersinia pestis
-
pH and temperature not specified in the publication
0.0081
5-([(E)-[2-(4-chlorophenyl)-5-oxo-1,3-oxazol-4(5H)-ylidene]methyl]amino)-2-hydroxybenzoic acid
Yersinia pestis
-
pH and temperature not specified in the publication
0.00461
5-([1-[(2-chloro-1,3-thiazol-5-yl)methyl]-1H-indol-3-yl]methylidene)-1,3-dimethylpyrimidine-2,4,6(1H,3H,5H)-trione
Yersinia pestis
-
pH and temperature not specified in the publication
0.0075
5-chloro-N-[6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazol-2-yl]-1-methyl-2-(methylthio)-1H-benz-imidazole-6-carboxamide
Homo sapiens
pH 7.0, 37°C
0.0194
5-methoxy-4-[(1E)-3-(4-methoxyphenyl)-3-oxoprop-1-en-1-yl]-2-(2-methylbut-3-en-2-yl)phenyl acetate
Homo sapiens
-
pH 6.0, 37°C
0.00189
5-[3-bromo-4-[(4-nitrobenzyl)oxy]benzylidene]pyrimidine-2,4,6(1H,3H,5H)-trione
Yersinia pestis
-
pH and temperature not specified in the publication
0.00473
5-[4-(3,4-dihydroisoquinolin-2(1H)-yl)-3-nitrobenzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
Yersinia pestis
-
pH and temperature not specified in the publication
0.00989
5-[4-[(2-chloro-6-fluorobenzyl)oxy]benzylidene]-1,3-dimethylpyrimidine-2,4,6(1H,3H,5H)-trione
Yersinia pestis
-
pH and temperature not specified in the publication
0.0011 - 0.003
6,7-dihydroxy-2-(4-hydroxyphenyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0003
6-chloro-7-(2,3-dihydro-1H-inden-1-ylamino)quinoline-5,8-dione
Homo sapiens
-
0.00021
6-chloro-7-[(2-morpholin-4-ylethyl)amino]quinoline-5,8-dione
Homo sapiens
-
0.0086 - 0.0172
6-hydroxy-2-(4-hydroxybenzyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0046
6-hydroxy-3-[1-[4-(naphthalen-1-ylamino)-4-oxobutyl]-1H-1,2,3-triazol-4-yl]-2-phenyl-1-benzofuran-5-carboxylic acid
Homo sapiens
-
-
0.3
6-oxo-6H-cyclohepta[b]furan-5,7-dicarboxylic acid
Homo sapiens
above, pH 7.0, 25°C
0.003
7-(2-((1H-imidazol-2-yl)thio)ethoxy)-2-phenyl-4H-chromen-4-one
Homo sapiens
pH 7.2, 37°C
0.0016
7-(2-(1H-1,2,4-triazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
Homo sapiens
pH 7.2, 37°C
0.004
7-(2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
Homo sapiens
pH 7.2, 37°C
0.005
7-(2-(4-nitro-1H-imidazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
Homo sapiens
pH 7.2, 37°C
0.0079
7-(2-(5-methyl-1H-tetrazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
Homo sapiens
pH 7.2, 37°C
0.007
7-(3-(4-nitro-1H-imidazol-1-yl)propoxy)-2-phenyl-4H-chromen-4-one
Homo sapiens
pH 7.2, 37°C
0.0039
7-(4-((1H-imidazol-2-yl)thio)butoxy)-2-phenyl-4H-chromen-4-one
Homo sapiens
pH 7.2, 37°C
0.0036
7-(4-(1H-1,2,4-triazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
Homo sapiens
pH 7.2, 37°C
0.0069
7-(4-(2-methyl-5-nitro-1H-imidazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
Homo sapiens
pH 7.2, 37°C
0.0151
7-(4-(5-methyl-1H-tetrazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
Homo sapiens
pH 7.2, 37°C
0.00082
7-chloro-6-[(2-morpholin-4-ylethyl)amino]quinoline-5,8-dione
Homo sapiens
-
0.0074 - 0.0124
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3'',4''-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0062 - 0.0268
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3''-carboxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.001 - 0.0022
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-carboxy-3''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0082 - 0.0184
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.05
7-hydroxy-2-(4-hydroxyphenyl)-2,3-dihydro-4H-chromen-4-one
Homo sapiens
-
above, pH 6.0, 37°C
0.0065 - 0.0173
7-hydroxy-2-(4-hydroxyphenylethyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.0053 - 0.0175
7-hydroxy-2-(4-hydroxyphenylmethyl)-3-[(1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
0.00087
8-hydroxy-3-methoxy-11-oxo-1-pentanoyl-6-pentyl-11H-dibenzo[b,e][1,4]dioxepine-7-carboxylic acid
Homo sapiens
-
-
0.00019
aquastatin A
Homo sapiens
-
-
0.0081
benzyl oleanolic acid amide
Homo sapiens
-
0.00861
benzyl oleanolic acid ester
Homo sapiens
-
0.0013
CinnGel 2ME
Homo sapiens
-
-
0.012
ent-3beta-angeloyloxykaur-16-en-19-oic acid
Homo sapiens
pH 6.0, 37°C
0.012
ent-3beta-tigloyloxykaur-16-en-19-oic acid
Homo sapiens
pH 6.0, 37°C
0.01916
ethyl (4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-1,2,3,3a,3b,4,6,6a,7,9a,10,10a,10b,11,12,12a-hexadecahydrocyclopenta[5,6]naphtho[1,2-f]indazol-1-yl]pentanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.04
ethyl (4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-8-amino-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinazolin-1-yl]pentanoate
Homo sapiens
-
IC50 above 0.04 mM, pH and temperature not specified in the publication
0.0138
glycyrrhetic acid
Homo sapiens
-
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA, and 1 mM dithiothreitol, at 37°C
0.034
H2O2
Mus musculus
pH not specified in the publication, temperature not specified in the publication
0.01274 - 0.02045
lithocholic acid
0.0137
lupenone
Homo sapiens
-
pH 6.0, 37°C
0.0056
lupeol
Homo sapiens
-
pH 6.0, 37°C
0.01947
maslinic acid
Homo sapiens
-
TCPTP
0.00904
methyl (4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-8-amino-6,6,10a,12a-tetramethyl-2,3,3a,3b,4,6,10,10a,10b,11,12,12a-dodecahydro-1H-cyclopenta[7,8]phenanthro[2,3-d][1,3]thiazol-1-yl]pentanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.02822
methyl (4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinoxalin-1-yl]pentanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.00964
methyl (6S,10S)-12-(2-hydroxybenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
Mycobacterium tuberculosis
-
inhibition of MptpB
0.00826
methyl (6S,10S)-12-(3,4-dichlorobenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
Mycobacterium tuberculosis
-
inhibition of MptpB
0.0107
methyl (6S,10S)-12-(3-bromo-4-fluorobenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
Mycobacterium tuberculosis
-
inhibition of MptpB
0.0061
methyl (6S,10S)-12-(3-hydroxybenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
Mycobacterium tuberculosis
-
inhibition of MptpB
0.00471
methyl (6S,10S)-12-[(4,6-dichloro-2H-chromen-3-yl)methyl]-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
Mycobacterium tuberculosis
-
inhibition of MptpB
0.00704
methyl (6S,10S)-12-[(4-chloro-6-fluoro-2H-chromen-3-yl)methyl]-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
Mycobacterium tuberculosis
-
inhibition of MptpB
0.0116
methyl (6S,10S)-12-[(5-chloro-1H-indol-3-yl)methyl]-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
Mycobacterium tuberculosis
-
inhibition of MptpB
0.00595
methyl (6S,10S)-12-[(5-methylfuran-2-yl)methyl]-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
Mycobacterium tuberculosis
-
inhibition of MptpB
0.2
methyl 2,4-dihydroxy-6-methylbenzoate
Homo sapiens
-
above
0.00742
methyl 3,8-dimethoxy-11-oxo-1-pentanoyl-6-pentyl-11H-dibenzo[b,e][1,4]dioxepine-7-carboxylate
Homo sapiens
-
-
0.2
methyl 3-formyl-2,4-dihydroxy-6-methylbenzoate
Homo sapiens
-
above
0.01321
methyl 4,4-dimethyl-3-oxochol-5-en-24-oate
Homo sapiens
-
pH and temperature not specified in the publication
0.00037
methyl 5-amino-6-(7-amino-6-methoxy-5,8-dioxo-5,8-dihydroquinolin-2-yl)-4-(2-hydroxy-3,4-dimethoxyphenyl)-3-methylpyridine-2-carboxylate
Homo sapiens
-
0.00302
methyl 8-hydroxy-3-methoxy-11-oxo-1-pentanoyl-6-pentyl-11H-dibenzo[b,e][1,4]dioxepine-7-carboxylate
Homo sapiens
-
-
0.0092
methyl oleanolic acid amide
Homo sapiens
-
0.00444
methyl oleanolic acid ester
Homo sapiens
-
0.0018
N,N'-[benzene-1,4-diylbis(propane-2,2-diylbenzene-4,1-diyl)]bis(1,1,1-trifluoromethanesulfonamide)
Homo sapiens
-
-
0.00089
N-(1,4-dioxo-1,4-dihydronaphthalen-2-yl)-N-(4-methylphenyl)acetamide
Homo sapiens
-
0.00062
N-(3-[(4-chlorophenyl)sulfanyl]-1,4-dioxo-1,4-dihydronaphthalen-2-yl)acetamide
Homo sapiens
-
0.0409
N-(6-ethoxy-1,3-benzothiazol-2-yl)-4-nitrobenzene sulfonamide
Rattus norvegicus
-
-
0.0195
N-(6-methyl-1,3-benzothiazol-2-yl)-4-nitrobenzenesulfonamide
Rattus norvegicus
-
-
0.01
N-([4-[difluoro(phosphono)methyl]phenyl]acetyl)-a-aspartyl-4-[difluoro(phosphono)methyl]phenylalaninamide
Homo sapiens
-
-
0.0039
N-[5-(dimethylamino)-2-hydroxy-3-methoxybenzyl]-N-methyl-2-(4-nitrophenyl)ethanaminium
Homo sapiens
-
0.0313
N-[6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazol-2-yl]-2,2,2-trifluoroacetamide
Homo sapiens
pH 7.0, 37°C
0.0025
NAT6-297775
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0003
NSC-87877
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0037 - 0.0076
oleanolic acid
0.00476
oleanolic acid amide
Homo sapiens
-
0.02
oleanolic alcohol
Homo sapiens
IC50 above 0.02 mM
0.0035
oleanonic acid
Homo sapiens
-
-
0.0039
pomolic acid
Homo sapiens
-
-
0.0011
rilobolide-6-O-methacrylate
Homo sapiens
pH 6.0, 37°C
0.0109
rotungenic acid
Homo sapiens
-
-
0.002
small t antigen
Homo sapiens
-
using p-nitrophenyl phosphate as a substrate
-
0.0562
Sodium vanadate
Homo sapiens
-
0.0188
spathodic acid
Homo sapiens
-
-
0.05
stigmasterol
Homo sapiens
-
IC50 above 0.05 mM, in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA, and 1 mM dithiothreitol, at 37°C
0.05
taraxerol
Homo sapiens
-
IC50 above 0.05 mM, in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA, and 1 mM dithiothreitol, at 37°C
0.022
tetrachyrin
Homo sapiens
pH 6.0, 37°C
0.0025 - 0.004
ursolic acid
0.0156
uvaol
Homo sapiens
-
-
0.0158
[2-bromo-4-[(E)-(7,8-dimethyl-3-oxo[1,3]thiazolo[3,2-a]benzimidazol-2(3H)-ylidene)methyl]-6-ethoxyphenoxy]acetic acid
Homo sapiens
pH 7.0, 25°C
0.3
[[1-(4-chlorophenyl)-2-methyl-1H-indol-5-yl]oxy]acetic acid
Homo sapiens
above, pH 7.0, 25°C
0.00219
[[4'-(2-butyl-1-benzofuran-3-yl)biphenyl-4-yl]oxy]acetic acid
Homo sapiens
pH 7.0, 37°C, PTP-B4
0.00148
(4aS,6aS,6bR,13aR)-10-acetyl-2,2,6a,6b,9,9,13a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
Homo sapiens
-
PTPB1
0.00493
(4aS,6aS,6bR,13aR)-10-acetyl-2,2,6a,6b,9,9,13a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
Homo sapiens
-
TCPTP
0.00175
(4aS,6aS,6bR,13aR)-10-hexanoyl-2,2,6a,6b,9,9,13a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
Homo sapiens
-
PTPB1
0.00566
(4aS,6aS,6bR,13aR)-10-hexanoyl-2,2,6a,6b,9,9,13a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
Homo sapiens
-
TCPTP
0.00192
(4aS,6aS,6bR,13aR)-11-amino-2,2,6a,6b,9,9,13a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,13,13a,13b,14,15b-hexadecahydropiceno[3,2-d][1,3]thiazole-4a(2H)-carboxylic acid
Homo sapiens
-
PTPB1
0.00644
(4aS,6aS,6bR,13aR)-11-amino-2,2,6a,6b,9,9,13a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,13,13a,13b,14,15b-hexadecahydropiceno[3,2-d][1,3]thiazole-4a(2H)-carboxylic acid
Homo sapiens
-
TCPTP
0.00165
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
Homo sapiens
-
PTPB1
0.00599
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
Homo sapiens
-
TCPTP
0.0026
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,13,13a,13b,14,15b-hexadecahydropiceno[2,3-d][1,2]oxazole-4a(2H)-carboxylic acid
Homo sapiens
-
PTPB1
0.00844
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,13,13a,13b,14,15b-hexadecahydropiceno[2,3-d][1,2]oxazole-4a(2H)-carboxylic acid
Homo sapiens
-
TCPTP
0.00064
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-10-(pyridin-3-ylcarbonyl)-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
Homo sapiens
-
PTPB1
0.00439
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-10-(pyridin-3-ylcarbonyl)-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
Homo sapiens
-
TCPTP
0.00081
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-10-(pyridin-4-ylcarbonyl)-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
Homo sapiens
-
PTPB1
0.00362
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-10-(pyridin-4-ylcarbonyl)-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
Homo sapiens
-
TCPTP
0.00139
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-10-phenyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
Homo sapiens
-
PTPB1
0.0038
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-10-phenyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
Homo sapiens
-
TCPTP
0.00178
(4aS,6aS,6bR,14aR)-11-amino-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
Homo sapiens
-
PTPB1
0.00551
(4aS,6aS,6bR,14aR)-11-amino-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
Homo sapiens
-
TCPTP
0.00261
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,11,14a-octamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
Homo sapiens
-
PTPB1
0.0065
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,11,14a-octamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
Homo sapiens
-
TCPTP
0.00273
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
Homo sapiens
-
PTPB1
0.00819
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
Homo sapiens
-
TCPTP
0.00179
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinoxaline-4a(2H)-carboxylic acid
Homo sapiens
-
PTPB1
0.00831
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinoxaline-4a(2H)-carboxylic acid
Homo sapiens
-
TCPTP
0.00061
(4aS,6aS,6bR,15aR)-2,2,6a,6b,9,9,15a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,15,15a,15b,16,17b-octadecahydro-4aH-chryseno[2,1-b]carbazole-4a-carboxylic acid
Homo sapiens
-
PTPB1
0.0016
(4aS,6aS,6bR,15aR)-2,2,6a,6b,9,9,15a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,15,15a,15b,16,17b-octadecahydro-4aH-chryseno[2,1-b]carbazole-4a-carboxylic acid
Homo sapiens
-
TCPTP
0.00143
(4aS,6aS,6bR,16aR)-2,2,6a,6b,9,9,16a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,16,16a,16b,17,18b-hexadecahydrochryseno[1,2-b]phenazine-4a(2H)-carboxylic acid
Homo sapiens
-
PTPB1
0.00588
(4aS,6aS,6bR,16aR)-2,2,6a,6b,9,9,16a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,16,16a,16b,17,18b-hexadecahydrochryseno[1,2-b]phenazine-4a(2H)-carboxylic acid
Homo sapiens
-
TCPTP
0.0229
(Z)-2-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0257
(Z)-2-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
PTP1B, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0324
(Z)-2-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp1, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0008
(Z)-3-(2-(2-carboxyphenyl)hydrazono)-2-oxoindoline-5-carboxylic acid
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0015
(Z)-3-(2-(2-carboxyphenyl)hydrazono)-2-oxoindoline-5-carboxylic acid
Homo sapiens
-
PTP1B, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0154
(Z)-3-(2-(2-carboxyphenyl)hydrazono)-2-oxoindoline-5-carboxylic acid
Homo sapiens
-
Shp1, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0468
(Z)-3-(2-(2-nitrophenyl)hydrazono)-2-oxoindoline-5-sulfonic acid
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.068
(Z)-3-(2-(2-nitrophenyl)hydrazono)-2-oxoindoline-5-sulfonic acid
Homo sapiens
-
Shp1, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0967
(Z)-3-(2-(2-nitrophenyl)hydrazono)-2-oxoindoline-5-sulfonic acid
Homo sapiens
-
PTP1B, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0158
(Z)-3-(2-(3-carboxyphenyl)hydrazono)-2-oxoindoline-5-carboxylic acid
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0382
(Z)-3-(2-(3-carboxyphenyl)hydrazono)-2-oxoindoline-5-carboxylic acid
Homo sapiens
-
PTP1B, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0724
(Z)-3-(2-(3-carboxyphenyl)hydrazono)-2-oxoindoline-5-carboxylic acid
Homo sapiens
-
Shp1, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0194
(Z)-3-(2-(5-(4-chlorobenzylcarbamoyl)-2-oxoindolin-3-ylidene)-hydrazinyl)benzoic acid
Homo sapiens
-
Shp1, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0223
(Z)-3-(2-(5-(4-chlorobenzylcarbamoyl)-2-oxoindolin-3-ylidene)-hydrazinyl)benzoic acid
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.3
(Z)-3-(2-(5-(4-chlorobenzylcarbamoyl)-2-oxoindolin-3-ylidene)-hydrazinyl)benzoic acid
Homo sapiens
-
IC50 above 0.3 mM, PTP1B, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0052
(Z)-3-(2-(5-(N-(2,4-dichlorophenethyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0193
(Z)-3-(2-(5-(N-(2,4-dichlorophenethyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
PTP1B, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0734
(Z)-3-(2-(5-(N-(2,4-dichlorophenethyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp1, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0055
(Z)-3-(2-(5-(N-(2-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0159
(Z)-3-(2-(5-(N-(2-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp1, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0194
(Z)-3-(2-(5-(N-(2-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
PTP1B, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0048
(Z)-3-(2-(5-(N-(3-chloro-4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0549
(Z)-3-(2-(5-(N-(3-chloro-4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
PTP1B, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.1228
(Z)-3-(2-(5-(N-(3-chloro-4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp1, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0038
(Z)-3-(2-(5-(N-(3-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0154
(Z)-3-(2-(5-(N-(3-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
PTP1B, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0425
(Z)-3-(2-(5-(N-(3-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp1, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0106
(Z)-3-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0631
(Z)-3-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
PTP1B, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0742
(Z)-3-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp1, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0014
(Z)-3-(2-(5-(N-(4-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.018
(Z)-3-(2-(5-(N-(4-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp1, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0188
(Z)-3-(2-(5-(N-(4-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
PTP1B, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.001
(Z)-3-(2-(5-(N-(4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0145
(Z)-3-(2-(5-(N-(4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
PTP1B, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0183
(Z)-3-(2-(5-(N-(4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp1, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.005
(Z)-3-(2-(5-(N-(4-methylbenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0113
(Z)-3-(2-(5-(N-(4-methylbenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
PTP1B, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0326
(Z)-3-(2-(5-(N-(4-methylbenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp1, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0074
(Z)-4-(2-(5-(N-(2-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0117
(Z)-4-(2-(5-(N-(2-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
PTP1B, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0608
(Z)-4-(2-(5-(N-(2-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp1, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0083
(Z)-4-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0328
(Z)-4-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
PTP1B, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0431
(Z)-4-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp1, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0059
(Z)-4-(2-(5-(N-(4-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0075
(Z)-4-(2-(5-(N-(4-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
PTP1B, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0181
(Z)-4-(2-(5-(N-(4-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp1, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0063
(Z)-4-(2-(5-(N-(4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0108
(Z)-4-(2-(5-(N-(4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
Shp1, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0114
(Z)-4-(2-(5-(N-(4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
Homo sapiens
-
PTP1B, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0013
(Z)-4-(2-(5-(N-benzylsulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl) benzoic acid
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0025
(Z)-4-(2-(5-(N-benzylsulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl) benzoic acid
Homo sapiens
-
PTP1B, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0071
(Z)-4-(2-(5-(N-benzylsulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl) benzoic acid
Homo sapiens
-
Shp1, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.005
2-(4-hydroxyphenyl)-3-[(3,4-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, PTP-B1
0.0126
2-(4-hydroxyphenyl)-3-[(3,4-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, LMW-PTP isozyme 2
0.0143
2-(4-hydroxyphenyl)-3-[(3,4-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, LMW-PTP isozyme 1
0.0007
2-(4-hydroxyphenyl)-3-[(4-carboxy-3-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, LMW-PTP isozyme 1
0.0009
2-(4-hydroxyphenyl)-3-[(4-carboxy-3-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, PTP-B1
0.0057
2-(4-hydroxyphenyl)-3-[(4-carboxy-3-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, LMW-PTP isozyme 2
0.0119
3-[(2-nitrophenyl)hydrazono]-2-oxo-2,3-dihydro-1H-indole-5-sulfonamide
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.1037
3-[(2-nitrophenyl)hydrazono]-2-oxo-2,3-dihydro-1H-indole-5-sulfonamide
Homo sapiens
-
Shp1, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.1566
3-[(2-nitrophenyl)hydrazono]-2-oxo-2,3-dihydro-1H-indole-5-sulfonamide
Homo sapiens
-
PTP1B, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0044
3-[(2-nitrophenyl)hydrazono]-2-oxo-2,3-dihydro-1H-indole-5-sulfonic acid 4-chlorobenzylamide
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0098
3-[(2-nitrophenyl)hydrazono]-2-oxo-2,3-dihydro-1H-indole-5-sulfonic acid 4-chlorobenzylamide
Homo sapiens
-
PTP1B, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0409
3-[(2-nitrophenyl)hydrazono]-2-oxo-2,3-dihydro-1H-indole-5-sulfonic acid 4-chlorobenzylamide
Homo sapiens
-
Shp1, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0045
3-[N'-(5-isopropylsulfamoyl-2-oxo-1,2-dihydroindol-3-ylidene)-hydrazino]benzoic acid
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0157
3-[N'-(5-isopropylsulfamoyl-2-oxo-1,2-dihydroindol-3-ylidene)-hydrazino]benzoic acid
Homo sapiens
-
Shp1, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0371
3-[N'-(5-isopropylsulfamoyl-2-oxo-1,2-dihydroindol-3-ylidene)-hydrazino]benzoic acid
Homo sapiens
-
PTP1B, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0045
4-[N'-(5-isopropylsulfamoyl-2-oxo-1,2-dihydroindol-3-ylidene)-hydrazino]benzoic acid
Homo sapiens
-
Shp2, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0093
4-[N'-(5-isopropylsulfamoyl-2-oxo-1,2-dihydroindol-3-ylidene)-hydrazino]benzoic acid
Homo sapiens
-
PTP1B, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0277
4-[N'-(5-isopropylsulfamoyl-2-oxo-1,2-dihydroindol-3-ylidene)-hydrazino]benzoic acid
Homo sapiens
-
Shp1, in 25 mM MOPS (pH 7.0), 50 mM NaCl, 0.05% (v/v) Tween 20, 1 mM dithiothreitol, at 25°C
0.0011
6,7-dihydroxy-2-(4-hydroxyphenyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, LMW-PTP isozyme 1
0.002
6,7-dihydroxy-2-(4-hydroxyphenyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, PTP-B1
0.003
6,7-dihydroxy-2-(4-hydroxyphenyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, LMW-PTP isozyme 2
0.0086
6-hydroxy-2-(4-hydroxybenzyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, LMW-PTP isozyme 1
0.0172
6-hydroxy-2-(4-hydroxybenzyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, LMW-PTP isozyme 2
0.0074
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3'',4''-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, LMW-PTP isozyme 1
0.0077
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3'',4''-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, PTP-B1
0.0124
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3'',4''-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, LMW-PTP isozyme 2
0.0062
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3''-carboxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, PTP-B1
0.0114
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3''-carboxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, LMW-PTP isozyme 1
0.0268
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3''-carboxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, LMW-PTP isozyme 2
0.001
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-carboxy-3''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, PTP-B1
0.0013
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-carboxy-3''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, LMW-PTP isozyme 1
0.0022
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-carboxy-3''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, LMW-PTP isozyme 2
0.0082
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, LMW-PTP isozyme 1
0.017
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, PTP-B1
0.0184
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, LMW-PTP isozyme 2
0.0065
7-hydroxy-2-(4-hydroxyphenylethyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, LMW-PTP isozyme 1
0.0173
7-hydroxy-2-(4-hydroxyphenylethyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, LMW-PTP isozyme 2
0.0053
7-hydroxy-2-(4-hydroxyphenylmethyl)-3-[(1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, LMW-PTP isozyme 1
0.0175
7-hydroxy-2-(4-hydroxyphenylmethyl)-3-[(1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH 7.0, 37°C, LMW-PTP isozyme 2
0.00001
ISIS 113715
Macaca mulatta
-
IC50 less than 0.00001 mM
-
0.00001
ISIS 113715
Macaca fascicularis
-
IC50 less than 0.00001 mM
-
0.01274
lithocholic acid
Homo sapiens
-
PTP1B, pH and temperature not specified in the publication
0.02045
lithocholic acid
Homo sapiens
-
TCPTP, pH and temperature not specified in the publication
0.0037
oleanolic acid
Homo sapiens
-
0.0076
oleanolic acid
Homo sapiens
-
-
0.0041
RK-682
Homo sapiens
-
-
0.0045
RK-682
Homo sapiens
-
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA, and 1 mM dithiothreitol, at 37°C
0.0045
RK-682
Homo sapiens
-
pH 6.0, 37°C
0.0025
ursolic acid
Homo sapiens
-
-
0.00308
ursolic acid
Homo sapiens
-
-
0.0031
ursolic acid
Homo sapiens
-
-
0.00374
ursolic acid
Homo sapiens
-
in 50 mM citrate (pH 6.0), 1 mM dithiothreitol, 1 mM EDTA, and 0.1 M NaCl, at 37°C
0.004
ursolic acid
Homo sapiens
in 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA and 1 mM dithiothreitol, at 37°C
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C10S
-
complete loss of activity
R16K
-
complete loss of activity
D194A
-
compared to wild-type, 5.4% activity with 4-nitrophenyl phosphate
D3A
-
compared to wild-type, 8% activity with 4-nitrophenyl phosphate
H136A
-
compared to wild-type, 7.7% activity with 4-nitrophenyl phosphate
H196A
-
compared to wild-type, 4.1% activity with 4-nitrophenyl phosphate
H42A
-
compared to wild-type, 6.8% activity with 4-nitrophenyl phosphate
H5A
-
compared to wild-type, 9.5% activity with 4-nitrophenyl phosphate
H7A
-
compared to wild-type, 6.3% activity with 4-nitrophenyl phosphate
C236A
Bracoviriform demolitoris
-
inactive mutant
C236S
Bracoviriform demolitoris
-
site-directed mutagenesis, mutant PTP-H2C236S, the non-fusion mutant has almost no enzymatic activity, while the thioredoxin-fusion form has low levels of activity
C649S
-
construction of a myc-tagged PTP3DELTAC649S mutant
C237S
-
catalytically dead mutant
D203A
-
substrate-trapping mutant
416AA
-
of PTPalpha, Km-value similar to wild-type, up to 2fold activation by tetrasodium 2-(((2-(3-(((3-(5-((2,5-disulfonatophenyl)carbamoyl)-1H-benzimidazol-2-yl)phenyl)carbamoyl)amino)phenyl)-1H-benzimidazol-5-yl)carbonyl)amino)benzene-1,4-disulfonate
529AA
-
of PTPalpha, Km-value similar to wild-type, up to 11.6fold activation by tetrasodium 2-(((2-(3-(((3-(5-((2,5-disulfonatophenyl)carbamoyl)-1H-benzimidazol-2-yl)phenyl)carbamoyl)amino)phenyl)-1H-benzimidazol-5-yl)carbonyl)amino)benzene-1,4-disulfonate
A122F
site-directed mutagenesis, affects inhibition by abietic acid and 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
A122S
site-directed mutagenesis, affects inhibition by abietic acid
A189S
site-directed mutagenesis, affects inhibition by 3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethylbenzofuran-6-sulfonic acid-[4-(thiazol-2-ylsulfamyl)phenyl]-amide and 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
A455N/V457Y/E597D
site-directed mutagenesis, the triple mutant of the PTPepsilon D2 domain is constructed to reconstitute the residues of the PTPepsilon D1 catalytic domain that are important for phosphatase activity, resulting in only a slight increase in the phosphatase activity compared with the wild-type D2 protein. The mutant is used for structure-based drug design
C1108S
-
mutant lacks catalytic activity
C1239S
-
catalytically inactive
C124S
-
site-directed mutagenesis, inactive mutant
C129S
-
decreased activity
C195A
-
site-directed mutagenesis, catalytically inactive mutant comprising residues 1-294, specific interaction between the Lyp substrate-trapping mutant and SKAP-HOM
C215D
active-site mutant, similar Km-values as wild type, but reduced kcat-values and activation by 1,2-epoxy-3-(p-nitrophenoxy)propane, use as substrate-trapping mutant
C216S
-
phosphatase-dead mutant of TCPTP
C227S
-
site-directed mutagenesis, catalytically inactive mutant comprising residues 1-294, specific interaction between the Lyp substrate-trapping mutant and SKAP-HOM
C231S
-
phosphatase-dead mutant of PEST
C258M
-
isoform PTP1B, mutation turns 1B isoform to PTPalpha-like enzyme in substrate recognition
C270A
inactive, substrate-trapping mutant of the HePTP catalytic domain (HePTP residues 44-339)
C270S
inactive, substrate-trapping mutant of the HePTP catalytic domain (HePTP residues 44-339)
C270S/T106D
inactive, substrate-trapping mutant of the HePTP catalytic domain (HePTP residues 44-339)
C377S
catalytically inactive Cdc25C
C433S
-
phosphatase-dead mutant of PTPalpha
C455S
crystallization data
C459S
-
substrate-trapping mutant of SHP2
C473D
active site mutant, weak substrate affinity and dissociates rapidly
C473S
strong substrate affinity and dissociates slowly
C488S
catalytically inactive Cdc25B
C92A
site-directed mutagenesis, affects inhibition by abietic acid and 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
C945S
-
site-directed mutagenesis of the essential cysteine residue to a serine in the islet cell antigen-related PTP results in the expression of the intracellular region which does not catalyze hydrolysis of 4-nitrophenyl phosphate
D195A/C227S
-
optimized substrate-trap mutant, used for identification of physiological enzyme substrates
D236A
substrate-trapping mutant of the HePTP catalytic domain (HePTP residues 44-339), shows 420fold reduced activity compared to the wild type enzyme
D236A/C270A/Q314A
inactive, substrate-trapping mutant of the HePTP catalytic domain (HePTP residues 44-339)
D236A/C270S/Q314A
inactive, substrate-trapping mutant of the HePTP catalytic domain (HePTP residues 44-339)
D236A/Q314A
substrate-trapping mutant of the HePTP catalytic domain (HePTP residues 44-339), shows 1255fold reduced activity compared to the wild type enzyme
D284A
-
catalytically inactive, no significant effect on proliferation in human umbilical vein endothelial cells
D48N
-
isoform PTP1B, mutation turns 1B isoform to PTPalpha-like enzyme in substrate recognition
D61G
-
the mutation causes hyperactivation of the SHP2 catalytic activity
D811A/C842S
site-directed mutagenesis, analysis of binding structure of substrate Eps15846-854 compared to wild-type enzyme and enzyme PTP1B
D811A/H812F/C842S/M883G
site-directed mutagenesis, analysis of binding structure of substrate Eps15846-854 compared to wild-type enzyme and enzyme PTP1B. THe mutant acts as a surrogate of the PTP1B active site, in complex with substrate Eps15846-854. Introduction of M883G substitution increased the flexibility of the side chain of Q886, thus facilitating interaction between F812 and the pTyr-Pro motif. In this complex structure, the phenyl side chain of F812 is shifted 3.7 A away from the active site pocket
D811E/C842S
site-directed mutagenesis, analysis of binding structure of substrate Eps15846-854 compared to wild-type enzyme and enzyme PTP1B
D92A
-
site-directed mutagenesis, the D92A mutation causes a 250 to 700fold reduction in phospholipid phosphatase activity of PTEN, the mutation perturbs the structure and function of the active site imposing significantly different impacts on the two activities of PTEN
E187C
site-directed mutagenesis, altered kinetics compared to the wild-type enzyme
E187C/S188C
site-directed mutagenesis, altered kinetics compared to the wild-type enzyme
F135Y
site-directed mutagenesis, affects inhibition by abietic acid, 3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethylbenzofuran-6-sulfonic acid-[4-(thiazol-2-ylsulfamyl)phenyl]-amide, and 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
F182H
isoform PTP1B, exchange of residue 182 with that of isoform PTPH1, modulation of functionality of catalytic center
F182Y
site-directed mutagenesis, affects inhibition by abietic acid and 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
F183C
site-directed mutagenesis, altered kinetics compared to the wild-type enzyme
F196Y
site-directed mutagenesis, affects inhibition by abietic acid and 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
F280Y
site-directed mutagenesis, does not affect abietane-type diterpenoids as inhibitors
F28A
-
decreased activity
G117E
-
mutant of PTP-1B, 45% increase in Km-value, decrease in kcat-value
G129E
-
naturally occuring mutation, the Cowden syndrome-associated G129E mutation abrogates the phospholipid phosphatase activity but not the phosphoprotein phosphatase activity of PTEN, the mutation perturbs the structure and function of the active site imposing significantly different impacts on the two activities of PTEN, complete loss of phospholipid phosphatase activity of the G129E PTEN mutant
G184C
site-directed mutagenesis, altered kinetics compared to the wild-type enzyme
G259Q
-
isoform PTP1B, mutation turns 1B isoform to PTPalpha-like enzyme in substrate recognition
G259S
site-directed mutagenesis, affects inhibition by 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
G496V
-
of PTPalpha, 70% increase in Km-value, up to 13.5fold activation by tetrasodium 2-(((2-(3-(((3-(5-((2,5-disulfonatophenyl)carbamoyl)-1H-benzimidazol-2-yl)phenyl)carbamoyl)amino)phenyl)-1H-benzimidazol-5-yl)carbonyl)amino)benzene-1,4-disulfonate
H175A
site-directed mutagenesis, affects inhibition by abietic acid and 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
H182F
isoform PTP1B, exchange of residue 182 with that of isoform PTPB1, modulation of functionality of catalytic center
K138A
-
increased activity
L119V
-
of PTP-1B, 30% decrease in kcat-value, crystallization data
L29A
-
decreased activity
M114V
-
mutant of PTP-1B, activity similar to wild-type
M258C
-
isoform PTPalpha, mutation turns alpha isoform to PTP1B-like enzyme in substrate recognition
N48D
-
isoform PTPalpha, mutation turns alpha isoform to PTP1B-like enzyme in substrate recognition
P181C
site-directed mutagenesis, altered kinetics compared to the wild-type enzyme
P181C/E187C
site-directed mutagenesis, altered kinetics compared to the wild-type enzyme
P181C/P186C
site-directed mutagenesis, altered kinetics compared to the wild-type enzyme
P186C
site-directed mutagenesis, altered kinetics compared to the wild-type enzyme
P186C/E187C
site-directed mutagenesis, altered kinetics compared to the wild-type enzyme
P87C/A122C
mutant asPTP1B, design of non-natural allosteric-inhibition sites in PTPs, in which a tricysteine moiety is engineered within the PTP catalytic domain at a conserved location outside of the active site. Introduction of the tricysteine motif, which does not exist in any wild-type PTP, serves to sensitize target PTPs to inhibition by a biarsenical compound, providing a generalizable strategy for the generation of allosterically sensitized (as) PTPs. The potency, selectivity, and kinetics of asPTP inhibition can be significantly improved by exploring the inhibitory action of a range of biarsenical compounds that differ in interarsenical distance, steric bulk, and electronic structure
Q259G
-
isoform PTPalpha, mutation turns alpha isoform to PTP1B-like enzyme in substrate recognition
Q314A
substrate-trapping mutant of the HePTP catalytic domain (HePTP residues 44-339), shows 13fold reduced activity compared to the wild type enzyme
R112A
site-directed mutagenesis, affects inhibition by abietic acid, 3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethylbenzofuran-6-sulfonic acid-[4-(thiazol-2-ylsulfamyl)phenyl]-amide, and 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
R33A
-
decreased activity
R362K
-
the Shp2 mutant shows a strongly decreased affinity for the inhibitor phenylhydrazonopyrazolone sulfonate 1
R47V
-
isoform PTP1B, mutation turns 1B isoform to PTPalpha-like enzyme in substrate recognition
R47V/D48N/M258C/G259Q
molecular dynamics simulations of the crystal structure, in comparison to wild-type, movement of Q262 is restricted
R492L
hotspot mutant, dramatically decreased activity despite showing no significant changes in crystal structure
S19A
site-directed mutagenesis, mutant PTPN12-S19A is efficient in inhibiting EGF-induced cell migration, the mutant does not produce significant differences in PTPN12's recognition of all HER2-phospho-peptides compared to wild-type PTPN12
S19E
site-directed mutagenesis, mutant PTPN12-S19E is less efficient in inhibiting EGF-induced cell migration, the mutant does not produce significant differences in PTPN12's recognition of all HER2-phospho-peptides compared to wild-type PTPN12
S295F
affects minimally catalytic activity, significantly reduces the potency of inhibitors derived from 7-bromo-6-difluoromethylphosphonate 3-naphthalenenitrile
S35E
-
decreased activity
S35E/T36E
-
increased activity
S39E
site-directed mutagenesis, the mutant impairs activity of PTPN12 toward all HER2-phosphopeptide by 2-3fold compared to wild-type, mutation S39E decreases the activity of PTPN12 toward all tested HER2 pY sites in vitro, the mutation directly affected the interaction between the PTPN12 and the residues flanking the pY of the HER2 phosphorylation sites
T106D
KIM-PTP specific substrate-trapping mutant, the introduced aspartate side chain facilitates the coordination of the bound peptides, thereby stabilizing the active dephosphorylation complex
T36E
-
decreased activity
up
-
hypoxia inducible factor-2, HIF-2, preferential activation of PTPRZ1 by HIF-2, involving ELK1, an E26 transformation-specific factor that can bind to HIF-2alpha but not HIF-1alpha. A deletion mutation of one of the two Ets binding motifs located near the principal hypoxia response element similarly decreases activation of the PTPRZ1 promoter by HIF-2. IFand Ets both bind to motifs on the PTPRZ1 promoter and cooperate inpreferential upregulation of PTPRZ1, binding of HIF-2 and ELK1 to nearby sites on the PTPRZ1 promoter region, overview
V113I
-
mutant of PTP-1B, activity similar to wild-type
V113I/M114V
-
mutant of PTP-1B, 50% decrease in kcat-value
V113T
site-directed mutagenesis, does not affect abietane-type diterpenoids as inhibitors
V121L
-
of isoform TCPTP, high increase in sensitivity against 4-((3E)-1-(1H-benzotriazol-1-yl)-1-(4-(difluoro(phosphono)methyl)benzyl)-4-phenylbut-3-en-1-yl)benzoic acid and (difluoro(4-((4E)-2-((4-fluorophenyl)carbonyl)-2-(4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)-5-phenylpent-4-en-1-yl)phenyl)methyl)phosphonic acid
V185C
site-directed mutagenesis, altered kinetics compared to the wild-type enzyme
V451M
site-directed mutagenesis, the mutation lies in a conserved motif adjacent to the protein tyrosine phosphatase (PTP) consensus sequence and alters catalytic function. Mutant V451M possesses increased catalytic activity as compared to the wild-type enzyme. When assayed with 4-nitrophenyl phosphatase as substrate, mutant V451M shows higher activity regardless of the pNPP substrate concentration used. The mutant shows increased thermolability compared to wild-type
V457Y/E597D
site-directed mutagenesis
V47R
-
isoform PTPalpha, mutation turns alpha isoform to PTP1B-like enzyme in substrate recognition
W179F
site-directed mutagenesis, the mutation in PTP1B causes only a minor reduction in kcat of about 2fold at pH 5.5, and the pH-rate profile remains fully bell-shaped. The kinetic isotopic effects are similar to those of the wild-type PTP1B showing that general acid catalysis remains effective. The affinity of the competitive inhibitors tungstate and molybdate for the active site is not affected by the W179F mutation. Crystal structures of the W179F mutant of PTP1B show the availability of both the normal loop open and closed positions, consistent with the kinetic results
Y152A/Y153A
site-directed mutagenesis, the mutation attenuates allosteric communication between the C-terminus and the WPD loop, affects inhibition by abietic acid, 3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethylbenzofuran-6-sulfonic acid-[4-(thiazol-2-ylsulfamyl)phenyl]-amide, and 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
Y46A
site-directed mutagenesis, substitution of Y46 with alalnine in PTP1B results in a 380fold increase in Km using pNPP as a substrate
Y497A
shows a significantly slower rate constant for association compared to that of the wild type enzyme
Y676I
site-directed mutagenesis, analysis of binding structure of substrate Eps15846-854 compared to wild-type enzyme and enzyme PTP1B, mutant Y676I mutant loses the catalytic activity completely
C215S
-
the mutant is catalytically inactive
C243S
very low stimulation by dithiothreitol
C297S
protein displays a complete lack of tetrameric species
C35S
very low stimulation by dithiothreitol
C453S
-
a catalytically inactive, dominant negative mutant of SHP-1
C459S
-
phosphatase-dead mutant of Shp2
D34N
phosphatase-inactive mutant. Knockin replacement of murine Pgp with its D34N mutant is embryonically lethal
D437A
-
catalytically inactive
R340M
-
catalytically inactive
R619W
naturally occuring polymorphisms, phenotype, overview. Ptpn22-/- mice and Ptpn22R619W mutant mice are backcrossed for more than 10 generations to the C57BL/6 strain, genotyping and phenotyping in bone marrow derived dendritic cell culture, overview
Y131A
-
residue phosphorylated during platelet-derived growth factor signaling, physiological role
Y132A
-
residue phosphorylated during platelet-derived growth factor signaling, physiological role
R619W
-
naturally occuring polymorphisms, phenotype, overview. Ptpn22-/- mice and Ptpn22R619W mutant mice are backcrossed for more than 10 generations to the C57BL/6 strain, genotyping and phenotyping in bone marrow derived dendritic cell culture, overview
-
C11S
-
MPtpA catalytic site, no enzymic activity
C160S
-
MPtpB catalytic site, no enzymic activity
C16A
-
the mutant retains the activity similar to the wild type enzyme
C53A
-
the mutant is insensitive to S-nitrosoglutathione treatment
D112N
-
GST fusion protein, no enzymic activity
D115N
-
GST fusion protein, no enzymic activity
D76N
-
GST fusion protein, no enzymic activity
H148N
-
GST fusion protein, no enzymic activity
H44N
-
GST fusion protein, acitivity slightly lower than wild-type
H78N
-
GST fusion protein, 8fold reduction of activity compared to wild-type
I115F
the mutant enzyme possesses a higher kcat at low temperatures compared to the wild type enzyme, the thermostability of the I115F mutant enzyme exhibits higher catalytic efficiency than the wild type enzyme
I115L
the mutant enzyme possesses a kcat at low temperatures similar to the wild type enzyme
I115M
the mutant enzyme possesses a higher kcat at low temperatures compared to the wild type enzyme, the thermostability of the I115M mutant enzyme exhibits higher catalytic efficiency than the wild type enzyme
I115V
the mutant enzyme possesses a kcat at low temperatures similar to the wild type enzyme
I307A
the mutant enzyme possesses a lower kcat at low temperatures compared to the wild type enzyme
I307F
the mutant enzyme possesses a lower kcat at low temperatures compared to the wild type enzyme
I307L
the mutant enzyme possesses a lower kcat at low temperatures compared to the wild type enzyme
I307M
the mutant enzyme possesses a lower kcat at low temperatures compared to the wild type enzyme
L145A
the mutant enzyme possesses a lower kcat at low temperatures compared to the wild type enzyme
L145F
the mutant enzyme possesses a lower kcat at low temperatures compared to the wild type enzyme
L145M
the mutant enzyme possesses a lower kcat at low temperatures compared to the wild type enzyme
L145V
the mutant enzyme possesses a lower kcat at low temperatures compared to the wild type enzyme
V79A
the mutant enzyme possesses a lower kcat at low temperatures compared to the wild type enzyme
V79I
the mutant enzyme possesses a lower kcat at low temperatures compared to the wild type enzyme
V79L
the mutant enzyme possesses a lower kcat at low temperatures compared to the wild type enzyme
V85F
the mutant enzyme possesses a lower kcat at low temperatures compared to the wild type enzyme
V85I
the mutant enzyme possesses a lower kcat at low temperatures compared to the wild type enzyme
V85L
the mutant enzyme possesses a lower kcat at low temperatures compared to the wild type enzyme
V85M
the mutant enzyme possesses a lower kcat at low temperatures compared to the wild type enzyme
D120A
-
site-directed mutagenesis, the mutation abrogates activity of PtpA with the artificial phosphatase substrate 4-nitrophenol phosphate, confirming its essentiality for function
C8A
site-directed mutagenesis, inactive enzyme mutant of SP-PTP
R14A
site-directed mutagenesis, the enzyme mutant of SP-PTP shows highly reduced activity compared to wild-type
D415A
-
isoform SynPPM3, no activity with 4-nitrophenyl phosphate, reduction in phosphoserine- and phosphotyrosine-activity against casein and carboxyamidomethylated and maleylated lysozyme
D415N
-
isoform SynPPM3, 5% activity with 4-nitrophenyl phosphate compared to wild-type, 50% reduction in phosphotyrosine-activity against carboxyamidomethylated and maleylated lysozyme
D444N
-
isoform SynPPM3, no activity with 4-nitrophenyl phosphate, reduction in phosphoserine- and phosphotyrosine-activity against casein and carboxyamidomethylated and maleylated lysozyme
D604N
-
isoform SynPPM3, no activity
D608N
-
isoform SynPPM3, 50% activity with 4-nitrophenyl phosphate compared to wild-type, 4fold increase in phosphotyrosine-activity against carboxyamidomethylated and maleylated lysozyme
D648N
-
isoform SynPPM3, 5% activity with 4-nitrophenyl phosphate compared to wild-type, large reduction in phosphoserine- and phosphotyrosine-activity against casein and carboxyamidomethylated and maleylated lysozyme
E414Q
-
isoform SynPPM3, similar activity with 4-nitrophenyl phosphate as wild-type, but 50% reduction in phosphoserine- and phosphotyrosine-activity against casein and carboxyamidomethylated and maleylated lysozyme
E618Q
-
isoform SynPPM3, 87% of activity with 4-nitrophenyl phosphate compared to wild-type, reduction in phosphoserine- and phosphotyrosine-activity against casein and carboxyamidomethylated and maleylated lysozyme
C93S
site-directed mutagenesis, inactive mutant
D63A
site-directed mutagenesis, the mutant shows reduced activity compared to wild-type
D63N
site-directed mutagenesis, the mutant shows reduced activity compared to wild-type
D63N/E132A
site-directed mutagenesis, the mutant shows reduced activity compared to wild-type
E132A
site-directed mutagenesis, the mutant shows about 1.5fold increased activity compared to wild-type
E132L
site-directed mutagenesis, the mutant shows reduced activity compared to wild-type
E132Q
site-directed mutagenesis, the mutant shows about 2.5fold increased activity compared to wild-type
G95A
site-directed mutagenesis, the mutant shows about 10fold increased activity compared to wild-type
Q136A
site-directed mutagenesis, the mutant shows reduced activity compared to wild-type
R124A
site-directed mutagenesis, the mutant shows reduced activity compared to wild-type
R124E
site-directed mutagenesis, the mutant shows reduced activity compared to wild-type
C93S
-
site-directed mutagenesis, inactive mutant
-
E132A
-
site-directed mutagenesis, the mutant shows about 1.5fold increased activity compared to wild-type
-
E132Q
-
site-directed mutagenesis, the mutant shows about 2.5fold increased activity compared to wild-type
-
Q136A
-
site-directed mutagenesis, the mutant shows reduced activity compared to wild-type
-
R124A
-
site-directed mutagenesis, the mutant shows reduced activity compared to wild-type
-
C93S
-
site-directed mutagenesis, inactive mutant
-
E132A
-
site-directed mutagenesis, the mutant shows about 1.5fold increased activity compared to wild-type
-
E132Q
-
site-directed mutagenesis, the mutant shows about 2.5fold increased activity compared to wild-type
-
Q136A
-
site-directed mutagenesis, the mutant shows reduced activity compared to wild-type
-
R124A
-
site-directed mutagenesis, the mutant shows reduced activity compared to wild-type
-
A33D
-
interferes with substrate binding
D356N
-
dramatically reduced activity, D356 acts as general acid/base
N34D
-
interferes with substrate binding
Q11R
-
interferes with substrate binding
R409A
-
dramatical decrease in kcat, 26-fold increase in Km-value
R409K
-
dramatical decrease in kcat, 1.9-fold increase in Km-value
V31G
-
interferes with substrate binding
416AA
-
of PTPalpha, Km-value similar to wild-type, up to 2fold activation by NF506
529AA
-
of PTPalpha, Km-value similar to wild-type, up to 11.6fold activation by NF506
C403S
-
a catalytically inactive mutant YopH
D356N
-
site-directed mutagenesis, a general acid mutant, catalytically inactive mutant, altered kinetic isotopic effects compared to wild-type
G496V
-
of PTPalpha, 70% increase in Km-value, up to 13.5fold activation by NF506
R409K
-
site-directed mutagenesis, the kcat for the R409K mutant of YopH is lower by four orders of magnitude and kinetic isotopic effects resemble those for the general acid mutant D356N
W354A
-
site-directed mutagenesis, the more drastic mutation to alanine in this position (W354A) results in a further reduction in rate compared to W354F, a full flattening of the basic limb of the pH-rate profile, and kinetic isotopic effects that are consistent with total loss of general acid catalysis. The W354A mutant cannot be crystallized, but the kinetic and kinetic isotopic effect data suggest that the WPD loop positioning is more compromised than in mutant W354F, and not even partial neutralization of the leaving group is possible
W354F
-
site-directed mutagenesis, the mutation in YopH results in a decrease in kcat by two orders of magnitude, loss of the basic limb of the pH-rate profile, and kinetic isotopic effects consistent with the leaving group departing as the anion, the mutant hsows an impaired general acid catalysis. The WPD loop in this mutant is immobile, fixed in a quasi-open position that leaves the Asp 356 side chain too far from the active site to effectively protonate the leaving group. The intermediate position of the WPD-loop in the W354F mutant evidently permits an intervening water molecule, bridging the aspartic acid and the substrate, to partially neutralize the leaving group during 4-nitrophenyl phosphate catalysis. The W354F mutation in YopH reduces the binding affinity for tungstate by about 6fold
C215S
crystallization data, in complex with substrates bis-(para-phosphophenyl) methane and 4-nitrophenyl phosphate
C215S
-
phosphatase-dead mutant of PTP1B
D181A
-
substrate-trapping mutant, kinetic and thermodynamic characterization
D181A
-
substrate-trapping mutant
D181A/Q262A
-
substrate-trapping mutant, kinetic and thermodynamic characterization, very high affinity for epidermal growth factor receptor
D181A/Q262A
-
substrate-trapping mutant
D811E
site-directed mutagenesis, analysis of binding structure of substrate Eps15846-854 compared to wild-type enzyme and enzyme PTP1B
D811E
site-directed mutagenesis, ectopic expression of the D811E mutant form of PTPN3 does not reduce phosphorylation of substrate peptide Eps15
E76K
-
leukemia-associated Shp2 mutant
E76K
-
the mutation causes hyperactivation of the SHP2 catalytic activity, dephosphorylation of STAT5 by SHP2 E76K is delayed
H812F
site-directed mutagenesis, analysis of binding structure of substrate Eps15846-854 compared to wild-type enzyme and enzyme PTP1B. The H812F mutant form of PTPN3 behaves similarly to the wild-type PTP1B, showing a 9fold increase in Km and a 3.6fold decrease in kcat relative to the wild-type PTPN3
H812F
site-directed mutagenesis, ectopic expression of the H812F mutant form of PTPN3 does not reduce phosphorylation of substrate peptide Eps15
C172S
site-directed mutagenesis
C172S
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site-directed mutagenesis
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D245A
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catalytically inactive
D245A
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substrate-trapping mutant
R283M
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inactive
R283M
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catalytically inactive
D126A
site-directed mutagenesis, mutant PtpA D126A behaves similarly to the PtpA wild-type through the whole expression and purification procedure, suggesting that this mutation does not significantly alter the enzyme structure, but there is a small rearrangement in the protein conformation of the mutant. PtpA wild-type and PtpA D126A mutant present similar values of Km , while the kcat for PtpA D126A is 40fold lower compared to wild-type PtpA, mutant D126A is barely active. PtpA D126A is covalently immobilized on a CM5 sensor chip to assess by surface plasmon resonance (SPR) its ability to bind specifically to macrophage components, SPR analysis of protein-protein interaction, overview
D126A
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site-directed mutagenesis, mutant PtpA D126A behaves similarly to the PtpA wild-type through the whole expression and purification procedure, suggesting that this mutation does not significantly alter the enzyme structure, but there is a small rearrangement in the protein conformation of the mutant. PtpA wild-type and PtpA D126A mutant present similar values of Km , while the kcat for PtpA D126A is 40fold lower compared to wild-type PtpA, mutant D126A is barely active. PtpA D126A is covalently immobilized on a CM5 sensor chip to assess by surface plasmon resonance (SPR) its ability to bind specifically to macrophage components, SPR analysis of protein-protein interaction, overview
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D126A
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site-directed mutagenesis, mutant PtpA D126A behaves similarly to the PtpA wild-type through the whole expression and purification procedure, suggesting that this mutation does not significantly alter the enzyme structure, but there is a small rearrangement in the protein conformation of the mutant. PtpA wild-type and PtpA D126A mutant present similar values of Km , while the kcat for PtpA D126A is 40fold lower compared to wild-type PtpA, mutant D126A is barely active. PtpA D126A is covalently immobilized on a CM5 sensor chip to assess by surface plasmon resonance (SPR) its ability to bind specifically to macrophage components, SPR analysis of protein-protein interaction, overview
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C10S
inactive, no dephosphorylation of phospho-Ptk1
C10S
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inactive, no dephosphorylation of phospho-Ptk1
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C8S
site-directed mutagenesis, mutation in the putative active site cysteine, almost inactive enzyme mutant
C8S
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site-directed mutagenesis, mutation in the putative active site cysteine, almost inactive enzyme mutant
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C235R
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indistinguishable from wild-type, the truncated enzyme YOP*DELTA162 has no altered catalytic properties
C235R
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the mutation results in enhanced enzyme stability
additional information
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overexpression of PTP3 inhibits nuclear accumulation of STATc at the slug stage
additional information
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truncated enzyme forms with reduced Km for 4-nitrophenyl phosphate
additional information
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design of further substrate-trapping mutants
additional information
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truncation mutant expressing the catalytic domain, significantly higher vmax and lower Km-values
additional information
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down-regulation of enzyme activity with small molecule inhibitors suppresses cell spreading and migration to fibronectin, increases Y527 phosphorylation in Src, and decreases phosphorylation of focal adhesion kinase, p130 Crk-associated substrate, and extracellular signal-regulated kinase 1/2
additional information
the mutants TCPTP-187 , PTP1B-186, HePTP-211, FAP-1-2364 , PTP-PEST-204 have a CCPGCC-insertion that leads to sensitisation toward fluorescein arsenical hairpin binder protein, the CCPGCC-insertion mutants PTPH1-816 and PTPalpha-406 are particularly attractive as inhibitor-sensitized enzymes in that they demonstrate kinetic parameters that are essentially indistinguishable (or marginally improved, in the case of PTPalpha-406) from the corresponding wild type enzymes in the absence of an allele-specific inhibitor
additional information
development of an engineering method for insertion of a chemical off switch into the catalytically essential loop region, the socalled WPD loop, of a protein tyrosine phosphatase using a combination of point mutations and amino acid insertions, the mutants displays FlAsH-binding cysteine residues, overview. Inhibition of the FlAsH-sensitized TCPTP mutants is rapid and specific, and strong FlAsH sensitivity is observed in mutants that contain as few as two cysteine point mutations in their engineered WPD loops
additional information
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knockdown of SHP-1 by small interfering RNA suppresses the effect of guggulsterone on induction of SHP-1 and on the inhibition of STAT3 activation
additional information
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knockdown of SHP-1 inhibits G1/S progression in prostate cancer cells through the regulation of components of the cell-cycle machinery. SHP-1 depletion in PC-3 cells induces by small interfering RNAs causes G1 phase cell-cycle arrest accompanied by changes in some components of the cellcycle machinery. SHP-1 knockdown increases p27Kip1 protein stability, its nuclear localization and p27 gene transcription. SHP-1 knockdown decreases the CDK6 levels, inducing retinoblastoma protein hypophosphorylation, downregulation of cyclin E and thereby a decrease in the CDK2 activity. Phenotype, overview
additional information
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knockout of isozyme p66shc significantly enhances IGF-I-dependent SHPS-1/SHP-2/Src/p52shc/Grb2 complex formation, and p52shc tyrosine phosphorylation and Grb2 association, while overexpression inhibits it, overview. Disruption of the SHP-2/SHPS-1 complex is associated with a reduction in Src and SHPS-1 as well as Src and p52shc association
additional information
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generation of stable cell lines expressing a short hairpin RNA targeting the phosphatase transcript and reduction of PTP1B expression levels down to 20%. Upon PTP1B overexpression, phosphorylation of PLC-gamma1 and Gab1 sharply decreases when compared with controls where PLC-gamma1 and Gab1 phosphorylations
additional information
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GST pull-down experiment with pervanadate-treated, to increase and preserve tyrosine phosphorylation RAW264.7 cell lysates with either GST alone, wild-type Lyp fused to GST (GST-Lyp), or the substrate-trapping fusion proteins GST-Lyp/C227S and GST-Lyp/D195A. Whereas no protein retained by GST or GST-Lyp is detectable, the GST-Lyp/C227S and GST-Lyp/D195A trapping mutants specifically bound SKAP-HOM, the failure to detect association of SKAP-HOM with wild-type Lyp indicates that the interaction between the Lyp trapping mutants and SKAP-HOM requires tyrosine phosphorylation
additional information
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the catalytically critical loop of the PTP domain, the WPD loop, can be engineered to contain cysteine-rich elements that bind the inhibitory biarsenical reagent
additional information
development and evaluation of a method for production and recovery of the properly folded intracellular domain of IA-2 fused to thioredoxin (TrxIA-2ic) in Escherichia coli GI698 and GI724 strains, overview
additional information
ectopic expression of the D811E or H812F mutant form of PTPN3 fails to reduce the level of endogenous EGFR and the phosphorylation of mitogen-activated protein kinase (MAPK) in response to EGF stimulation. Transfection of human embryonic kidney HEK293T cells with the wild-type PTPN3 significantly decreases EGF-induced Y849 phosphorylation of Eps15, whereas ectopic expression of the D811E or H812F mutant form of PTPN3 does not affect the Y849 phosphorylation levels of Eps15. In the H1975 line-derived from human non-small-cell lung cancer, in which the wild-type form of PTPN3 can downregulate EGFR signaling via dephosphorylating Eps15, ectopic expression of the D811E or H812F mutant form of PTPN3 fails to reduce the level of endogenous EGFR and the phosphorylation of mitogen-activated protein kinase (MAPK) in response to EGF stimulation
additional information
ectopic expression of the D811E or H812F mutant form of PTPN3 fails to reduce the level of endogenous EGFR and the phosphorylation of mitogen-activated protein kinase (MAPK) in response to EGF stimulation. Transfection of human embryonic kidney HEK293T cells with the wild-type PTPN3 significantly decreases EGF-induced Y849 phosphorylation of Eps15, whereas ectopic expression of the D811E or H812F mutant form of PTPN3 does not affect the Y849 phosphorylation levels of Eps15. In the H1975 line-derived from human non-small-cell lung cancer, in which the wild-type form of PTPN3 can downregulate EGFR signaling via dephosphorylating Eps15, ectopic expression of the D811E or H812F mutant form of PTPN3 fails to reduce the level of endogenous EGFR and the phosphorylation of mitogen-activated protein kinase (MAPK) in response to EGF stimulation
additional information
ectopic expression of the D811E or H812F mutant form of PTPN3 fails to reduce the level of endogenous EGFR and the phosphorylation of mitogen-activated protein kinase (MAPK) in response to EGF stimulation. Transfection of human embryonic kidney HEK293T cells with the wild-type PTPN3 significantly decreases EGF-induced Y849 phosphorylation of Eps15, whereas ectopic expression of the D811E or H812F mutant form of PTPN3 does not affect the Y849 phosphorylation levels of Eps15. In the H1975 line-derived from human non-small-cell lung cancer, in which the wild-type form of PTPN3 can downregulate EGFR signaling via dephosphorylating Eps15, ectopic expression of the D811E or H812F mutant form of PTPN3 fails to reduce the level of endogenous EGFR and the phosphorylation of mitogen-activated protein kinase (MAPK) in response to EGF stimulation
additional information
ectopic expression of the D811E or H812F mutant form of PTPN3 fails to reduce the level of endogenous EGFR and the phosphorylation of mitogen-activated protein kinase (MAPK) in response to EGF stimulation. Transfection of human embryonic kidney HEK293T cells with the wild-type PTPN3 significantly decreases EGF-induced Y849 phosphorylation of Eps15, whereas ectopic expression of the D811E or H812F mutant form of PTPN3 does not affect the Y849 phosphorylation levels of Eps15. In the H1975 line-derived from human non-small-cell lung cancer, in which the wild-type form of PTPN3 can downregulate EGFR signaling via dephosphorylating Eps15, ectopic expression of the D811E or H812F mutant form of PTPN3 fails to reduce the level of endogenous EGFR and the phosphorylation of mitogen-activated protein kinase (MAPK) in response to EGF stimulation
additional information
ectopic expression of the D811E or H812F mutant form of PTPN3 fails to reduce the level of endogenous EGFR and the phosphorylation of mitogen-activated protein kinase (MAPK) in response to EGF stimulation. Transfection of human embryonic kidney HEK293T cells with the wild-type PTPN3 significantly decreases EGF-induced Y849 phosphorylation of Eps15, whereas ectopic expression of the D811E or H812F mutant form of PTPN3 does not affect the Y849 phosphorylation levels of Eps15. In the H1975 line-derived from human non-small-cell lung cancer, in which the wild-type form of PTPN3 can downregulate EGFR signaling via dephosphorylating Eps15, ectopic expression of the D811E or H812F mutant form of PTPN3 fails to reduce the level of endogenous EGFR and the phosphorylation of mitogen-activated protein kinase (MAPK) in response to EGF stimulation
additional information
generation of the isolated intracellular catalytic domain of PTP-oc (DELTAPTP-oc)
additional information
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generation of the isolated intracellular catalytic domain of PTP-oc (DELTAPTP-oc)
additional information
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in thymocytes of enzyme-deficient animal, cells develop normally, but show increased tyrosine phosphorylation of specific proteins, increased Fyn activity due to enhanced phosphorylation of Y528 and Y417, and hyperphosphorylation of Cbp/PAG
additional information
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construction of PTPH1 knockout mice, no immunological phenotype in primary T cells derived from PTPH1-KO mice, carrageenan induces a trend of slightly increased spontaneous pain sensitivity in PTPH1-KO mice compared to wild-type littermates, but no differences in cytokine release, induced pain perception and cellular infiltration, but LPS-induced TNFalpha, MCP-1, and IL10 release is significantly reduced in PTPH1-KO plasma compared to wild-type plasma, overview
additional information
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generation of PTP1B-/- mice, neuron-specific PTP1B-/- mice, and muscle specific-PTP1B-/- mice. Neuronal PTP1B-deficient mutant mice show inhibition of hypothalamic AMP-activated protein kinase, AMPK, and isoform-specific activation of AMPK in peripheral tissues, e.g. muscle and adipose tissue, overview
additional information
generation of specific shRNA cell lines for DEP-1 knockout
additional information
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generation of specific shRNA cell lines for DEP-1 knockout
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additional information
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enzyme activity is significantly suppressed in the liver microsomes of regucalcin transgenic rats
additional information
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the DELTAsiw14 disruptant exhibits caffeine sensitivity
additional information
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genetic deletion of ptpA or ptpB does not affect in vitro growth or cell wall integrity
additional information
A-549 human lung cells infected with group A Streptococcus (GAS) mutants lacking enzyme SP-PTP display increased Ser-/Thr-/Tyr-phosphorylation. Generation of a M1T1DELTAPTP enzyme knockout mutant, phenotype, overview
additional information
A-549 human lung cells infected with group A Streptococcus (GAS) mutants lacking enzyme SP-PTP display increased Ser-/Thr-/Tyr-phosphorylation. Generation of Streptoccocus pyogenes mutant lacking the ptp-(Spy_0036) gene derived from the Type M1 M1T15448 strain by allelic replacement
additional information
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A-549 human lung cells infected with group A Streptococcus (GAS) mutants lacking enzyme SP-PTP display increased Ser-/Thr-/Tyr-phosphorylation. Generation of Streptoccocus pyogenes mutant lacking the ptp-(Spy_0036) gene derived from the Type M1 M1T15448 strain by allelic replacement
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additional information
Q6JHV2
mutantv enzyme lacking C-terminal CAAX motif localizes to the cytoplasm
additional information
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mutantv enzyme lacking C-terminal CAAX motif localizes to the cytoplasm
additional information
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overview
additional information
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study on regions for substrate binding and for chaperone binding for translocation
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