Information on EC 3.4.22.52 - calpain-1

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The expected taxonomic range for this enzyme is: Eukaryota

EC NUMBER
COMMENTARY hide
3.4.22.52
-
RECOMMENDED NAME
GeneOntology No.
calpain-1
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REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
broad endopeptidase specificity
show the reaction diagram
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
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endopeptidase; peptides, endopeptidase
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CAS REGISTRY NUMBER
COMMENTARY hide
689772-75-6
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78990-62-2
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ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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SwissProt
Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
strain FCR-3
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Manually annotated by BRENDA team
strain FCR-3
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
metabolism
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calpain 1 is involved in the degradation of endothelial nitric oxide synthase and heat shock protein 90 and the phosphorylation of endothelial nitric oxide synthase
physiological function
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
(4-(4-dimethylaminophenylazo)benzoyl)-TPLKSPPPSPR-(5[(2-aminoethyl)amino]naphthalene-1-sulfonic acid) + H2O
(4-(4-dimethylaminophenylazo)benzoyl)-TPLK + SPPPSPR-(5[(2-aminoethyl)amino]naphthalene-1-sulfonic acid)
show the reaction diagram
-
-
-
-
?
(5(6)-carboxyfluorescin)-GGGQLYGG-(Nbeta-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)-RRK-(5- and 6-carboxytetramethylrhodamine)-OH + H2O
(5(6)-carboxyfluorescin)-GGGQLY + GG-(Nbeta-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)-RRK-(5- and 6-carboxytetramethylrhodamine)-OH
show the reaction diagram
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-
-
-
?
(EDANS)-EALFAERK-(DABCYL) + H2O
(EDANS)-EA + LFAERK-(DABCYL)
show the reaction diagram
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about 30% cleavage preference
-
-
?
(EDANS)-EPLFAARK-(DABCYL) + H2O
(EDANS)-EPLFA + ARK-(DABCYL)
show the reaction diagram
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the sequence PLFAAR is an even better substrate for the calpain 1 protease core than PLFAER, 100% cleavage preference
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-
?
(EDANS)-EPLFAERK-(DABCYL) + H2O
(EDANS)-EPLFA + ERK-(DABCYL)
show the reaction diagram
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about 40% cleavage preference
-
-
?
(EDANS)-EPLFGERK-(DABCYL) + H2O
(EDANS)-EPLF + GERK-(DABCYL)
show the reaction diagram
-
less than 20% cleavage preference
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-
?
(EDANS)-EPLFMERK-(DABCYL) + H2O
(EDANS)-EPLF + MERK-(DABCYL)
show the reaction diagram
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the peptide sequence PLFMER is rapidly cleaved by the calpain 1 core at the F-M bond with about 45% cleavage preference
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?
2',3'-cyclic nucleotide 3'-phosphodiesterase + H2O
?
show the reaction diagram
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?
2-aminobenzoyl-EVYGMMY(3-NO2)-OH + H2O
2-aminobenzoyl-EVY + GMMY(3-NO2)-OH
show the reaction diagram
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-
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?
4,4-difluoro-5,7-dimethyl-4-bora-31,4a-diaza-s-indacene-3-propioyl-labeled casein + H2O
?
show the reaction diagram
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-
-
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?
5-([4,6-dichlorotriazin-2-yl]amino)fluorescin-labeled microtubule-associated protein 2 + H2O
?
show the reaction diagram
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-
-
-
?
7-methoxycoumarin-4-acetyl-GGGNIFGG-(Nbeta-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)-KK-OH + H2O
7-methoxycoumarin-4-acetyl-GGGNIF + GG-(Nbeta-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)-KK-OH
show the reaction diagram
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-
-
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?
7-methoxycoumarin-4-acetyl-GGGNIYGG-(Nbeta-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)-KK-OH + H2O
7-methoxycoumarin-4-acetyl-GGGNIY + GG-(Nbeta-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)-KK-OH
show the reaction diagram
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-
-
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?
7-methoxycoumarin-4-acetyl-GGGNLFGG-(Nbeta-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)-KK-OH + H2O
7-methoxycoumarin-4-acetyl-GGGNLF + GG-(Nbeta-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)-KK-OH
show the reaction diagram
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-
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?
7-methoxycoumarin-4-acetyl-GGGNLYGG-(Nbeta-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)-KK-OH + H2O
7-methoxycoumarin-4-acetyl-GGGNLY + GG-(Nbeta-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)-KK-OH
show the reaction diagram
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-
-
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?
7-methoxycoumarin-4-acetyl-GGGQIFGG-(Nbeta-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)-KK-OH + H2O
7-methoxycoumarin-4-acetyl-GGGQIF + GG-(Nbeta-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)-KK-OH
show the reaction diagram
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-
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?
7-methoxycoumarin-4-acetyl-GGGQLFGG-(Nbeta-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)-KK-OH + H2O
7-methoxycoumarin-4-acetyl-GGGQLF + GG-(Nbeta-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)-KK-OH
show the reaction diagram
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?
7-methoxycoumarin-4-acetyl-GGGQLYGG-(Nbeta-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)-KK-OH + H2O
7-methoxycoumarin-4-acetyl-GGGQLY + GG-(Nbeta-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)-KK-OH
show the reaction diagram
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?
acetyl-Leu-Leu-Tyr-7-amido-4-trifluoromethyl coumarin + H2O
?
show the reaction diagram
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?
acetyl-LLY-7-amido-4-fluoromethylcoumarin + H2O
acetyl-LLY + 7-amino-4-fluoromethylcoumarin
show the reaction diagram
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?
AIF + H2O
?
show the reaction diagram
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?
alpha-actinin + H2O
?
show the reaction diagram
alpha-fodrin + H2O
?
show the reaction diagram
alpha-II-spectrin + H2O
?
show the reaction diagram
alpha-spectrin
?
show the reaction diagram
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-
-
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?
alpha-spectrin + H2O
?
show the reaction diagram
alpha-spectrin II + H2O
?
show the reaction diagram
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-
-
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?
alpha-subunit of fodrin + H2O
150000 Da fragment + ?
show the reaction diagram
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?
alpha-synuclein + H2O
145000 DA fragment + 150 Da fragment + ?
show the reaction diagram
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-
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?
alphaII-spectrin + H2O
?
show the reaction diagram
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Fanconi anemia proteins play an important role in maintaining the stability of alphaII-spectrin in the cell by regulating its cleavage by mu-calpain
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?
apoptosis inducing factor + H2O
truncated apoptosis inducing factor + ?
show the reaction diagram
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?
apoptosis-inducing factor + H2O
?
show the reaction diagram
apoptosis-inducing factor + H2O
truncated apoptosis-inducing factor + ?
show the reaction diagram
Bax protein + H2O
?
show the reaction diagram
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-
-
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?
beta-integrin + H2O
?
show the reaction diagram
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?
Bfl-1 protein + H2O
?
show the reaction diagram
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mu-calpain cleaves Bfl-1 at two major sites in its N-terminus releasing three fragments of 28000 Da, 12000 Da and 17500 Da
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?
BH3-only Bcl2 interacting domain + H2O
?
show the reaction diagram
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BH3-only Bcl2 interacting domain is a direct target of a soluble active calpain 1 present in cells expressing hepatitis C virus proteins
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?
Boc-Leu-Met-7-amido-4-chloromethylcoumarin + H2O
Boc-Leu-Met + 7-amino-4-chloromethylcoumarin
show the reaction diagram
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10 microM, 20 min, 37 C, with or without magnetic bead stimulation
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?
casein + H2O
?
show the reaction diagram
caspase-7 + H2O
?
show the reaction diagram
-
recombinant caspase-7 is directly cleaved and activated by calpain-1 within the large subunit of caspase-7 to produce the large subunit p18 and p17
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?
collapsin response mediator protein 1 + H2O
?
show the reaction diagram
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?
collapsin response mediator protein 2 + H2O
?
show the reaction diagram
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?
collapsin response mediator protein 3 + H2O
?
show the reaction diagram
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?
collapsin response mediator protein 4 + H2O
?
show the reaction diagram
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-
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?
COX-2 + H2O
?
show the reaction diagram
-
-
-
-
?
cyclin dependent kinase-5 + H2O
p25-CDK5
show the reaction diagram
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-
-
-
?
desmin + H2O
?
show the reaction diagram
dye-Gln-Gln-Gln-Glu-Val-Tyr-Gly-Met-Met-Pro-Arg-Asp-pSer-Ala + H2O
dye-Gln-Gln-Gln-Glu-Val-Tyr + Gly-Met-Met-Pro-Arg-Asp-pSer-Ala
show the reaction diagram
-
-
-
-
?
E-(EDANS)-PLFAERK-(Dabcyl) + H2O
?
show the reaction diagram
-
-
-
-
?
E-(EDANS-)PLF-AERK-(Dabcyl) + H2O
?
show the reaction diagram
-
-
-
-
?
filamin A + H2O
?
show the reaction diagram
-
-
-
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?
filamin-1 + H2O
?
show the reaction diagram
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-
-
-
?
fluorescin thiocarbamoyl-labeled casein + H2O
?
show the reaction diagram
-
-
-
-
?
fodrin + H2O
?
show the reaction diagram
Frizzled-7 + H2O
?
show the reaction diagram
full-length glutamic acid decraboxylase67 + H2O
truncated glutamic acid decarboxylase67 + ?
show the reaction diagram
gamma-filamin + H2O
?
show the reaction diagram
Hsp70.1 + H2O
?
show the reaction diagram
-
Hsp70.1 in the CA-1 tissue is an in-vivo substrate of activated mu-calpain, carbonylated Hsp70.1 in the CA-1 tissue by artificial oxidative stressors such as hydroxynonenal or hydrogen peroxide is much more vulnerable to the calpain cleavage
-
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?
human epithelial growth factor receptor 2 + H2O
75000 Da fragment + 42000 Da fragment
show the reaction diagram
-
overexpression of calpain1 or activation of endogenous calpain during adhesion or trastuzumab treatment of trastuzumab-sensitive cells induces cleavage of cytoplasmic domains of human epithelial growth factor receptor 2/phospho-human epithelial growth factor receptor 2 protein
-
-
?
I-kappaBalpha polymer + H2O
?
show the reaction diagram
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-
-
-
?
insulin-like growth factor binding protein-2 + H2O
?
show the reaction diagram
-
the primary cleavage site in insulin-like growth factor binding protein-2 is localized to the non-conserved central linker regions
-
-
?
insulin-like growth factor binding protein-3 + H2O
?
show the reaction diagram
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the primary cleavage site in insulin-like growth factor binding protein-3 is localized to the non-conserved central linker regions. In vitro binding of mu-calpain to insulin-like growth factor binding protein-3 is a Ca2+-dependent reaction with a rapid on/off rate
-
-
?
integrin + H2O
?
show the reaction diagram
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-
-
-
?
integrin beta3 + H2O
?
show the reaction diagram
-
-
-
-
?
K-(5(6)-carboxyfluorescein)-EVYGMMK(4-(4-dimethylaminophenylazo)benzoyl)-OH + H2O
K-(5(6)-carboxyfluorescein)-EVY + GMMK(4-(4-dimethylaminophenylazo)benzoyl)-OH
show the reaction diagram
-
-
-
-
?
L-plastin + H2O
?
show the reaction diagram
-
L-plastin interaction with integrin is regulated through cleavage of beta-integrin by micro-calpain
-
-
?
LIS1 protein + H2O
?
show the reaction diagram
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-
-
-
?
lysosomal associated membrane protein 2 + H2O
?
show the reaction diagram
MAP2 + H2O
?
show the reaction diagram
mature apoptosis-inducing factor (62 kDa) + H2O
cleaved apoptosis-inducing factor (57 kDa) + ?
show the reaction diagram
-
cleaved by the mitochondrial mu-calpain near its N-terminus
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-
?
microtubule-associated protein 1
?
show the reaction diagram
-
-
-
-
?
microtubule-associated protein 2
?
show the reaction diagram
-
-
-
-
?
microtubule-associated protein 2 + H2O
?
show the reaction diagram
-
calpain translates high-frequency Ca2+ transients into decomposition of its sensitive substrate microtubule-associated protein 2
-
-
?
mitochondrial major Ca2+ extruding pathway Na+/Ca2+ exchanger + H2O
?
show the reaction diagram
-
cleaved by the mitochondrial mu-calpain
-
-
?
myelin-associated glycoprotein + H2O
?
show the reaction diagram
myofibril + H2O
?
show the reaction diagram
-
-
-
-
?
myofibrillar protein + H2O
?
show the reaction diagram
-
-
-
-
?
N-acetyl-LLY-7-amido-4-fluoromethylcoumarin + H2O
N-acetyl-LLY + 7-amino-4-fluoromethylcoumarin
show the reaction diagram
-
-
-
-
N-acetyl-LLY-7-amido-4-fluromethylcoumarin + H2O
N-acetyl-LLY + 7-amino-4-fluoromethylcoumarin
show the reaction diagram
-
-
-
-
?
N-benzyloxycarbonyl-L-Leu-L-Arg-4-methoxy-2-naphthylamide + H2O
N-benzyloxycarbonyl-L-Leu-L-Arg + 4-methoxy-2-naphthylamine
show the reaction diagram
-
-
-
-
?
N-benzyloxycarbonyl-L-Leu-L-Arg-7-amido-4-methylcoumarin + H2O
N-benzyloxycarbonyl-L-Leu-L-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
N-benzyloxycarbonyl-L-Leu-L-Arg-7-amido-4-trifluoromethylcoumarin + H2O
N-benzyloxycarbonyl-L-Leu-L-Arg + 7-amino-4-trifluoromethylcoumarin
show the reaction diagram
-
-
-
-
?
N-succinyl-L-leucyl-L-valyl-L-tyrosinyl-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
N-succinyl-Leu-Tyr-7-amido-4-methylcoumarin + H2O
N-succinyl-Leu-Tyr + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
N-succinyl-LLVY-7-amido-4-methylcoumarin + H2O
N-succinyl-LLVY + 7-amino-4-methylcoumarin
show the reaction diagram
Na+/Ca2+ exchanger isoform 3 + H2O
?
show the reaction diagram
-
-
-
-
?
neuronal calcium sensor-1 + H2O
?
show the reaction diagram
-
mu-calpain cleavage of neuronal calcium sensor-1 occurs within an N-terminal pseudoEF-hand domain (at Lys36), which is unable to bind Ca2+
-
-
?
neuronal nitric oxide synthase + H2O
?
show the reaction diagram
nNOS + H2O
?
show the reaction diagram
-
-
-
-
?
NR2 subunit of NMDA subtype of glutamate receptor + H2O
?
show the reaction diagram
-
all three subtypes of NR2 subunits can be proteolyzed, cleavage of NR2A, NR2B and NR2C subunits is limited to their C-terminal region. Two cleavage sites at amino acids 1279 and 1330. Cleavage of NR2A-containing receptors does not alter basic NMDA receptor properties including calcium uptake, MK801 binding or electrophysiological measurement
-
-
?
NR2B subunit of NMDA receptor + H2O
?
show the reaction diagram
-
-
-
-
?
p12 subunit of human DNA polymerase delta + H2O
?
show the reaction diagram
-
the proteolysis of p12 by mu-calpain may be through a DNA polymerase delta4/PCNA complex. The p12/DNA polymerase delta is a target as a nuclear substrate of mu-calpain in calcium-triggered apoptosis
-
-
?
p35 + H2O
p25 + ?
show the reaction diagram
-
-
-
-
?
plasma membrane Ca2+-ATPase isoform 1 + H2O
?
show the reaction diagram
-
readily and completely degraded by m-calpain
-
-
?
plasma membrane Ca2+-ATPase isoform 2 + H2O
?
show the reaction diagram
-
slow hydrolysis only to large fragments
-
-
?
plasma membrane Ca2+-ATPase isoform 4 + H2O
?
show the reaction diagram
-
slow hydrolysis only to large fragments
-
-
?
podoplanin + H2O
?
show the reaction diagram
-
podoplanin stability is post-translationally regulated by calpain-1
-
-
?
pro-interleukin-33 + H2O
interleukin-33 + ?
show the reaction diagram
-
-
-
-
?
Rad21 + H2O
?
show the reaction diagram
-
calpain-1 cleaves Rad21 at Leu192
-
-
?
recombinant procaspase-3 + H2O
?
show the reaction diagram
recombinant procaspase-9 + H2O
?
show the reaction diagram
RecTat101 + H2O
?
show the reaction diagram
-
-
-
-
?
RhoA + H2O
?
show the reaction diagram
spectrin + H2O
?
show the reaction diagram
striatal-enriched protein tyrosine phosphatase + H2O
?
show the reaction diagram
-
calpain-cleavage of striatal-enriched protein tyrosine phosphatase 61 is NMDAR-dependent, Cdk5 enhances calpain-mediated cleavage of striatal-enriched protein tyrosine phosphatase 61, calpain cleaves recombinant striatal-enriched protein tyrosine phosphatase 46 in a dose-dependent manner
-
-
?
succinyl-bovine serum albumin + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-bovine-serum-albumin + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-casein + H2O
?
show the reaction diagram
succinyl-insulin B + H2O
?
show the reaction diagram
succinyl-L-Leu-L-Leu-L-Val-7-amido-4-methylcoumarin + H2O
succinyl-L-Leu-L-Leu-L-Val + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
succinyl-L-Leu-L-Leu-L-Val-L-Tyr-7-amido-4-methylcoumarin + H2O
succinyl-L-Leu-L-Leu-L-Val-L-Tyr + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
succinyl-L-Leu-L-Met-7-amido-4-methylcoumarin + H2O
succinyl-L-Leu-L-Met + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
succinyl-L-Leu-L-Tyr-4-methoxy-2-naphthylamide + H2O
succinyl-L-Leu-L-Tyr + 4-methoxy-2-naphthylamine
show the reaction diagram
-
-
-
-
?
succinyl-L-Leu-L-Tyr-7-amido-4-methylcoumarin + H2O
succinyl-L-Leu-L-Tyr + 7-amino-4-methylcoumarin
show the reaction diagram
succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-Leu-Tyr-4-methylcoumaryl-7-amide + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-LLVY-7-amido-4-methylcoumarin + H2O
succinyl-LLVY + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
succinyl-protamine + H2O
?
show the reaction diagram
talin + H2O
?
show the reaction diagram
tau protein + H2O
?
show the reaction diagram
-
-
-
-
?
tert-butyloxycarbonyl-L-Leu-L-Met-7-amido-4-chloromethylcoumarin + H2O
tert-butyloxycarbonyl-L-Leu-L-Met + 7-amino-4-chloromethylcoumarin
show the reaction diagram
-
-
-
-
?
tert-butyloxycarbonyl-L-Leu-L-Met-7-amido-4-methylcoumarin + H2O
tert-butyloxycarbonyl-L-Leu-L-Met + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
tert-butyloxycarbonyl-L-leucyl-L-methionine-7-amido-4-chloromethylcoumarin + H2O
tert-butyloxycarbonyl-L-leucyl-L-methionine + 7-amino-4-chloromethylcoumarin
show the reaction diagram
-
-
-
-
?
tert-butyloxycarbonyl-L-Val-L-Leu-L-Lys-7-amido-4-methylcoumarin + H2O
tert-butyloxycarbonyl-L-Val-L-Leu-L-Lys + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
tert-butyloxycarbonyl-Leu-Met-7-amido-4-chloromethylcoumarin + H2O
tert-butyloxycarbonyl-Leu-Met + 7-amino-4-chloromethylcoumarin
show the reaction diagram
-
-
-
-
?
titin + H2O
?
show the reaction diagram
troponin + H2O
?
show the reaction diagram
-
-
-
-
?
troponin complex + H2O
?
show the reaction diagram
utrophin + H2O
?
show the reaction diagram
-
-
-
-
?
vimentin + H2O
?
show the reaction diagram
-
-
-
-
?
[2-Abz]-Ser-Thr-Phe-Ala-Gln-Pro-[3-nitrotyrosine]-NH2 + H2O
[2-Abz]-Ser-Thr-Phe + Ala-Gln-Pro-[3-nitrotyrosine]-NH2
show the reaction diagram
-
-
-
-
?
[4-((4-(dimethylamino)phenyl)azo)benzoic acid, succinimidyl ester]-Thr-Pro-Leu-Lys-Ser-Pro-Pro-Pro-Ser-Pro-Arg-[5-((2-aminoethyl)amino)naphthalene-1-sulfonic acid] + H2O
?
show the reaction diagram
-
-
-
-
?
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
alpha-actinin + H2O
?
show the reaction diagram
alpha-spectrin + H2O
?
show the reaction diagram
alpha-spectrin II + H2O
?
show the reaction diagram
-
-
-
-
?
alphaII-spectrin + H2O
?
show the reaction diagram
-
Fanconi anemia proteins play an important role in maintaining the stability of alphaII-spectrin in the cell by regulating its cleavage by mu-calpain
-
-
?
apoptosis inducing factor + H2O
truncated apoptosis inducing factor + ?
show the reaction diagram
-
-
-
-
?
apoptosis-inducing factor + H2O
?
show the reaction diagram
-
although calpain I cleaves recombinant apoptosis-inducing factor in a cell free system, in intact cells under conditions where endogenous calpain is activated by either N-methyl-D-aspartate or N-methyl-N'-nitro-N-nitrosoguanidine administration, apoptosis-inducing factor is not cleaved
-
-
?
apoptosis-inducing factor + H2O
truncated apoptosis-inducing factor + ?
show the reaction diagram
caspase-7 + H2O
?
show the reaction diagram
-
recombinant caspase-7 is directly cleaved and activated by calpain-1 within the large subunit of caspase-7 to produce the large subunit p18 and p17
-
-
?
desmin + H2O
?
show the reaction diagram
filamin A + H2O
?
show the reaction diagram
-
-
-
-
?
filamin-1 + H2O
?
show the reaction diagram
-
-
-
-
?
fodrin + H2O
?
show the reaction diagram
Frizzled-7 + H2O
?
show the reaction diagram
-
calpain-1 is a regulator of Frizzled-7 turnover at the plasma membrane
-
-
?
full-length glutamic acid decraboxylase67 + H2O
truncated glutamic acid decarboxylase67 + ?
show the reaction diagram
-
in mu-calpain knockout mice, the level of truncated glutamic acid decarboxylase67 in the brain is greatly reduced compared with the wild-type. mu-Calpain is activated by neuronal stimulation and Ca2+-influx
-
-
?
I-kappaBalpha polymer + H2O
?
show the reaction diagram
-
-
-
-
?
integrin + H2O
?
show the reaction diagram
-
-
-
-
?
lysosomal associated membrane protein 2 + H2O
?
show the reaction diagram
MAP2 + H2O
?
show the reaction diagram
mature apoptosis-inducing factor (62 kDa) + H2O
cleaved apoptosis-inducing factor (57 kDa) + ?
show the reaction diagram
-
cleaved by the mitochondrial mu-calpain near its N-terminus
-
-
?
microtubule-associated protein 2 + H2O
?
show the reaction diagram
-
calpain translates high-frequency Ca2+ transients into decomposition of its sensitive substrate microtubule-associated protein 2
-
-
?
mitochondrial major Ca2+ extruding pathway Na+/Ca2+ exchanger + H2O
?
show the reaction diagram
-
cleaved by the mitochondrial mu-calpain
-
-
?
myelin-associated glycoprotein + H2O
?
show the reaction diagram
-
calpain overexpression due to *OH stress, IFN-gamma stimulation, or Ca2+ influx is involved in C6 cell death
-
-
?
Na+/Ca2+ exchanger isoform 3 + H2O
?
show the reaction diagram
-
-
-
-
?
neuronal nitric oxide synthase + H2O
?
show the reaction diagram
NR2B subunit of NMDA receptor + H2O
?
show the reaction diagram
-
-
-
-
?
p12 subunit of human DNA polymerase delta + H2O
?
show the reaction diagram
-
the proteolysis of p12 by mu-calpain may be through a DNA polymerase delta4/PCNA complex. The p12/DNA polymerase delta is a target as a nuclear substrate of mu-calpain in calcium-triggered apoptosis
-
-
?
p35 + H2O
p25 + ?
show the reaction diagram
-
-
-
-
?
Rad21 + H2O
?
show the reaction diagram
-
calpain-1 cleaves Rad21 at Leu192
-
-
?
recombinant procaspase-3 + H2O
?
show the reaction diagram
recombinant procaspase-9 + H2O
?
show the reaction diagram
RhoA + H2O
?
show the reaction diagram
-
calpain cleaves RhoA and generates a form that inhibits integrin-induced stress fiber assembly and cell spreading
-
-
?
spectrin + H2O
?
show the reaction diagram
striatal-enriched protein tyrosine phosphatase + H2O
?
show the reaction diagram
-
calpain-cleavage of striatal-enriched protein tyrosine phosphatase 61 is NMDAR-dependent, Cdk5 enhances calpain-mediated cleavage of striatal-enriched protein tyrosine phosphatase 61, calpain cleaves recombinant striatal-enriched protein tyrosine phosphatase 46 in a dose-dependent manner
-
-
?
talin + H2O
?
show the reaction diagram
tau protein + H2O
?
show the reaction diagram
-
-
-
-
?
titin + H2O
?
show the reaction diagram
troponin complex + H2O
?
show the reaction diagram
utrophin + H2O
?
show the reaction diagram
-
-
-
-
?
vimentin + H2O
?
show the reaction diagram
-
-
-
-
?
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
((1S)-1-((((1S)-1-benzyl-3-cyclopropylamino-2,3-di-oxopropyl)amino)carbonyl)-3-methylbutyl)carbamic acid 5-methoxy-3-oxapentyl ester
-
SNJ-1945
(-)-epicatechin 5-gallate
-
-
(2S)-2-[[(4-fluorophenyl)sulfonyl]amino]-N-[(3S)-2-hydroxytetrahydrofuran-3-yl]-3-methylbutanamide
-
-
(2S,3S)-trans-epoxysuccinyl-L-leucylamido-3-methylbutane ethyl ester
-
broad-spectrum calpain inhibitor
(2S,5S)-5-benzyl-6-hydroxy-2-(2-methylpropyl)morpholin-3-one
-
SNJ-1757
(3S)-2-hydroxytetrahydrofuran-3-yl N-[(10H-phenothiazin-2-yloxy)acetyl]-L-threonyl-L-leucinate
-
-
(3S)-2-hydroxytetrahydrofuran-3-yl N-[(2S)-2-[[(10H-phenothiazin-2-yloxy)acetyl]amino]butanoyl]-L-leucinate
-
-
(3S)-3-[[N-(10H-phenothiazin-2-ylcarbonyl)-L-norvalyl]amino]tetrahydrofuran-2-yl acetate
-
BN-82270
(4S)-3-[(4-methylphenyl)sulfonyl]-N-(1-oxo-3-phenylpropan-2-yl)-1,3-thiazolidine-4-carboxamide
-
-
(6S,9S,16R)-6-(hydroxymethyl)-9-(2-methylpropyl)-16-phenyl-2,15-dioxa-7,10,13-triazabicyclo[16.2.2]docosa-1(20),18,21-triene-8,11,14-trione
-
-
(6S,9S,16R)-9-(2-methylpropyl)-8,11,14-trioxo-16-phenyl-2,15-dioxa-7,10,13-triazabicyclo[16.2.2]docosa-1(20),18,21-triene-6-carbaldehyde
-
less potent inhibitor with greater than 2fold selectivity for ovine calpain 1 over calpain 2
(7S,10S,13S,26S)-13,26-dibenzyl-7-methyl-10-(propan-2-yl)-5,7,8,10,11,13,14,25,26,28-decahydrotetrabenzo[k,m,t,v][1,4,7,10,15,18]hexaazacyclotetracosine-6,9,12,15,24,27-hexone
-
-
(7S,10S,17R)-10-(2-methylpropyl)-9,12,15-trioxo-17-phenyl-2,16-dioxa-8,11,14-triazabicyclo[17.2.2]tricosa-1(21),19,22-triene-7-carbaldehyde
-
potent inhibitor of calpain with greater than 7fold selectivity for ovine calpain 2 over ovine calpain 1
(7S,10S,17R)-7-(hydroxymethyl)-10-(2-methylpropyl)-17-phenyl-2,16-dioxa-8,11,14-triazabicyclo[17.2.2]tricosa-1(21),19,22-triene-9,12,15-trione
-
-
(8S,11S,18R)-11-(2-methylpropyl)-10,13,16-trioxo-18-phenyl-2,17-dioxa-9,12,15-triazabicyclo[18.2.2]tetracosa-1(22),20,23-triene-8-carbaldehyde
-
-
(8S,11S,18R)-8-(hydroxymethyl)-11-(2-methylpropyl)-18-phenyl-2,17-dioxa-9,12,15-triazabicyclo[18.2.2]tetracosa-1(22),20,23-triene-10,13,16-trione
-
-
(9R,12S,19R)-12-(2-methylpropyl)-11,14,17-trioxo-19-phenyl-2,18-dioxa-7-thia-10,13,16-triazabicyclo[19.2.2]pentacosa-1(23),21,24-triene-9-carbaldehyde
-
-
(9R,12S,19R)-9-(hydroxymethyl)-12-(2-methylpropyl)-19-phenyl-2,18-dioxa-7-thia-10,13,16-triazabicyclo[19.2.2]pentacosa-1(23),21,24-triene-11,14,17-trione
-
-
([(2Z)-2-[(3S)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetyl]oxy)ethynyl (2Z)-[(3R)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]ethanoate
-
-
1,2-bis(o-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid tetra(acetoxymethyl) ester
-
-
1-(2-chloro-4-hydroxyphenyl)-4-oxo-7-(pyridin-4-yl)-1,4-dihydroquinoline-3-carboxamide
-
-
1-[(4-methylphenyl)sulfonyl]-N-(1-oxo-3-phenylpropan-2-yl)-D-prolinamide
-
-
2-methyl-N-[(2S)-1-oxo-3-phenylpropan-2-yl]-7,8-dihydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
-
3,4-dichlorophenyl (2-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]ethyl)amidosulfite
-
IC50: 56 nM
3,4-dichlorophenyl (3-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]propyl)amidosulfite
-
IC50: 56 nM
3-([4-[2-(methoxymethoxy)phenyl]-4-oxobutanoyl]amino)-2-oxo-4-phenylbutanamide
-
reversible inhibitor
3-([N-[(benzyloxy)carbonyl]-L-leucyl]amino)-2-oxo-4-phenylbutanoic acid
-
reversible inhibitor
3-acetyl-2-[(2,4-dichlorophenyl)amino]-8-(trifluoromethyl)quinolin-4(1H)-one
-
-
3-acetyl-2-[(3-fluorophenyl)amino]-8-phenylquinolin-4(1H)-one
-
-
3-acetyl-2-[(4-chlorophenyl)amino]-5,8-difluoroquinolin-4(1H)-one
-
-
3-acetyl-2-[(4-tert-butylphenyl)amino]-5,8-difluoroquinolin-4(1H)-one
-
-
3-acetyl-2-[(4-tert-butylphenyl)amino]-8-chloro-6-nitroquinolin-4(1H)-one
-
-
3-acetyl-2-[[3,5-bis(trifluoromethyl)phenyl]amino]-5,8-difluoroquinolin-4(1H)-one
-
-
3-acetyl-5,8-dibromo-2-[(4-bromophenyl)amino]quinolin-4(1H)-one
-
-
3-acetyl-5,8-dichloro-2-[(2,4-dichlorophenyl)amino]quinolin-4(1H)-one
-
-
3-acetyl-6,8-difluoro-2-[(2,4,5-trifluorophenyl)amino]quinolin-4(1H)-one
-
-
3-acetyl-6-chloro-2-[(2,4-dichlorophenyl)amino]-8-nitroquinolin-4(1H)-one
-
-
3-acetyl-6-chloro-2-[(2-chloro-4-methylphenyl)amino]-8-nitroquinolin-4(1H)-one
-
-
3-acetyl-6-chloro-8-(trifluoromethyl)-2-[[4-(trifluoromethyl)phenyl]amino]quinolin-4(1H)-one
-
-
3-acetyl-7,8-dichloro-2-[[3-(trifluoromethyl)phenyl]amino]quinolin-4(1H)-one
-
-
3-acetyl-8-bromo-5-chloro-2-[(4-chlorophenyl)amino]quinolin-4(1H)-one
-
-
3-acetyl-8-chloro-2-[(2,4-dibromophenyl)amino]-5-methylquinolin-4(1H)-one
-
-
3-acetyl-8-chloro-2-[(2-fluoro-5-methylphenyl)amino]-5-(trifluoromethyl)quinolin-4(1H)-one
-
-
3-acetyl-8-chloro-2-[(3-methylphenyl)amino]-5-nitroquinolin-4(1H)-one
-
-
3-acetyl-8-chloro-2-[(4-chloro-2-fluorophenyl)amino]-5-methylquinolin-4(1H)-one
-
-
3-acetyl-8-chloro-2-[(4-chlorophenyl)amino]-6-nitroquinolin-4(1H)-one
-
-
3-acetyl-8-chloro-5-fluoro-2-(phenylamino)quinolin-4(1H)-one
-
-
3-acetyl-8-chloro-5-methyl-2-[(2,3,4-trifluorophenyl)amino]quinolin-4(1H)-one
-
-
3-acetyl-8-chloro-5-methyl-2-[(2,4,5-trifluorophenyl)amino]quinolin-4(1H)-one
-
-
4-(4-bromophenyl)-3-([N-[5-(1,2-dithiolan-3-yl)pentanoyl]-L-leucyl]amino)-2-oxobutanoic acid
-
reversible inhibitor
4-fluorophenyl (2-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]ethyl)amidosulfite
-
IC50: 29 nM
4-fluorophenyl (3-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]propyl)amidosulfite
-
IC50: 50 nM
4-nitrophenyl (2-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]ethyl)amidosulfite
-
IC50: 47 nM
4-nitrophenyl (3-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]propyl)amidosulfite
-
IC50: 50 nM
4-[([(2Z)-2-[(3S)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetyl]oxy)methyl]benzyl (2Z)-[(3R)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]ethanoate
-
-
5-azanylidyne-N-[[(2S,3S)-3-(ethoxycarbonyl)oxiran-2-yl]carbonyl]-L-norvalyl-L-arginyl-L-tryptophanamide
-
irreversible inhibitor
5-formyl-N-[(2S)-3-methyl-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxobutan-2-yl]-1H-pyrrole-2-carboxamide
-
CAT0059
5-formyl-N-[(2S)-3-methyl-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxobutan-2-yl]furan-2-carboxamide
-
-
5-formyl-N-[(2S)-3-methyl-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxobutan-2-yl]thiophene-2-carboxamide
-
-
A23187
-
-
acetyl-calpastatin peptide
-
50 microM
-
acetyl-DPMSSTYIEE-betaAla-GKREVTIPPKYRELLA-NH2
-
-
acetyl-DPMSSTYIEELGK-NH2
-
-
acetyl-DPMSSTYIEELGKREVT-betaAla-PPKYRELLA-NH2
-
-
acetyl-DPMSSTYIEELGKREVTIPPKYR-NH2
-
-
acetyl-DPMSSTYIEELGKREVTIPPKYREL-NH2
-
-
acetyl-DPMSSTYIEELGKREVTIPPKYRELLA-NH2
-
CP1B peptide
acetyl-Leu-Leu-Met-CHO
-
-
acetyl-Leu-Leu-Nle-CHO
acetyl-REVTIPPKYRELLA-NH2
-
-
acetyl-RRMKWKKDPMSSTYIEELGKREVTIPPKYRELLA-NH2
-
-
acetyl-RYKPPITVERKGLEEIYTSS-NH2
-
-
acetyl-SSTTYIEELGKREVTIPPKYR-NH2
-
-
acetyl-SSTYIEELGK-NH-(CH2O)2-CH2C(O)-TIPPKYR-NH2
-
-
acetyl-SSTYIEELGKREVTIPPK-NH2
-
-
acetyl-SSTYIEELGKREVTIPPKYR-NH2
-
-
acetyl-SSTYIEELGKREVTIPPKYRELLA-NH2
-
-
acetyl-TYIEELGKREVTIPPKYR-NH2
-
-
acetyl-TYIEELGKREVTIPPKYRELLA-NH2
-
-
AK-275
-
reversible inhibitor
-
AK-295
AK-295-D1
-
reversible inhibitor
-
AK-295-D2
-
reversible inhibitor
-
Al3+
-
inactivates enzyme from smooth muscle at millimolar concentrations of Ca2+, calpain 1 and 2
ALLM
-
reversible inhibitor
antipain
-
0.01 mM, 80-90% inhibition
benzyl (2Z)-[(3S)-3-sec-butyl-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetate
-
-
benzyl [(6S,9S,12S)-6-formyl-9-(2-methylpropyl)-8,11-dioxo-2-oxa-7,10-diazabicyclo[12.2.2]octadeca-1(16),14,17-trien-12-yl]carbamate
-
-
benzyl [(7S,10S,13S)-7-formyl-10-(2-methylpropyl)-9,12-dioxo-2-oxa-8,11-diazabicyclo[13.2.2]nonadeca-1(17),15,18-trien-13-yl]carbamate
-
CAT811
benzyl [(8S,11S,14S)-8-formyl-11-(2-methylpropyl)-10,13-dioxo-2-oxa-9,12-diazabicyclo[14.2.2]icosa-1(18),16,19-trien-14-yl]carbamate
-
-
butyl (2Z)-[(3S)-3-(butan-2-yl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]ethanoate
-
-
Calmidazolium
-
-
calpain inhibitor 1
-
synthetic calpain inhibitor
calpain inhibitor III
calpain inhibitor peptide III
-
-
calpain inhibitor VI
-
-
calpain inhibitor-1
calpain inhibitor-III
calpain VI inhibitor
calpastatin
calpastatin 1
-
calpain 1 is under constant inhibiting effect of active calpastatin 1
-
calpastatin peptides
-
-
-
Calpeptin
carbobenzoxy-valinyl-phenylalaninal
-
-
CP1B peptide
-
a 20-mer peptide truncated from region B of calpastatin inhibitory domain 1, 1000fold more selective for mu-calpain than cathepsin L
-
Cystatin
-
engineered cystatins. Recombinant hybrids of human stefin B with KS2 and DELTAL110 deletion mutants of chicken cystatin-KD2 hybrids. Substitution of the N-terminal contact region of stefin B by ther corresponding KD2 sequence results in a calpain inhibitor with a Ki-value of 188 nM. Deletion of L110 improves inhibition 4 to 8fold. All engineered cystatins are temporary inhibitors
-
dimethyl (2S,2'S)-2,2'-[biphenyl-2,2'-diylbis(carbonylimino)]bis(3-phenylpropanoate)
-
-
DPMSSTYIEELGKREVTIPPKYRELLA
-
2 hot spots are detected in which the residues critical for inhibitory function are clustered: Leu11-Gly12 and Thr17-Ile18-Pro19
E-64d
-
irreversible inhibitor
E64d
-
-
EGTA
-
-
Ep-460
-
irreversible inhibitor
ethyl 3-([N-[(benzyloxy)carbonyl]-L-leucyl]amino)-2-oxo-4-phenylbutanoate
-
reversible inhibitor
ethyl 4-(4-bromophenyl)-3-([N-[5-(1,2-dithiolan-3-yl)pentanoyl]-L-leucyl]amino)-2-oxobutanoate
-
reversible inhibitor
heat shock protein 90
-
incubation of calpain-1 at a molar ratio of 1:1 with heat shock protein 90, at increasing Ca2+ concentrations, results in a significant decrease of calpain proteolytic activity at [Ca2+] up to 0.04 mM. At higher Ca2+ concentrations, the inhibiting effect of heat shock protein 90 is no more detectable
-
inhibitor protein Ci1
-
non-specific inhibitor
-
iodoacetic acid
-
0.25 mM, complete
ionomycin
-
-
lactacystin
-
1 microM
Leupeptin
MDL-28170
MDL-28710
-
complete inhibition at 100 nM
MDL28170
methyl (2-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]ethyl)amidosulfite
-
IC50: 89 nM
methyl (2Z)-[(3S)-3-sec-butyl-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetate
-
-
methyl (3S)-4-cyclohexyl-3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxobutanoate
-
IC50: 1000 nM
methyl (S,S,Z)-(3-sec-butyl-1-oxo-2,3-dihydro-1H-isoquinolin-4-ylidene)acetate
-
strong inhibitor
methyl N-[(2Z)-2-[(3S)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetyl]-L-isoleucyl-L-isoleucinate
-
-
methyl N-[(2Z)-2-[(3S)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetyl]-L-isoleucyl-L-isoleucyl-L-isoleucinate
-
-
methyl N-[(2Z)-2-[(3S)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetyl]-L-leucyl-L-phenylalaninate
-
-
methyl N-[(2Z)-2-[(3S)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetyl]-L-valyl-L-phenylalaninate
-
-
methyl N-[[2'-([(2S)-1-[(2'-aminobiphenyl-2-yl)amino]-1-oxo-3-phenylpropan-2-yl]carbamoyl)biphenyl-2-yl]carbonyl]-L-phenylalanyl-L-valinate
-
-
MG115
-
inhibitory effect in micromolar concentrations, 1 mircoM
N'-((1S,2R)-1-benzyl-3-[(3,5-dimethoxybenzyl)amino]-2-hydroxypropyl)-N,N-dipropylbenzene-1,3-dicarboxamide
-
IC50: 20 nM
N-((1S)-1-benzyl-2,3-dioxo-3-[(2-phenylethyl)amino]propyl)-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
IC50: 63 nM
N-((1S)-1-benzyl-3-[(1-methylethyl)amino]-2,3-dioxopropyl)-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
IC50: 205 nM
N-((1S)-1-benzyl-3-[(2-methoxyethyl)amino]-2,3-dioxopropyl)-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
IC50: 200 nM
N-((1S)-1-benzyl-3-[(cyclopropylmethyl)amino]-2,3-dioxopropyl)-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
IC50: 286 nM
N-((1S)-1-[(butylamino)(oxo)acetyl]-3-methylbutyl)-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
-
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-1-(1-benzothiophen-2-ylcarbonyl)piperidine-4-carboxamide
-
reversible inhibitor
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-2-[(E)-2-[4-[(diethylamino)methyl]phenyl]ethenyl]benzamide
-
reversible inhibitor
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-3-methyl-4-oxo-1,4-dihydroquinoline-2-carboxamide
-
reversible inhibitor
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-3-methyl-4-oxo-4H-chromene-2-carboxamide
-
reversible inhibitor
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-4-methyl-6-methylidene-1,6-dihydropyridine-3-carboxamide
-
reversible inhibitor
N-acetyl-L-Leu-L-Leu-L-Met
-
-
N-acetyl-L-leucyl-L-leucyl-L-norleucinal
-
broad-spectrum calpain inhibitor
N-acetyl-Leu-Leu-Nle-CHO
-
complete inhibition at 0.5 mM
N-acetyl-Leu-Leu-Norleu-al
-
-
N-acetyl-Leu-Leu-norleucinal
-
2-fold increase in Tat levels after pre-treating with ALLN, 10 microM
N-benzyloxycarbonyl-L-leucyl-L-leucyl-L-tyrosyl fluoromethylketone
-
broad-spectrum calpain inhibitor
N-[(1S)-1-benzyl-2,3-dioxo-3-(pentylamino)propyl]-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
IC50: 150 nM
N-[(1S)-1-benzyl-2,3-dioxo-3-(prop-2-en-1-ylamino)propyl]-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
IC50: 200 nM
N-[(1S)-1-benzyl-2-oxoethyl]-N2-[(benzyloxy)carbonyl]-L-leucinamide
-
-
N-[(1S)-1-benzyl-3-(benzylamino)-2,3-dioxopropyl]-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
IC50: 81 nM
N-[(1S)-1-benzyl-3-(butylamino)-2,3-dioxopropyl]-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
-
N-[(1S)-1-benzyl-3-(ethylamino)-2,3-dioxopropyl]-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
IC50: 340 nM
N-[(2S)-1-oxo-3-phenylpropan-2-yl]-7,8-dihydro-2H-[1,4]dioxino[2,3-g][1,2,4]benzothiadiazine-3-carboxamide 1,1-dioxide
-
-
N-[(2S)-1-[[(3S)-2-hydroxytetrahydrofuran-3-yl]amino]-1-oxopentan-2-yl]-10H-phenothiazine-2-carboxamide
-
BN-82204
N-[(2S)-3,4-dioxo-1-phenyl-4-([3-[(phenylsulfonyl)amino]propyl]amino)butan-2-yl]-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
reversible inhibitor
N-[(2S)-4-(2-benzylhydrazinyl)-3,4-dioxo-1-phenylbutan-2-yl]-N2-[(benzyloxy)carbonyl]-L-leucinamide
-
reversible inhibitor
N-[(2S)-4-(butylamino)-3,4-dioxo-1-phenylbutan-2-yl]-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
-
reversible inhibitor
N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2S)-4-fluoro-1-(4-hydroxyphenyl)-3-oxobutan-2-yl]-L-leucinamide
-
irreversible inhibitor
N-[1-(4-bromophenyl)-4-(ethylamino)-3,4-dioxobutan-2-yl]-N2-[5-(1,2-dithiolan-3-yl)pentanoyl]-L-leucinamide
-
reversible inhibitor
N-[[(1R)-1-phenyl-2-(4-propoxyphenyl)ethoxy]carbonyl]glycyl-N-[(2S)-1-hydroxypentan-2-yl]-L-leucinamide
-
-
N-[[(1R)-1-phenyl-2-(4-propoxyphenyl)ethoxy]carbonyl]glycyl-N-[(2S)-1-oxopentan-2-yl]-L-leucinamide
-
potent inhibitor with more than 2.5fold selectivity for ovine calpain 1 over ovine calpain 2
N-[[(2R,3R)-3-(ethoxycarbonyl)oxiran-2-yl]carbonyl]-L-histidyl-L-arginyl-L-tryptophanamide
-
irreversible inhibitor
N2-[(2S)-2-([[(2R,3R)-3-(ethoxycarbonyl)oxiran-2-yl]carbonyl]amino)pent-4-enoyl]-L-arginyl-L-tryptophanamide
-
irreversible inhibitor
N2-[(benzyloxy)carbonyl]-N-[4-(ethylamino)-3,4-dioxo-1-phenylbutan-2-yl]-L-leucinamide
-
reversible inhibitor
NaCl
-
mu-calpain is more active at 165 mM NaCl than at 295 mM NaCl
PCP1B peptide
-
-
-
PD-150606
-
-
PD-151746
-
-
PD150606
penetratin
-
-
penicillide
-
-
pepstatin A
-
1 mM, 60-80% inhibition
phenyl (2-[(3-([(1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]ethyl)amidosulfite
-
IC50: 76 nM
phenyl (2-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]ethyl)amidosulfite
-
IC50: 40 nM
phenyl (3-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]propyl)amidosulfite
-
IC50: 35 nM
ritonavir
-
also inhibits calcium-stimulated calpain activity in PC12 cells in situ. Ritonavir or analogues of the drug should by investigated as cytoprotective agents in conditions where cell death or injury is mediated via calpain activation
SJA-6017
-
reversible inhibitor
SNJ-1715
-
reversible inhibitor
SNJ-1945
SNJ1715
-
-
TLCK
-
0.1 mM, 60-80% inhibition
Z-Val-Phe-CHO
-
i.e. MDL-28710, 1.0 microM
ZLLY-CH2F
-
irreversible inhibitor
additional information
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
2-mercaptoethanol
-
required for maximal activity
angiotensin II
-
1.2-fold increased activity of calpain-1, influence in expression of calpain-1
Ca2+
-
required for activation of mu-calpain. Membrane-binding of mu-calpain is Ca2+-dependent. Membrane binding of mu-calpain is due to the exposed hydrophobic surface of the active site conformation and does not reduce the Ca2+ requirement for activation
endotoxin
-
treatment with 12 mg/kg endotoxin increases diaphragm calpain activity and active calpain I protein
-
NS5A protein
-
the nonstructural hepatitis C virus protein NS5Ais sufficient to activate a calpain 1
-
additional information
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.043
2-aminobenzoyl-EVYGMMY(3-NO2)-OH
-
pH and temperature not specified in the publication
0.00074
4,4-difluoro-5,7-dimethyl-4-bora-31,4a-diaza-s-indacene-3-propioyl-labeled casein
-
pH and temperature not specified in the publication
-
0.053
casein
-
pH and temperature not specified in the publication
0.0131
fluorescin thiocarbamoyl-labeled casein
-
pH and temperature not specified in the publication
-
0.00005
fodrin
-
pH and temperature not specified in the publication
-
0.0046
K-(5(6)-carboxyfluorescein)-EVYGMMK(4-(4-dimethylaminophenylazo)benzoyl)-OH
-
pH and temperature not specified in the publication
0.37
N-benzyloxycarbonyl-L-Leu-L-Arg-4-methoxy-2-naphthylamide
-
pH and temperature not specified in the publication
0.19
N-benzyloxycarbonyl-L-Leu-L-Arg-7-amido-4-methylcoumarin
-
pH and temperature not specified in the publication
0.46
N-benzyloxycarbonyl-L-Leu-L-Arg-7-amido-4-trifluoromethylcoumarin
-
pH and temperature not specified in the publication
0.002
succinyl-bovine serum albumin
-
pH and temperature not specified in the publication
-
2
succinyl-bovine-serum albumin
-
pH 7.5, 25C
-
0.0081
succinyl-casein
0.284 - 283.5
succinyl-insulin B
0.2
succinyl-L-Leu-L-Leu-L-Val-7-amido-4-methylcoumarin
1.2
succinyl-L-Leu-L-Met-7-amido-4-methylcoumarin
-
pH and temperature not specified in the publication
0.43
succinyl-L-Leu-L-Tyr-4-methoxy-2-naphthylamide
-
pH and temperature not specified in the publication
4.7
succinyl-L-Leu-L-Tyr-7-amido-4-methylcoumarin
-
pH and temperature not specified in the publication
0.063 - 63
succinyl-protamine
5.9
tert-butyloxycarbonyl-L-Val-L-Leu-L-Lys-7-amido-4-methylcoumarin
-
pH and temperature not specified in the publication
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.025
2-aminobenzoyl-EVYGMMY(3-NO2)-OH
Homo sapiens
-
pH and temperature not specified in the publication
0.11
K-(5(6)-carboxyfluorescein)-EVYGMMK(4-(4-dimethylaminophenylazo)benzoyl)-OH
Homo sapiens
-
pH and temperature not specified in the publication
0.52
N-benzyloxycarbonyl-L-Leu-L-Arg-4-methoxy-2-naphthylamide
Homo sapiens
-
pH and temperature not specified in the publication
0.02
N-benzyloxycarbonyl-L-Leu-L-Arg-7-amido-4-methylcoumarin
Homo sapiens
-
pH and temperature not specified in the publication
0.07
N-benzyloxycarbonyl-L-Leu-L-Arg-7-amido-4-trifluoromethylcoumarin
Homo sapiens
-
pH and temperature not specified in the publication
0.29
succinyl-L-Leu-L-Leu-L-Val-7-amido-4-methylcoumarin
Homo sapiens
-
pH and temperature not specified in the publication
0.029
succinyl-L-Leu-L-Leu-L-Val-L-Tyr-7-amido-4-methylcoumarin
Homo sapiens
-
pH and temperature not specified in the publication
0.062
succinyl-L-Leu-L-Met-7-amido-4-methylcoumarin
Homo sapiens
-
pH and temperature not specified in the publication
0.12
succinyl-L-Leu-L-Tyr-4-methoxy-2-naphthylamide
Homo sapiens
-
pH and temperature not specified in the publication
0.37
succinyl-L-Leu-L-Tyr-7-amido-4-methylcoumarin
Homo sapiens
-
pH and temperature not specified in the publication
0.49
tert-butyloxycarbonyl-L-Val-L-Leu-L-Lys-7-amido-4-methylcoumarin
Homo sapiens
-
pH and temperature not specified in the publication
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000081
1-[(4-methylphenyl)sulfonyl]-N-(1-oxo-3-phenylpropan-2-yl)-D-prolinamide
-
pH and temperature not specified in the publication
0.0000085
3-([N-[(benzyloxy)carbonyl]-L-leucyl]amino)-2-oxo-4-phenylbutanoic acid
-
pH and temperature not specified in the publication
0.00005
4-(4-bromophenyl)-3-([N-[5-(1,2-dithiolan-3-yl)pentanoyl]-L-leucyl]amino)-2-oxobutanoic acid
-
pH and temperature not specified in the publication
0.017
acetyl-DPMSSTYIEE-betaAla-GKREVTIPPKYRELLA-NH2
-
pH and temperature not specified in the publication
0.0069
acetyl-DPMSSTYIEELGK-NH2
-
pH 7.5, 12C
0.0024
acetyl-DPMSSTYIEELGKREVT-betaAla-PPKYRELLA-NH2
-
pH and temperature not specified in the publication
0.0000008
acetyl-DPMSSTYIEELGKREVTIPPKYR-NH2
-
pH 7.5, 12C
0.0000005
acetyl-DPMSSTYIEELGKREVTIPPKYREL-NH2
-
pH 7.5, 12C
0.0000002
acetyl-DPMSSTYIEELGKREVTIPPKYRELLA-NH2
-
pH and temperature not specified in the publication
0.035
acetyl-REVTIPPKYRELLA-NH2
-
pH 7.5, 12C
0.00000019
acetyl-RRMKWKKDPMSSTYIEELGKREVTIPPKYRELLA-NH2
-
pH and temperature not specified in the publication
0.726
acetyl-RYKPPITVERKGLEEIYTSS-NH2
-
pH 7.5, 12C
0.000026
acetyl-SSTTYIEELGKREVTIPPKYR-NH2
-
pH and temperature not specified in the publication
0.0117
acetyl-SSTYIEELGK-NH-(CH2O)2-CH2C(O)-TIPPKYR-NH2
-
pH 7.5, 12C
0.017
acetyl-SSTYIEELGKREVTIPPK-NH2
-
pH 7.5, 12C
0.000026
acetyl-SSTYIEELGKREVTIPPKYR-NH2
-
pH 7.5, 12C
0.0000006
acetyl-SSTYIEELGKREVTIPPKYRELLA-NH2
-
pH 7.5, 12C
0.000093
acetyl-TYIEELGKREVTIPPKYR-NH2
0.0000022
acetyl-TYIEELGKREVTIPPKYRELLA-NH2
-
pH 7.5, 12C
0.000026
CP1B peptide
-
pH and temperature not specified in the publication
-
0.0018
ethyl 3-([N-[(benzyloxy)carbonyl]-L-leucyl]amino)-2-oxo-4-phenylbutanoate
-
pH and temperature not specified in the publication
0.01
ethyl 4-(4-bromophenyl)-3-([N-[5-(1,2-dithiolan-3-yl)pentanoyl]-L-leucyl]amino)-2-oxobutanoate
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.000009
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-1-(1-benzothiophen-2-ylcarbonyl)piperidine-4-carboxamide
-
pH and temperature not specified in the publication
0.000027
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-2-[(E)-2-[4-[(diethylamino)methyl]phenyl]ethenyl]benzamide
-
pH and temperature not specified in the publication
0.0000047
N-[(2S)-4-(2-benzylhydrazinyl)-3,4-dioxo-1-phenylbutan-2-yl]-N2-[(benzyloxy)carbonyl]-L-leucinamide
-
pH and temperature not specified in the publication
0.00002
N-[1-(4-bromophenyl)-4-(ethylamino)-3,4-dioxobutan-2-yl]-N2-[5-(1,2-dithiolan-3-yl)pentanoyl]-L-leucinamide
-
pH and temperature not specified in the publication
0.0002
N2-[(benzyloxy)carbonyl]-N-[4-(ethylamino)-3,4-dioxo-1-phenylbutan-2-yl]-L-leucinamide
-
pH and temperature not specified in the publication
0.0000005
PCP1B peptide
-
pH and temperature not specified in the publication
-
0.00000018
penetratin
-
pH and temperature not specified in the publication
0.0059
ritonavir
-
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00088
(2S)-2-[[(4-fluorophenyl)sulfonyl]amino]-N-[(3S)-2-hydroxytetrahydrofuran-3-yl]-3-methylbutanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0007
(2S,5S)-5-benzyl-6-hydroxy-2-(2-methylpropyl)morpholin-3-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000038
(3S)-2-hydroxytetrahydrofuran-3-yl N-[(10H-phenothiazin-2-yloxy)acetyl]-L-threonyl-L-leucinate
Homo sapiens
-
pH and temperature not specified in the publication
0.000089
(3S)-2-hydroxytetrahydrofuran-3-yl N-[(2S)-2-[[(10H-phenothiazin-2-yloxy)acetyl]amino]butanoyl]-L-leucinate
Homo sapiens
-
pH and temperature not specified in the publication
0.001
(3S)-3-[[N-(10H-phenothiazin-2-ylcarbonyl)-L-norvalyl]amino]tetrahydrofuran-2-yl acetate
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.013
(6S,9S,16R)-6-(hydroxymethyl)-9-(2-methylpropyl)-16-phenyl-2,15-dioxa-7,10,13-triazabicyclo[16.2.2]docosa-1(20),18,21-triene-8,11,14-trione
Ovis aries
-
pH and temperature not specified in the publication
0.0004
(6S,9S,16R)-9-(2-methylpropyl)-8,11,14-trioxo-16-phenyl-2,15-dioxa-7,10,13-triazabicyclo[16.2.2]docosa-1(20),18,21-triene-6-carbaldehyde
Ovis aries
-
pH and temperature not specified in the publication
0.029
(7S,10S,13S,26S)-13,26-dibenzyl-7-methyl-10-(propan-2-yl)-5,7,8,10,11,13,14,25,26,28-decahydrotetrabenzo[k,m,t,v][1,4,7,10,15,18]hexaazacyclotetracosine-6,9,12,15,24,27-hexone
Homo sapiens
-
pH and temperature not specified in the publication
0.00022
(7S,10S,17R)-10-(2-methylpropyl)-9,12,15-trioxo-17-phenyl-2,16-dioxa-8,11,14-triazabicyclo[17.2.2]tricosa-1(21),19,22-triene-7-carbaldehyde
Ovis aries
-
pH and temperature not specified in the publication
0.00175
(7S,10S,17R)-7-(hydroxymethyl)-10-(2-methylpropyl)-17-phenyl-2,16-dioxa-8,11,14-triazabicyclo[17.2.2]tricosa-1(21),19,22-triene-9,12,15-trione
Ovis aries
-
pH and temperature not specified in the publication
0.00017
(8S,11S,18R)-11-(2-methylpropyl)-10,13,16-trioxo-18-phenyl-2,17-dioxa-9,12,15-triazabicyclo[18.2.2]tetracosa-1(22),20,23-triene-8-carbaldehyde
Ovis aries
-
pH and temperature not specified in the publication
0.00134
(8S,11S,18R)-8-(hydroxymethyl)-11-(2-methylpropyl)-18-phenyl-2,17-dioxa-9,12,15-triazabicyclo[18.2.2]tetracosa-1(22),20,23-triene-10,13,16-trione
Ovis aries
-
pH and temperature not specified in the publication
0.00315
(9R,12S,19R)-12-(2-methylpropyl)-11,14,17-trioxo-19-phenyl-2,18-dioxa-7-thia-10,13,16-triazabicyclo[19.2.2]pentacosa-1(23),21,24-triene-9-carbaldehyde
Ovis aries
-
pH and temperature not specified in the publication
0.05
(9R,12S,19R)-9-(hydroxymethyl)-12-(2-methylpropyl)-19-phenyl-2,18-dioxa-7-thia-10,13,16-triazabicyclo[19.2.2]pentacosa-1(23),21,24-triene-11,14,17-trione
Ovis aries
-
pH and temperature not specified in the publication
59
([(2Z)-2-[(3S)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetyl]oxy)ethynyl (2Z)-[(3R)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]ethanoate
Sus scrofa
-
-
0.0005
1-(2-chloro-4-hydroxyphenyl)-4-oxo-7-(pyridin-4-yl)-1,4-dihydroquinoline-3-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000006
2-methyl-N-[(2S)-1-oxo-3-phenylpropan-2-yl]-7,8-dihydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
Homo sapiens
-
pH and temperature not specified in the publication
0.000056
3,4-dichlorophenyl (2-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]ethyl)amidosulfite
0.00034
3-([4-[2-(methoxymethoxy)phenyl]-4-oxobutanoyl]amino)-2-oxo-4-phenylbutanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0192
3-acetyl-2-[(2,4-dichlorophenyl)amino]-8-(trifluoromethyl)quinolin-4(1H)-one
Homo sapiens
-
using [2-Abz]-Ser-Thr-Phe-Ala-Gln-Pro-[3-nitrotyrosine]-NH2 as substrate, in 50 mM Tris-HCl, 50 mM NaCl, 1 mM EDTA, 5 mM beta-mercaptoethanol, pH 7.5, at 25C
0.03
3-acetyl-2-[(3-fluorophenyl)amino]-8-phenylquinolin-4(1H)-one
0.00369 - 0.00743
3-acetyl-2-[(4-tert-butylphenyl)amino]-8-chloro-6-nitroquinolin-4(1H)-one
0.03
3-acetyl-2-[[3,5-bis(trifluoromethyl)phenyl]amino]-5,8-difluoroquinolin-4(1H)-one
Homo sapiens
-
IC50 above 0.03 mM, using [2-Abz]-Ser-Thr-Phe-Ala-Gln-Pro-[3-nitrotyrosine]-NH2 as substrate, in 50 mM Tris-HCl, 50 mM NaCl, 1 mM EDTA, 5 mM beta-mercaptoethanol, pH 7.5, at 25C
0.00169 - 0.00359
3-acetyl-5,8-dibromo-2-[(4-bromophenyl)amino]quinolin-4(1H)-one
0.00317 - 0.00399
3-acetyl-5,8-dichloro-2-[(2,4-dichlorophenyl)amino]quinolin-4(1H)-one
0.03
3-acetyl-6,8-difluoro-2-[(2,4,5-trifluorophenyl)amino]quinolin-4(1H)-one
Homo sapiens
-
IC50 above 0.03 mM, using [2-Abz]-Ser-Thr-Phe-Ala-Gln-Pro-[3-nitrotyrosine]-NH2 as substrate, in 50 mM Tris-HCl, 50 mM NaCl, 1 mM EDTA, 5 mM beta-mercaptoethanol, pH 7.5, at 25C
0.00316 - 0.00464
3-acetyl-6-chloro-2-[(2,4-dichlorophenyl)amino]-8-nitroquinolin-4(1H)-one
0.00239 - 0.00373
3-acetyl-6-chloro-2-[(2-chloro-4-methylphenyl)amino]-8-nitroquinolin-4(1H)-one
0.03
3-acetyl-6-chloro-8-(trifluoromethyl)-2-[[4-(trifluoromethyl)phenyl]amino]quinolin-4(1H)-one
0.00353 - 0.00994
3-acetyl-8-bromo-5-chloro-2-[(4-chlorophenyl)amino]quinolin-4(1H)-one
0.000277 - 0.00306
3-acetyl-8-chloro-2-[(2,4-dibromophenyl)amino]-5-methylquinolin-4(1H)-one
0.03
3-acetyl-8-chloro-2-[(2-fluoro-5-methylphenyl)amino]-5-(trifluoromethyl)quinolin-4(1H)-one
0.00456 - 0.00808
3-acetyl-8-chloro-2-[(4-chlorophenyl)amino]-6-nitroquinolin-4(1H)-one
0.03
3-acetyl-8-chloro-5-fluoro-2-(phenylamino)quinolin-4(1H)-one
0.000029
4-fluorophenyl (2-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]ethyl)amidosulfite
Homo sapiens
-
IC50: 29 nM
0.00005
4-fluorophenyl (3-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]propyl)amidosulfite
Homo sapiens
-
IC50: 50 nM
0.000047
4-nitrophenyl (2-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]ethyl)amidosulfite
Homo sapiens
-
IC50: 47 nM
0.00005
4-nitrophenyl (3-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]propyl)amidosulfite
Homo sapiens
-
IC50: 50 nM
5
4-[([(2Z)-2-[(3S)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetyl]oxy)methyl]benzyl (2Z)-[(3R)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]ethanoate
Homo sapiens
-
-
0.00033
5-azanylidyne-N-[[(2S,3S)-3-(ethoxycarbonyl)oxiran-2-yl]carbonyl]-L-norvalyl-L-arginyl-L-tryptophanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00029
5-formyl-N-[(2S)-3-methyl-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxobutan-2-yl]-1H-pyrrole-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00096
5-formyl-N-[(2S)-3-methyl-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxobutan-2-yl]furan-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00044
5-formyl-N-[(2S)-3-methyl-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxobutan-2-yl]thiophene-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00019
acetyl-Leu-Leu-Nle-CHO
Rattus norvegicus
-
pH and temperature not specified in the publication
85
benzyl (2Z)-[(3S)-3-sec-butyl-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetate
Sus scrofa
-
-
0.0004
benzyl [(6S,9S,12S)-6-formyl-9-(2-methylpropyl)-8,11-dioxo-2-oxa-7,10-diazabicyclo[12.2.2]octadeca-1(16),14,17-trien-12-yl]carbamate
Homo sapiens
-
pH and temperature not specified in the publication
0.00022
benzyl [(7S,10S,13S)-7-formyl-10-(2-methylpropyl)-9,12-dioxo-2-oxa-8,11-diazabicyclo[13.2.2]nonadeca-1(17),15,18-trien-13-yl]carbamate
Homo sapiens
-
pH and temperature not specified in the publication
0.00017
benzyl [(8S,11S,14S)-8-formyl-11-(2-methylpropyl)-10,13-dioxo-2-oxa-9,12-diazabicyclo[14.2.2]icosa-1(18),16,19-trien-14-yl]carbamate
Homo sapiens
-
pH and temperature not specified in the publication
0.000008
calpain inhibitor III
Rattus norvegicus
-
pH and temperature not specified in the publication
0.0000075
calpain inhibitor VI
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000052
Calpeptin
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000064
dimethyl (2S,2'S)-2,2'-[biphenyl-2,2'-diylbis(carbonylimino)]bis(3-phenylpropanoate)
Homo sapiens
-
pH and temperature not specified in the publication
0.0015
E-64
Homo sapiens
-
-
0.000199 - 0.0002
MDL28170
0.000089
methyl (2-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]ethyl)amidosulfite
Homo sapiens
-
IC50: 89 nM
0.000025
methyl (2Z)-[(3S)-3-sec-butyl-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetate
Sus scrofa
-
-
0.001
methyl (3S)-4-cyclohexyl-3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxobutanoate
Homo sapiens
-
IC50: 1000 nM
0.000025
methyl (S,S,Z)-(3-sec-butyl-1-oxo-2,3-dihydro-1H-isoquinolin-4-ylidene)acetate
Homo sapiens
-
pH and temperature not specified in the publication
0.000447
methyl N-[(2Z)-2-[(3S)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetyl]-L-isoleucyl-L-isoleucinate
Sus scrofa
-
-
0.000159
methyl N-[(2Z)-2-[(3S)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetyl]-L-isoleucyl-L-isoleucyl-L-isoleucinate
Sus scrofa
-
-
0.000066
methyl N-[(2Z)-2-[(3S)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetyl]-L-leucyl-L-phenylalaninate
Sus scrofa
-
-
0.000626
methyl N-[(2Z)-2-[(3S)-3-(1-methylpropyl)-1-oxo-2,3-dihydroisoquinolin-4(1H)-ylidene]acetyl]-L-valyl-L-phenylalaninate
Sus scrofa
-
-
0.000000087
methyl N-[[2'-([(2S)-1-[(2'-aminobiphenyl-2-yl)amino]-1-oxo-3-phenylpropan-2-yl]carbamoyl)biphenyl-2-yl]carbonyl]-L-phenylalanyl-L-valinate
Homo sapiens
-
pH and temperature not specified in the publication
0.00002
N'-((1S,2R)-1-benzyl-3-[(3,5-dimethoxybenzyl)amino]-2-hydroxypropyl)-N,N-dipropylbenzene-1,3-dicarboxamide
Homo sapiens
-
IC50: 20 nM
0.000063
N-((1S)-1-benzyl-2,3-dioxo-3-[(2-phenylethyl)amino]propyl)-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
Homo sapiens
-
IC50: 63 nM
0.000205
N-((1S)-1-benzyl-3-[(1-methylethyl)amino]-2,3-dioxopropyl)-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
Homo sapiens
-
IC50: 205 nM
0.0002
N-((1S)-1-benzyl-3-[(2-methoxyethyl)amino]-2,3-dioxopropyl)-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
Homo sapiens
-
IC50: 200 nM
0.000286
N-((1S)-1-benzyl-3-[(cyclopropylmethyl)amino]-2,3-dioxopropyl)-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
Homo sapiens
-
IC50: 286 nM
0.00071
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-3-methyl-4-oxo-1,4-dihydroquinoline-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00004
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-3-methyl-4-oxo-4H-chromene-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0028
N-(4-amino-3,4-dioxo-1-phenylbutan-2-yl)-4-methyl-6-methylidene-1,6-dihydropyridine-3-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00015
N-[(1S)-1-benzyl-2,3-dioxo-3-(pentylamino)propyl]-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
Homo sapiens
-
IC50: 150 nM
0.0002
N-[(1S)-1-benzyl-2,3-dioxo-3-(prop-2-en-1-ylamino)propyl]-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
Homo sapiens
-
IC50: 200 nM
0.00024
N-[(1S)-1-benzyl-2-oxoethyl]-N2-[(benzyloxy)carbonyl]-L-leucinamide
Sus scrofa
-
-
0.000081
N-[(1S)-1-benzyl-3-(benzylamino)-2,3-dioxopropyl]-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
Homo sapiens
-
IC50: 81 nM
0.00034
N-[(1S)-1-benzyl-3-(ethylamino)-2,3-dioxopropyl]-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
Homo sapiens
-
IC50: 340 nM
0.000028
N-[(2S)-1-oxo-3-phenylpropan-2-yl]-7,8-dihydro-2H-[1,4]dioxino[2,3-g][1,2,4]benzothiadiazine-3-carboxamide 1,1-dioxide
Homo sapiens
-
pH and temperature not specified in the publication
0.000023
N-[(2S)-1-[[(3S)-2-hydroxytetrahydrofuran-3-yl]amino]-1-oxopentan-2-yl]-10H-phenothiazine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000035
N-[(2S)-3,4-dioxo-1-phenyl-4-([3-[(phenylsulfonyl)amino]propyl]amino)butan-2-yl]-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
Homo sapiens
-
pH and temperature not specified in the publication
0.00005
N-[(2S)-4-(butylamino)-3,4-dioxo-1-phenylbutan-2-yl]-2-ethyl-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazine-3-carboxamide 1,1-dioxide
Homo sapiens
-
pH and temperature not specified in the publication
0.0032
N-[[(1R)-1-phenyl-2-(4-propoxyphenyl)ethoxy]carbonyl]glycyl-N-[(2S)-1-hydroxypentan-2-yl]-L-leucinamide
Ovis aries
-
pH and temperature not specified in the publication
0.00005
N-[[(1R)-1-phenyl-2-(4-propoxyphenyl)ethoxy]carbonyl]glycyl-N-[(2S)-1-oxopentan-2-yl]-L-leucinamide
Ovis aries
-
pH and temperature not specified in the publication
0.00078
N2-[(2S)-2-([[(2R,3R)-3-(ethoxycarbonyl)oxiran-2-yl]carbonyl]amino)pent-4-enoyl]-L-arginyl-L-tryptophanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000076
phenyl (2-[(3-([(1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]ethyl)amidosulfite
Homo sapiens
-
IC50: 76 nM
0.00004
phenyl (2-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]ethyl)amidosulfite
Homo sapiens
-
IC50: 40 nM
0.000035
phenyl (3-[(3-([(2-ethyl-1,1-dioxido-3,4,7,8-tetrahydro-2H-[1,4]dioxino[2,3-g][1,2]benzothiazin-3-yl)carbonyl]amino)-2-oxo-4-phenylbutanoyl)amino]propyl)amidosulfite
Homo sapiens
-
IC50: 35 nM
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6.5 - 8
-
pH 6.5: about 35% of maximal activity, pH 8.0: about 50% of maximal activity
6.5
-
m-calpain
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
37
-
assay at 37C, 20 min, with or without magnetic bead stimulation
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
activation of mu-calpain in platelets from patients with type 2 diabetes mellitus
Manually annotated by BRENDA team
-
; area 1
Manually annotated by BRENDA team
-
from patients with recurrent miscarriage and healthy women with informed consent
Manually annotated by BRENDA team
-
low level
Manually annotated by BRENDA team
-
postmortem muscle
Manually annotated by BRENDA team
-
loss of activity during postmortem aging
Manually annotated by BRENDA team
-
loss of activity during postmortem aging
Manually annotated by BRENDA team
-
rheumatic synovial cell line. mu-calpain, regulates MMP-3 release by rheumatic synovial cells, in addition to exerting its own degradative action on cartilage
Manually annotated by BRENDA team
-
first molar of foetal ICR mice from embryonic day 14 to postnatal day 7
Manually annotated by BRENDA team
-
progenitor HCN-A94-2
Manually annotated by BRENDA team
-
NO-induced motility in osteoclasts requires regulated Ca2+ release, which activates mu-calpain. This occurs via the inositol (1,4,5)-trisphosphate receptor 1
Manually annotated by BRENDA team
-
originated from kidney
Manually annotated by BRENDA team
-
elevated levels of calpain-1 in glaucomatous trabecular meshwork. However, calpain activity in glaucomatous trabecular meshwork is only about 50% of that in controls. Modification by iso-levuglandins renders calpain-1 inactive
Manually annotated by BRENDA team
-
loss of activity during postmortem aging
Manually annotated by BRENDA team
-
neuroblastoma
Manually annotated by BRENDA team
additional information