Information on EC 2.7.11.13 - protein kinase C and Organism(s) Homo sapiens

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The enzyme appears in selected viruses and cellular organisms

EC NUMBER
COMMENTARY hide
2.7.11.13
-
RECOMMENDED NAME
GeneOntology No.
protein kinase C
SYSTEMATIC NAME
IUBMB Comments
ATP:protein phosphotransferase (diacylglycerol-dependent)
A family of serine- and threonine-specific protein kinases that depend on lipids for activity. They can be activated by calcium but have a requirement for the second messenger diacylglycerol. Members of this group of enzymes phosphorylate a wide variety of protein targets and are known to be involved in diverse cell-signalling pathways. Members of the protein kinase C family also serve as major receptors for phorbol esters, a class of tumour promoters.
CAS REGISTRY NUMBER
COMMENTARY hide
141436-78-4
calcium-dependent protein kinase C
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
metabolism
-
overexpression of the enzyme isoforms: PKCalpha, PKCbeta, and PKCtheta, but not PKCgamma, stimulates protein kinase CK2 activity
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
alphatomega peptide + ATP
ADP + phosphorylated-alphatomega peptide
show the reaction diagram
-
an improved PKCalpha-responsive polyion complex (PIC) to measure PKCalpha activity is reported. The polycation molecule is the poly(amidoamine) (PAMAM) dendrimer modified with both cationic PKCalpha-specific peptide substrates (alphatomega, FKKQGSFAKKK-NH2) and near infrared (NIR) fluorophores (Cy5.5), and the polyanion molecule is the quencher (BHQ-3)-modified chondroitin sulfate
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + AAKIQASFRGHMARKK
ADP + AAKIQApSFRGHMARKK
show the reaction diagram
-
-
-
-
?
ATP + ADAM17
ADP + phosphorylated ADAM17
show the reaction diagram
-
-
-
-
?
ATP + ADKRRSVRIGA
ADP + ADKRRpSVRIGA
show the reaction diagram
-
-
-
-
?
ATP + Akt
ADP + phosphorylated Akt
show the reaction diagram
ATP + alpha1D Ca channel
ADP + phosphorylated alpha1D Ca channel
show the reaction diagram
-
-
-
-
?
ATP + ARKRERTYSFGHHA
ADP + ARKRERTYpSFGHHA
show the reaction diagram
-
-
-
-
?
ATP + ASQKRPSQRH
ADP + ASQKRPpSQRH
show the reaction diagram
-
-
-
-
?
ATP + calcium-independent phospholipase A2
ADP + phosphorylated calcium-independent phospholipase A2
show the reaction diagram
ATP + casein kinase 1delta
ADP + phosphorylated casein kinase 1delta
show the reaction diagram
-
phosphorylation at Ser328, Thr329, and Ser370
-
-
?
ATP + CREB1 protein
ADP + phosphorylated CREB1 protein
show the reaction diagram
-
-
-
-
?
ATP + CTP:phosphoethanolamine cytidylyltransferase
ADP + phosphorylated CTP:phosphoethanolamine cytidylyltransferase
show the reaction diagram
-
phosphorylation at Ser215 and Ser223
-
-
?
ATP + diacylglycerol kinase-zeta
ADP + phosphorylated diacylglycerol kinase-zeta
show the reaction diagram
ATP + EF factor 1
ADP + phosphorylated EF factor 1
show the reaction diagram
-
i.e. eukaryotic translation elongation factor 1-alpha1, in vitro phosphorylation
-
-
?
ATP + extracellular signal-regulated kinase 2
ADP + phosphorylated extracellular signal-regulated kinase 2
show the reaction diagram
-
-
-
-
?
ATP + extracellular signal-related kinase
ADP + phosphorylated extracellular signal-related kinase
show the reaction diagram
-
-
-
-
?
ATP + FAFKKSFKLAG
ADP + FAFKKpSFKLAG
show the reaction diagram
-
-
-
-
?
ATP + FKKQGSFAKKK
ADP + phosphorylated FKKQGSFAKKK
show the reaction diagram
-
highly specific substrate for isozyme PKCalpha relative to other isozymes, 60% phosphorylation rate with isozyme PKCalpha, less than 20% phosphorylation rate with other PKC isozymes
-
-
?
ATP + FKLKRKGSFKKFA
ADP + FKLKRKGpSFKKFA
show the reaction diagram
-
-
-
-
?
ATP + Fyn
ADP + phosphorylated Fyn
show the reaction diagram
-
Fyn is a tyrosine protein kinase of the Src family, phosphorylation at a serine residue
-
-
?
ATP + Galpha-interacting, vesicle-associated protein
ADP + phosphorylated-Galpha-interacting, vesicle-associated protein
show the reaction diagram
-
PKCtheta, down-regulates Galpha-interacting, vesicle-associated protein (GIV's) guanine exchange factor, GEF function by phosphorylating Ser-1689 located within GIV's GEF motif. PKCtheta specifically binds and phosphorylates GIV at S1689, and this phosphoevent abolishes GIV's ability to bind and activate trimeric G proteins Galphai
-
-
-
ATP + histone H1
ADP + phosphorylated histone H1
show the reaction diagram
PKD2 activated by phorbol esters efficiently phosphorylate the exogenous substrate histone H1
-
-
?
ATP + histone H2
ADP + phosphorylated histone H2
show the reaction diagram
-
in vitro phosphorylation
-
-
?
ATP + histone H3
ADP + phosphorylated histone H3
show the reaction diagram
-
in vitro phosphorylation
-
-
?
ATP + inhibitory killer cell Ig-like receptor
ADP + phosphorylated inhibitory killer cell Ig-like receptor
show the reaction diagram
ATP + insulin receptor
ADP + phosphorylated insulin receptor
show the reaction diagram
-
isozyme PKCalpha
-
-
?
ATP + insulin receptor substrate-1
ADP + phosphorylated insulin receptor substrate-1
show the reaction diagram
-
-
-
-
?
ATP + IRS
ADP + phosphorylated IRS
show the reaction diagram
-
isozymes PKCalpha and PKCdelta, phosphorylation on Ser307
-
-
?
ATP + IVRKATLRRLL
ADP + IVRKApTLRRLL
show the reaction diagram
-
-
-
-
?
ATP + KFKRPTLRRVR
ADP + KFKRPpTLRRVR
show the reaction diagram
-
-
-
-
?
ATP + KKKRFSFKKAF
ADP + KKKRFpSFKKAF
show the reaction diagram
-
-
-
-
?
ATP + KLAGFSFKKNK
ADP + KLAGFpSFKKNK
show the reaction diagram
-
-
-
-
?
ATP + KPCB protein
ADP + phosphorylated KPCB protein
show the reaction diagram
-
-
-
-
?
ATP + lamin A
ADP + phosphorylated lamin A
show the reaction diagram
-
a nuclear membrane protein, isozyme PKCalpha
-
-
?
ATP + lamin C
ADP + phosphorylated lamin C
show the reaction diagram
-
a nuclear membrane protein, isozyme PKCalpha, phosphorylation at Ser572
-
-
?
ATP + LLRMFSFKAPA
ADP + LLRMFpSFKAPA
show the reaction diagram
-
-
-
-
?
ATP + metabotropic glutamate receptor 5
ADP + phosphorylated metabotropic glutamate receptor 5
show the reaction diagram
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
show the reaction diagram
-
-
-
-
?
ATP + myristoylated alanine-rich C kinase substrate
ADP + phosphorylated myristoylated alanine-rich C kinase substrate
show the reaction diagram
-
a major PKC substrate
-
-
?
ATP + myristoylated alanine-rich C-kinase (152-164)
ADP + phosphorylated myristoylated alanine-rich C-kinase (152-164)
show the reaction diagram
-
-
-
-
?
ATP + NADPH oxidase
ADP + phosphorylated NADPH oxidase
show the reaction diagram
-
-
-
-
?
ATP + NRFARKGSLRQKNV
ADP + NRFARKGpSLRQKNV
show the reaction diagram
-
-
-
-
?
ATP + phosphoinositide-dependent kinase
ADP + phosphorylated phosphoinositide-dependent kinase
show the reaction diagram
ATP + phospholipase D1
ADP + phosphorylated phospholipase D1
show the reaction diagram
-
phosphorylation by PKC
-
-
?
ATP + phospholipase D2
ADP + phosphorylated phospholipase D2
show the reaction diagram
-
phosphorylation by PKCalpha
-
-
?
ATP + PKC-alpha-derived peptide
ADP + phosphorylated PKC-alpha-derived peptide
show the reaction diagram
in the presence of the classical PKC activators phosphatidylserine/diacylglycerol, PKC alpha phosphorylates a PKC-alpha pseudosubstrate-derived peptide, an epidermal-growth-factor-receptor-derived peptide, histone III-S and myelin basic protein to an equal extent, whilst PKC zeta phosphorylates only the PKC-alpha-derived peptide
-
-
?
ATP + protein
ADP + phosphoprotein
show the reaction diagram
ATP + protein kinase CK2alpha
ADP + phosphorylated protein kinase CK2alpha
show the reaction diagram
-
phosphorylation at serines 194 and 277
-
-
?
ATP + protein kinase CK2beta
ADP + phosphorylated protein kinase CK2beta
show the reaction diagram
-
phosphorylation at serine 148
-
-
?
ATP + RFARKGSLRQKNV
ADP + phoshorylated RFARKGSLRQKNV
show the reaction diagram
-
a commercially available peptide substrate
-
-
?
ATP + RFARKGSLRQKNV
ADP + phosphorylated RFARKGSLRQKNV
show the reaction diagram
-
-
-
-
?
ATP + RFARKGSLRQKNV
ADP + RFARKGphosphoSLRQKNV
show the reaction diagram
-
synthetic peptide substrate
-
-
?
ATP + RRFKRQGSFFYFF
ADP + RRFKRQGpSFFYFF
show the reaction diagram
-
-
-
-
?
ATP + RRRRSIIFI
ADP + RRRRpSIIFI
show the reaction diagram
-
-
-
-
?
ATP + RVVGGSLRGAQ
ADP + RVVGGpSLRGAQ
show the reaction diagram
-
-
-
-
?
ATP + transient receptor potential protein V4
ADP + phosphorylated transient receptor potential protein vanilloid 4
show the reaction diagram
-
-
-
-
?
ATP + transient receptor potential protein vanilloid 1
ADP + phosphorylated transient receptor potential protein vanilloid 1
show the reaction diagram
-
-
-
-
?
ATP + vascular endothelial growth factor receptor 2
ADP + phosphorylated vascular endothelial growth factor receptor 2
show the reaction diagram
-
phosphorylation at Ser1188 and Ser 1191
-
-
?
ATP + [low density lipoprotein receptor-related protein]
ADP + phosphorylated [low density lipoprotein receptor-related protein]
show the reaction diagram
N6-phenyl-ATP + RFARKGSLRQKNV
N6-phenyl-ADP + RFARKGphosphoSLRQKNV
show the reaction diagram
-
synthetic peptide substrate, recombinant isozyme PKCalpha mutant M417A
-
-
?
Rab11 + ATP
ADP + phosphorylated Rab11
show the reaction diagram
-
Rab11 is differentially phosphorylated in vitro by several purified PKC isoenzymes. Ser 177 is identified as the single PKC-phosphorylated residue in Rab11
-
-
?
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
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + calcium-independent phospholipase A2
ADP + phosphorylated calcium-independent phospholipase A2
show the reaction diagram
-
PKC regulates membrane-associated, calcium-independent phospholipase A2 in coronary artery endothelial cells in competition to thrombin, overview
-
-
?
ATP + casein kinase 1delta
ADP + phosphorylated casein kinase 1delta
show the reaction diagram
-
phosphorylation at Ser328, Thr329, and Ser370
-
-
?
ATP + CTP:phosphoethanolamine cytidylyltransferase
ADP + phosphorylated CTP:phosphoethanolamine cytidylyltransferase
show the reaction diagram
-
phosphorylation at Ser215 and Ser223
-
-
?
ATP + diacylglycerol kinase-zeta
ADP + phosphorylated diacylglycerol kinase-zeta
show the reaction diagram
-
the enzyme, especially isozyme PKCalpha, inhibits binding of diacylglycerol kinase-zeta to the retinoblastoma protein
-
-
?
ATP + inhibitory killer cell Ig-like receptor
ADP + phosphorylated inhibitory killer cell Ig-like receptor
show the reaction diagram
-
the enzyme regulates expression and function of inhibitory killer cell Ig-like receptors in NK cells, KIR negatively regulate NK cell cytotoxicity by activating Src homology 2 domain-containing protein tyrsine phospatase 1 and 2, overview
-
-
?
ATP + metabotropic glutamate receptor 5
ADP + phosphorylated metabotropic glutamate receptor 5
show the reaction diagram
-
isozyme-specific phosphorylation of metabotropic glutamate receptor 5 by PKCdelta blocks Ca2+ oscillation and oscillatory translocation of Ca2+-dependent PKCgamma
-
-
?
ATP + NADPH oxidase
ADP + phosphorylated NADPH oxidase
show the reaction diagram
-
-
-
-
?
ATP + phosphoinositide-dependent kinase
ADP + phosphorylated phosphoinositide-dependent kinase
show the reaction diagram
-
phosphoinositide-dependent kinases are conserved substrates of PKC
-
-
?
ATP + protein kinase CK2alpha
ADP + phosphorylated protein kinase CK2alpha
show the reaction diagram
-
phosphorylation at serines 194 and 277
-
-
?
ATP + protein kinase CK2beta
ADP + phosphorylated protein kinase CK2beta
show the reaction diagram
-
phosphorylation at serine 148
-
-
?
ATP + [low density lipoprotein receptor-related protein]
ADP + phosphorylated [low density lipoprotein receptor-related protein]
show the reaction diagram
-
involved in regulation of endocytosis and association with adaptor molecules, e.g. Shc, Dab1, or CED-6/GULP
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
N6-phenyl-ATP
-
preferred by PKCalpha mutant M417A to phosphorylate peptide and protein substrates, no activity with the wild-type PKCalpha
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Cd2+
-
cell exposure to 0.020 mM cadmium for 24 h results in PKC activation
Mn2+
-
-
Zn2+
-
PKC contains zinc finger structures that are important for its enzymatic activity
additional information
-
presence of only one cysteine-rich, zinc finger-like domain, absence of an apparent Ca(2+)-binding region
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2R)-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
-
1,1'-(1,10-decanediyl)bis[1-amino isoquinolinium] diiodide
-
-
1,1'-(1,10-decanediyl)bis[2-amino-1-methylbenzimidazolium] diiodide
-
-
1,1'-(1,10-decanediyl)bis[2-methylbenzothiazolium] diiodide
-
-
1,1'-(1,10-decanediyl)bis[2-methylbenzoxazolium] diiodide
-
-
1,1'-(1,10-decanediyl)bis[2-methylquinolinium] diiodide
-
-
1,1'-(1,10-decanediyl)bis[4-amino-2-methyl quinolinium] diiodide
-
-
1,1'-(1,10-decanediyl)bis[4-aminoquinolinium] diiodide
-
-
1,1'-(1,10-decanediyl)bis[4-N,N,dimethylaminoquinolinium] diiodide
-
-
1,1'-(1,10-decanediyl)bis[quinolinium] diiodide
-
-
1,1'-decane-1,10-diylbis(4-aminopyridinium) diiodide
-
-
1,1'-decane-1,10-diylbis[4-(dimethylamino)pyridinium]
-
-
1,6-bis[N-(1-methylquinolinium-2-methyl)amino]-hexane diiodide
-
-
1-(1,4-diazepan-1-yl)-3-(pyridin-4-yl)-2,6-naphthyridine
-
-
1-(piperazin-1-yl)-3-(pyridin-4-yl)-2,6-naphthyridine
-
-
1-methoxypropan-2-yl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 49%
1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]piperidin-3-amine
-
-
2,7,11-triamino-3,6,13-trihydroxy-5-methyl-6,7,8,9,15,16-hexahydro-5H,14H-5,9-epoxy-4b,9a,15-triazadibenzo[b,h]cyclonona[1,2,3,4-jkl]cyclopenta[e]-as-indacen-14-one
-
-
2,7,11-triamino-3,6-dihydroxy-5-methyl-6,7,8,9,15,16-hexahydro-5H,14H-5,9-epoxy-4b,9a,15-triazadibenzo[b,h]cyclonona[1,2,3,4-jkl]cyclopenta[e]-as-indacen-14-one
-
-
2,7-diamino-3,6,13-trihydroxy-5-methyl-6,7,8,9,15,16-hexahydro-5H,14H-5,9-epoxy-4b,9a,15-triazadibenzo[b,h]cyclonona[1,2,3,4-jkl]cyclopenta[e]-as-indacen-14-one
-
-
2,7-diamino-3,6-dihydroxy-5-methyl-6,7,8,9,15,16-hexahydro-5H,14H-5,9-epoxy-4b,9a,15-triazadibenzo[b,h]cyclonona[1,2,3,4-jkl]cyclopenta[e]-as-indacen-14-one
-
-
2-([3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]amino)ethanol
-
-
2-([3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]oxy)ethanamine
-
-
2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carbonitrile
-
0.03 mM, inhibition: 87%
2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylic acid
-
0.03 mM, inhibition: 65%
2-fluorobenzyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 100%
2-methoxyethyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 57%
2-methyl-6-(phenylethynyl)-pyridine
-
complete inhibition of PKCgamma oscillation at 0.05 mM
2-methyl-N1-[3-(3-methylpyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
-
2-methyl-N1-[3-(pyridin-3-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
-
2-methyl-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
-
2-methylbenzyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 64%
3-(1-(3-(dimethylamino)propyl)-2-methyl-1H-indol-3-yl)-4-(2-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
a bisindolylmaleimide analogue of BIM-1 inhibitor
3-cyanobenzyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 70%
3-methoxybenzyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 100%
3-methylbenzyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 67%
3-phenyl-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
-
-
3-[1-[3-(dimethylamino)propyl]-5-methoxy-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
Go6983, PKC-specific inhibitor, complete inhibition at 500 nM
4-amino-1,2-dimethylquinolinium
-
-
4-amino-1-decyl-2-methylquinolinium iodide
-
-
4-cyanobenzyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 10%
4-fluorobenzyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 2%
4-methylbenzyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 50%
4-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]piperazin-2-one
-
-
alsterpaullone
-
7% inhibition of PKCalpha at 0.01 mM
arachidonoyl fluoromethylketone
-
inhibition of PKCgamma oscillation at 0.1 mM
AVGPRPQT
-
-
benzyl 2-amino-4-(1,3-benzodioxol-5-yl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 85%
benzyl 2-amino-4-(2-fluoro-4-methoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 78%
benzyl 2-amino-4-(2-fluorophenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 57%
benzyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 100%
benzyl 2-amino-4-(3-cyanophenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 25%
benzyl 2-amino-4-(3-fluorophenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 53%
benzyl 2-amino-4-(3-methoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 57%
benzyl 2-amino-4-(3-methylphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 68%
benzyl 2-amino-4-(4-methoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 86%
benzyl 2-amino-4-(4-methylphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 60%
benzyl 2-amino-4-[3-(trifluoromethyl)phenyl]thiophene-3-carboxylate
-
0.03 mM, inhibition: 29%
benzyl 2-amino-4-[4-(trifluoromethyl)phenyl]thiophene-3-carboxylate
-
0.03 mM, inhibition: 21%
bisindolylmaleimide
-
strong inhibition of PKCalpha
bisindolylmaleimide derivatives
-
-
bisindolylmaleimide I
-
-
bromoerol lactone
-
slight inhibition of PKCgamma oscillation at 0.1 mM
calphostin C
-
PKC-specific inhibitor
CG53353
-
inhibitor of isozyme PKCbetaII
compound 48/80
-
complete inhibition of PKCgamma oscillation at 0.1 mM
CRLVLASC
-
targets isozyme PKCgamma, blocks formalin-induced pain response
cytochalasine D
-
inhibition of PKCgamma oscillation at 0.01 mM
EAVSLKPT
-
targets isozyme PKCepsilon, reverses psi epsilonRACK-mediated protection, and decreases formalin-induced pain response
enzastaurin
-
oral serine/threonine kinase inhibitor
ethanol
-
0.03%, inhibition of PKCgamma oscillation at 0.1 mM
ethyl 2-(carbamoylamino)-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 14%
ethyl 2-amino-4-(1,3-benzodioxol-5-yl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 100%
ethyl 2-amino-4-(2-fluoro-4-methoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 100%
ethyl 2-amino-4-(2-fluorophenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 62%
ethyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 100%
ethyl 2-amino-4-(3-cyanophenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 32%
ethyl 2-amino-4-(3-fluoro-4-methoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 100%
ethyl 2-amino-4-(3-fluorophenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 38%
ethyl 2-amino-4-(3-methoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 82%
ethyl 2-amino-4-(3-methylphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 77%
ethyl 2-amino-4-(4-aminophenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 100%
ethyl 2-amino-4-(4-methoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 100%
ethyl 2-amino-4-(4-methylphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 80%
ethyl 2-amino-4-[3-(trifluoromethyl)phenyl]thiophene-3-carboxylate
-
0.03 mM, inhibition: 16%; 0.03 mM, inhibition: 30%
ethyl 2-amino-4-[4-(dimethylamino)phenyl]thiophene-3-carboxylate
-
0.03 mM, inhibition: 100%
ethyl 4-(3,4-dimethoxyphenyl)-2-(dimethylamino)thiophene-3-carboxylate
-
0.03 mM, inhibition: 60%
ethyl 4-(3,4-dimethoxyphenyl)-2-(methylamino)thiophene-3-carboxylate
-
0.03 mM, inhibition: 32%
ethyl 4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 3%
FLLDPY
-
-
FNGLLKIKI
-
protects from cardiac ischaemic injury
FTRKRQRAMRRVHQ
-
autoregulatory pseudosubstrate sequence, residues 24-40, lung enzyme
GF 109203X
GF109203X
Go-6983
-
isoform PKCalpha-specific inhibitor
Goe6976
-
-
Goe6983
-
-
G 6976
-
slight inhibition of PKCalpha
G 6983
-
-
G6976
-
-
HDAPIGYD
-
protects from cardiac ischaemic injury, from graft coronary artery disease, and activates potassium current, inhibits sodium current
indirubin-3'-monoxime
-
32% inhibition of PKCalpha at 0.01 mM
K-252a
-
strong inhibition
KGDYEKILVALCGGN
-
targets isozyme PKCbeta
KLFIMNL
-
targets isozyme PKCbetaI, inhibits cardiomyocyte hypertrophy
KQKTKTIK T
-
targets isozyme PKCbeta
LEPEGK
-
-
MDPNGLSDPYVKL
-
targets isozyme PKCbeta, blocks Ca2+ current
MRAAEDPM
-
increased injury from cardiac ischaemia
myr-PKC
-
specific protein kinase C inhibitor
-
N,N,N,N',N',N'-hexaethyldecane-1,10-diaminium
-
-
N-(5'-([(3S,8aS)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-4',5'-dihydro-1'H-spiro[cyclopropane-1,6'-pyrrolo[3,4-c]pyrazol]-3'-yl)pyridine-2-carboxamide
-
-
N-(5-([(2S)-2-benzyl-4-methylpiperazin-1-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-3-phenoxybenzamide
-
-
N-(5-([(2S)-2-benzyl-4-methylpiperazin-1-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)benzamide
-
-
N-(5-([(3S,7S,8aS)-7-fluoro-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
-
N-(5-([(3S,8aS)-3-ethylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
-
N-(5-([(3S,8aS)-7,7-difluoro-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
-
N-(5-([(8aS)-3,3-dimethylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
-
N-(6,6-dimethyl-5-([(3R,8aR)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
0.001 mM, 13% inhibition
N-(6,6-dimethyl-5-([(3R,8aS)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
0.001 mM, 24% inhibition
N-(6,6-dimethyl-5-([(3S,8aR)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
-
N-(6,6-dimethyl-5-([(3S,8aS)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
-
N-(6,6-dimethyl-5-[(4-methylpiperazin-1-yl)carbonyl]-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)benzamide
-
-
N-(6-ethyl-6-methyl-5-([(3S,8aS)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
-
N-cyclohexa-1,3-dien-1-yl-N,N,N',N',N'-pentaphenyldecane-1,10-diaminium
-
-
N-methyl-N'-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
-
-
N-methyl-N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
-
-
N-[2-(pyridin-4-yl)pyrido[3,4-d]pyrimidin-4-yl]ethane-1,2-diamine
-
-
N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
-
-
N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,3-diamine
-
-
N-[3-(pyridin-4-yl)-2,7-naphthyridin-1-yl]ethane-1,2-diamine
-
-
N-[3-(pyridin-4-yl)isoquinolin-1-yl]ethane-1,2-diamine
-
-
N-[5-(hexahydropyrrolo[1,2-a]pyrazin-2(1H)-ylcarbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl]benzamide
-
-
N-[7-(pyridin-4-yl)-1,6-naphthyridin-5-yl]ethane-1,2-diamine
-
-
N-[7-(pyridin-4-yl)isoquinolin-5-yl]ethane-1,2-diamine
-
-
N1-(3-[2-(propan-2-ylamino)pyridin-4-yl]-2,6-naphthyridin-1-yl)-2-methylpropane-1,2-diamine
-
-
N1-[3-(2-aminopyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
-
-
N1-[3-(3-chloropyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
-
-
N1-[3-(3-fluoropyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
-
-
NGRKI
-
-
PAWHD
-
-
phenyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 48%
propan-2-yl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 100%
propidiumiodide
-
-
PYIALNVD
-
-
pyridin-4-ylmethyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 53%
QEVIRNN
-
targets isozyme PKCbetaII, inhibits cardiomyocyte hypertrophy and activates potassium channels
RACK1 peptide I homologue
-
-
-
Ro-31-7549
-
specific inhibitor for isozyme PKCalpha
Ro-31-8220
-
strong inhibition of PKCalpha
Ro-31-8425
-
-
rottlerin
safranine O
-
-
SFNSYELGSL
-
targets isozyme PKCdelta, protects from cardiac ischaemic injury, from cerebral injury, from graft coronary artery disease, and increases fibroblast proliferation
SIKIWD
-
targets isozyme PKCbeta
SIYRRGARRWRKLYRAN
-
targets isozyme PKCzeta, which leads to inhibition of fibroblast proliferation
SLNPEWNE
-
targets isozyme PKCbeta
SRIGQ
-
-
staurosporine
thapsigargin
-
complete inhibition of PKCgamma oscillation at 0.005 mM
Tween 80
-
inhibits the enzyme at high concentration
[2-amino-4-(3,4-dimethoxyphenyl)thiophen-3-yl][(benzylamino)oxy]methanone
-
0.03 mM, inhibition: 43%
[2-amino-4-(3,4-dimethoxyphenyl)thiophen-3-yl][(ethylamino)oxy]methanone
-
0.03 mM, inhibition: 50%
[2-amino-4-(3,4-dimethoxyphenyl)thiophen-3-yl]{[(2-methoxyethyl)amino]oxy}methanone
-
0.03 mM, inhibition: 55%
[2-amino-4-(3,4-dimethoxyphenyl)thiophen-3-yl]{[(pyridin-4-ylmethyl)amino]oxy}methanone
-
0.03 mM, inhibition: 3%
{3-[5-amino-4-(ethoxycarbonyl)thiophen-3-yl]phenyl}carbamate
-
0.03 mM, inhibition: 89%
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1,2-diacyl-sn-glycerol
-
-
1,2-dioleoyl-sn-glycerol
-
activates
12-O-Tetradecanoylphorbol 13-acetate
12-O-tetradecanoylphorbol-13-acetate
-
-
4beta-phorbol 12-myristate 13-acetate
arachidonic acid
-
alone or a combination of gamma-linolenic acid and phosphatidylserine slightly enhances PKC zeta activity; slightly enhances PKC zeta activity
CSF-1
-
CSF-1 increases PKCgamma Thr 410 phosphorylation and kinase activity in 32D.R cells
-
diacylglycerol
fatty acids
-
activation mechanism
gamma-linolenic acid
-
a combination of gamma-linolenic acid and phosphatidylserine slightly enhances PKC zeta activity
gastrin
-
physiological activator of PKD2 in human AGS-B cells stably transfected with the CCK(B)/gastrin receptor
hypericin
-
competes with 12-O-tetradecanoylphorbol 13-acetate for binding to the regulatory domain of PKC, localization of PKC isozymes alpha, delta, and gamma, high affinty binding and interaction witht he C1B domain of PKC, molecular modeling
Insulin
-
activates PKC isozymes alpha, betaII, delta, and zeta in several cell types, activation mechanism
-
ionomycin
-
-
kenpaullone
-
20% activation of PKCalpha at 0.01 mM
phorbol 12,13-dibutyrate
-
-
phorbol 12-myristate 13-acetate
Phorbol esters
-
bind to and stimulate the kinase activity of PKC-L
phorbol-ester-12-13-dibutyrate
-
-
phosphatidylserine
Phospholipids
-
regulatory function for isozymes alpha, betaI, betaII, gamma, delta, epsilon, eta, and theta
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0093 - 0.0828
ATP
0.0166 - 0.0599
FKKQGSFAKKK
0.0124
N6-phenyl-ATP
-
pH 7.4, 37C, recombinant isozyme PKCalpha mutant M417A
additional information
additional information
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000338
N-(5'-([(3S,8aS)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-4',5'-dihydro-1'H-spiro[cyclopropane-1,6'-pyrrolo[3,4-c]pyrazol]-3'-yl)pyridine-2-carboxamide
-
pH and temperature not specified in the publication
0.000541
N-(5-([(2S)-2-benzyl-4-methylpiperazin-1-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-3-phenoxybenzamide
-
pH and temperature not specified in the publication
0.000189
N-(5-([(2S)-2-benzyl-4-methylpiperazin-1-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)benzamide
-
pH and temperature not specified in the publication
0.000109
N-(5-([(3S,7S,8aS)-7-fluoro-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
pH and temperature not specified in the publication
0.000046
N-(5-([(3S,8aS)-3-ethylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
pH and temperature not specified in the publication
0.01
N-(5-([(3S,8aS)-7,7-difluoro-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
pH and temperature not specified in the publication
0.000125
N-(5-([(8aS)-3,3-dimethylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
pH and temperature not specified in the publication
0.000092
N-(6,6-dimethyl-5-([(3S,8aR)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
pH and temperature not specified in the publication
0.000029
N-(6,6-dimethyl-5-([(3S,8aS)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
pH and temperature not specified in the publication
0.000541
N-(6,6-dimethyl-5-[(4-methylpiperazin-1-yl)carbonyl]-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)benzamide
-
pH and temperature not specified in the publication
0.000062
N-(6-ethyl-6-methyl-5-([(3S,8aS)-3-methylhexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]carbonyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)pyridine-2-carboxamide
-
pH and temperature not specified in the publication
0.000131
N-[5-(hexahydropyrrolo[1,2-a]pyrazin-2(1H)-ylcarbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl]benzamide
-
pH and temperature not specified in the publication
additional information
additional information
-
Ki values of the pseudosubstrates in nano- to micromolar range
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000002 - 0.000829
(2R)-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
0.03
1,1'-(1,10-decanediyl)bis[1-amino isoquinolinium] diiodide
Homo sapiens
-
pH 7.4
0.014
1,1'-(1,10-decanediyl)bis[2-amino-1-methylbenzimidazolium] diiodide
Homo sapiens
-
pH 7.4
0.017
1,1'-(1,10-decanediyl)bis[2-methylbenzothiazolium] diiodide
Homo sapiens
-
pH 7.4
0.036
1,1'-(1,10-decanediyl)bis[2-methylbenzoxazolium] diiodide
Homo sapiens
-
pH 7.4
0.022
1,1'-(1,10-decanediyl)bis[2-methylquinolinium] diiodide
Homo sapiens
-
pH 7.4
0.007
1,1'-(1,10-decanediyl)bis[4-amino-2-methyl quinolinium] diiodide
Homo sapiens
-
pH 7.4
0.03
1,1'-(1,10-decanediyl)bis[4-aminoquinolinium] diiodide
Homo sapiens
-
pH 7.4
0.029
1,1'-(1,10-decanediyl)bis[4-N,N,dimethylaminoquinolinium] diiodide
Homo sapiens
-
pH 7.4
0.072
1,1'-(1,10-decanediyl)bis[quinolinium] diiodide
Homo sapiens
-
pH 7.4
0.112
1,1'-decane-1,10-diylbis(4-aminopyridinium) diiodide
Homo sapiens
-
pH 7.4
0.231
1,1'-decane-1,10-diylbis[4-(dimethylamino)pyridinium]
Homo sapiens
-
pH 7.4
0.03
1,6-bis[N-(1-methylquinolinium-2-methyl)amino]-hexane diiodide
Homo sapiens
-
pH 7.4
0.000004 - 0.000661
1-(1,4-diazepan-1-yl)-3-(pyridin-4-yl)-2,6-naphthyridine
0.000006 - 0.001
1-(piperazin-1-yl)-3-(pyridin-4-yl)-2,6-naphthyridine
0.000008 - 0.000865
1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]piperidin-3-amine
0.000081 - 0.001
2-([3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]amino)ethanol
0.000082 - 0.001
2-([3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]oxy)ethanamine
0.000052 - 0.001
2-methyl-N1-[3-(3-methylpyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
0.001
2-methyl-N1-[3-(pyridin-3-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
Homo sapiens
-
value higher than, pH and temperature not specified in the publication
0.000009 - 0.000967
2-methyl-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
0.005
3-methoxybenzyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.000403 - 0.001
3-phenyl-N1-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,2-diamine
3.59
4-amino-1,2-dimethylquinolinium
Homo sapiens
-
pH 7.4
0.117
4-amino-1-decyl-2-methylquinolinium iodide
Homo sapiens
-
pH 7.4
0.000735 - 0.001
4-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]piperazin-2-one
0.006
benzyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.0075
bisindolylmaleimide I
Homo sapiens
-
pH not specified in the publication, 30C
0.002
ethyl 2-amino-4-(1,3-benzodioxol-5-yl)thiophene-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.004
ethyl 2-amino-4-(2-fluoro-4-methoxyphenyl)thiophene-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.001
ethyl 2-amino-4-(4-aminophenyl)thiophene-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.002
ethyl 2-amino-4-(4-methoxyphenyl)thiophene-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.0025
G 6983
Homo sapiens
-
pH not specified in the publication, 30C
0.25
N,N,N,N',N',N'-hexaethyldecane-1,10-diaminium
Homo sapiens
-
pH 7.4
0.094
N-cyclohexa-1,3-dien-1-yl-N,N,N',N',N'-pentaphenyldecane-1,10-diaminium
Homo sapiens
-
pH 7.4
0.000079 - 0.001
N-methyl-N'-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
0.000024 - 0.001
N-methyl-N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
0.000027 - 0.001
N-[2-(pyridin-4-yl)pyrido[3,4-d]pyrimidin-4-yl]ethane-1,2-diamine
0.000005 - 0.0009
N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]ethane-1,2-diamine
0.00001 - 0.000779
N-[3-(pyridin-4-yl)-2,6-naphthyridin-1-yl]propane-1,3-diamine
0.001
N-[3-(pyridin-4-yl)-2,7-naphthyridin-1-yl]ethane-1,2-diamine
Homo sapiens
-
value higher than, pH and temperature not specified in the publication
0.000743 - 0.001
N-[3-(pyridin-4-yl)isoquinolin-1-yl]ethane-1,2-diamine
0.000401 - 0.001
N-[7-(pyridin-4-yl)-1,6-naphthyridin-5-yl]ethane-1,2-diamine
0.000044 - 0.001
N-[7-(pyridin-4-yl)isoquinolin-5-yl]ethane-1,2-diamine
0.000862 - 0.001
N1-(3-[2-(propan-2-ylamino)pyridin-4-yl]-2,6-naphthyridin-1-yl)-2-methylpropane-1,2-diamine
0.00006 - 0.001
N1-[3-(2-aminopyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
0.000015 - 0.001
N1-[3-(3-chloropyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
0.000018 - 0.001
N1-[3-(3-fluoropyridin-4-yl)-2,6-naphthyridin-1-yl]-2-methylpropane-1,2-diamine
0.006
propan-2-yl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.016
propidiumiodide
Homo sapiens
-
pH 7.4
0.000008
Ro-31-8425
Homo sapiens
-
pH 7.3, 25C
0.048
safranine O
Homo sapiens
-
pH 7.4
0.00023
staurosporine
Homo sapiens
-
pH and temperature not specified in the publication
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.2
-
assay at
7.3
-
assay at
7.4
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
21
-
assay at room temperature
22
-
assay at room temperature
25
-
assay at
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
AGS-B cell
Manually annotated by BRENDA team
-
shows higher levels of PKCalpha than normal breast tissue
Manually annotated by BRENDA team
-
high expression of isozyme PKCalpha in most cell lines, overview
Manually annotated by BRENDA team
-
isozyme PKCgamma
Manually annotated by BRENDA team
-
recombinant PKCalpha
Manually annotated by BRENDA team
-
from normal sigmoid colon
Manually annotated by BRENDA team
-
Burkitt lymphoma cell line
Manually annotated by BRENDA team
-
follicular lymphoma cell line
Manually annotated by BRENDA team
-
follicular lymphoma cell line
Manually annotated by BRENDA team
-
diffuse large B-cell lymphoma cell line
Manually annotated by BRENDA team
-
Burkitt lymphoma cell line
Manually annotated by BRENDA team
-
myeloma cell line
Manually annotated by BRENDA team
-
diffuse large B-cell lymphoma cell line
Manually annotated by BRENDA team
-
precursor T-lymphoblastic leukemia cell line
Manually annotated by BRENDA team
-
Burkitt lymphoma cell line
Manually annotated by BRENDA team
-
Burkitt lymphoma cell line
Manually annotated by BRENDA team
-
diffuse large B-cell lymphoma cell line
Manually annotated by BRENDA team
-
Burkitt lymphoma cell line
Manually annotated by BRENDA team
-
Burkitt lymphoma cell line
Manually annotated by BRENDA team
-
Burkitt lymphoma cell line
Manually annotated by BRENDA team
-
shows higher levels of PKCalpha than normal liver tissue
Manually annotated by BRENDA team
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Burkitt lymphoma cell line
Manually annotated by BRENDA team
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myeloid progenitor cell line 32D.R
Manually annotated by BRENDA team
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isozyme PKCbetaII
Manually annotated by BRENDA team
-
Burkitt lymphoma cell line
Manually annotated by BRENDA team
-
isozyme PKCalpha
Manually annotated by BRENDA team
-
fibroblast cell line
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
activated PKCbetaII and PKCbetaI are translocated from cytosol, juxtanuclear location, isozyme-specific translocation of PKCbetaII and not PKCbetaI to a juxtanuclear subset of recycling endosomes, involvement of phospholipase D
Manually annotated by BRENDA team
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localization of PKC isozymes alpha, delta, and gamma, is influenced by hypericin, high affinity binding and interaction with the C1B domain of PKC, molecular modeling
Manually annotated by BRENDA team
additional information
PDB
SCOP
CATH
ORGANISM
UNIPROT
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
65000
-
x * 65000
103925
-
x * 103925, calculation from nucleotide sequence
105000
-
x * 105000, SDS-PAGE
120000
-
x * 120000, SDS-PAGE
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
-
PKC domain composition
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phosphoprotein
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phorbol 12,13-dibutyrate in the presence of dioleoylphosphatidylserine stimulates the autophosphorylation of PKD2 in a synergistic fashion. Phorbol esters also stimulate autophosphorylation of PKD2 in intact cells, C-terminal Ser876 is an in vivo phosphorylation site within PKD2 that is correlated with the activation status of the kinase
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
purified recombinant isozyme PKCbetaII catalytic domain, residues 321-673, hanging drop vapour diffusion method, 8 mg/ml protein in 0.1 M acetamidoiminodiacetic acid, pH 6.5, and 1.7-2.3 M sodium acetate, 19C, X-ray diffraction structure determination and analysis at 3.2 A resolution, molecular replacement, modeling
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Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
partial; partial purification of the PKC-zeta isoenzyme
-
recombinant full-length enzyme by nickel affinity chromatography, proteolytic clevage of the recombinant full-length enzyme to obtain the catalytic domain, followed by anion exchange chromatography and gel filtration
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Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
co-expression of PKC isozymes and insulin in HEK-293 or CHO cells, interaction analysis, overview
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expressed in HEK-293 cells and human-derived rhabdhomyosarcoma cells; expressed in HEK-293 cells and human-derived rhabdhomyosarcoma cells; expressed in HEK-293 cells and human-derived rhabdhomyosarcoma cells; expressed in HEK-293 cells and human-derived rhabdhomyosarcoma cells
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expressed in HeLa cells
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expression in COS cells
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expression in COS1 cells; expression in COS1 cells
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expression in COS7 cells
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expression in recombinant baculovirus-infected insect cells; expression in recombinant baculovirus-infected insect cells, overexpression in NIH 3T3 cells or insect cells
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expression in the baculovirus insect-cell expression system
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expression of FLAG-tagged wild-type and mutant isozyme PLCalpha in MCF-10A human breast epithelial cells
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expression of full-length His-tagged isoform PKCbetaII in Spodoptera frugiperda Sf21 cells
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expression of GFP-tagged PKC
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expression of GFP-tagged wild-type PKC isozymes in HEK-293 cells, and of GFP-tagged PKCgamma wild-type and mutants lacking the C1 or C2 domain in HEK-293 cells
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expression of wild-type and mutant isoyzem PKCalpha in COS-7 cells, co-expression of PKCalpha with diacylglycerol kinase-zeta and retinoblastoma protein in COS-7 cells
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isolation of cDNA
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isozymes PKCbetaII and PKCbetaI are products of alternative splicing of gene PKCbeta, expression of GFP- or HA-tagged isozymes PKCbetaII, wild-type and mutant, and PKCbetaI in HEK-293 or HeLa cells
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protein kinase C-epsilon E1 and E2, expression in Sf9 cells, the recombinant protein displays protein kinase C activity and phorbol ester binding activity
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the 5' segment of the gene for protein kinase C beta is cloned from a human leukocyte genomic library in EMBL3 bacteriophage
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EXPRESSION
ORGANISM
UNIPROT
LITERATURE
knockdown of diacylglycerol kinase delta enhances PKCalpha activity
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prolonged PKC activation by phorbol esters is downregulates PKC for at least 24 h
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
K368D
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site-directed mutagenesis of isozyme PKCalpha ATP-binding site, a dominant-negative mutant
K371R
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site-directed mutagenesis, inactive isozyme PKCbetaII mutant
M417A
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site-directed mutagenesis, utilizes the alternate cofactor N6-phenyl-ATP
additional information
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine
-
a phase II trial of enzastaurin is conducted to determine the 6-month progression-free survival rate in advanced non-small-cell lung cancer using Enzaustaurin: 13% of the patients have a progression-free survival for more than 6 months
molecular biology
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a technique is developed to detect PKCalpha activity in a cancerous cell lysate through the simple measurement of fluorescence intensity. The principle of this methodology is based on a fluorescence increase associated with polyion complex dissociation due to phosphorylation by PKCalpha