Information on EC 2.7.11.13 - protein kinase C

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The expected taxonomic range for this enzyme is: Eukaryota

EC NUMBER
COMMENTARY hide
2.7.11.13
-
RECOMMENDED NAME
GeneOntology No.
protein kinase C
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + a protein = ADP + a phosphoprotein
show the reaction diagram
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
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
female and male, several isozymes
-
-
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
isozyme PKCbeta; WB strain, ATCC 30957, isozymes beta, delta, epsilon, theta and zeta
SwissProt
Manually annotated by BRENDA team
catfish, female
-
-
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
Mus musculus C57BL/6
C57BL/6 mice
-
-
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
metabolism
-
PKC activity controls serine racemase phosphorylation and D-serine levels both in vitro and in vivo
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
-
-
?
Arg-Phe-Ala-Arg-Lys-Gly-Ser-Leu-Arg-Gln-Lys-Asn-Val + ATP
Arg-Phe-Ala-Arg-Lys-Gly-phosphoSer-Leu-Arg-Gln-Lys-Asn-Val + ADP
show the reaction diagram
-
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + ADAM17
ADP + phosphorylated ADAM17
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 + Bcl-xL
ADP + phosphorylated Bcl-xL
show the reaction diagram
ATP + Btk
ADP + phosphorylated Btk
show the reaction diagram
ATP + calcium-activated potassium channel alpha subunit Slo1
ADP + phosphorylated calcium-activated potassium channel alpha subunit Slo1
show the reaction diagram
-
-
-
-
?
ATP + calcium-independent phospholipase A2
ADP + phosphorylated calcium-independent phospholipase A2
show the reaction diagram
ATP + calmodulin
ADP + phosphorylated calmodulin
show the reaction diagram
-
phosphorylation at Thr497 in the calmodulin-binding domain, binding is competitive to substrate endothelial nitric oxide synthase
-
-
?
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 + endothelial nitric oxide synthase
ADP + phosphorylated endothelial nitric oxide synthase
show the reaction diagram
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 + 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 + 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 + GluR6 kainate receptor subunit
ADP + phosphorylated GluR6 kainate receptor subunit
show the reaction diagram
-
two specific residues on the GluR6 C terminus, Ser846 and Ser868, are phosphorylated by protein kinase C, PKC phosphorylation of GluR6 retains GluR6 in the endoplasmic reticulum
-
-
?
ATP + glycine transporter 2
ADP + phosphorylated glycine transporter 2
show the reaction diagram
-
-
-
-
?
ATP + hematopoietic-specific G-protein Galpha15
ADP + phosphorylated hematopoietic-specific G-protein Galpha15
show the reaction diagram
-
recombinant substrate expressed in COS-7 cells, phosphorylation at Ser334, mutant G-protein Galpha15 S334A is inactive as substrate for PKC
-
-
?
ATP + hematopoietic-specific G-protein Galpha15 peptide
ADP + phosphorylated hematopoietic-specific G-protein Galpha15 peptide
show the reaction diagram
-
the PKC phosphorylation site peptide sequence RKGSR includes Ser334
-
-
?
ATP + hematopoietic-specific G-protein Galpha16
ADP + phosphorylated hematopoietic-specific G-protein Galpha16
show the reaction diagram
-
substrate from HL-60 cells, phosphorylation at Ser336, mutant G-protein Galpha16 S336A is inactive as substrate for PKC
-
-
?
ATP + hematopoietic-specific G-protein Galpha16 peptide
ADP + phosphorylated hematopoietic-specific G-protein Galpha16 peptide
show the reaction diagram
-
the PKC phosphorylation site peptide sequence KKGARSRR includes Ser336
-
-
?
ATP + histone
ADP + phosphorylated histone
show the reaction diagram
ATP + histone H1
ADP + phosphorylated histone H1
show the reaction diagram
ATP + histone H1-IIIS
ADP + phosphorylated histone H1-IIIS
show the reaction diagram
isozyme PKCbeta
-
-
?
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 + histone III-SS
ADP + phosphorylated histone III-SS
show the reaction diagram
-
commercial substrate
-
-
?
ATP + histone IIIS
ADP + phosphorylated histone IIIS
show the reaction diagram
poor substrate
-
-
?
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
ATP + insulin receptor substrate 1
ADP + phosphorylated insulin receptor substrate 1
show the reaction diagram
ATP + insulin receptor substrate-1
ADP + phosphorylated insulin receptor substrate-1
show the reaction diagram
ATP + insulin receptor substrate-3
ADP + phosphorylated insulin receptor substrate-3
show the reaction diagram
-
-
-
-
?
ATP + insulin receptor substrate-4
ADP + phosphorylated insulin receptor substrate-4
show the reaction diagram
-
-
-
-
?
ATP + IRS
ADP + phosphorylated IRS
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 + LC3
ADP + phosphorylated LC3
show the reaction diagram
-
-
-
-
?
ATP + metabotropic glutamate receptor 5
ADP + phosphorylated metabotropic glutamate receptor 5
show the reaction diagram
ATP + mutant protein p22phox(P156Q)
ADP + phosphorylated mutant protein p22phox(P156Q)
show the reaction diagram
-
-
-
-
?
ATP + mutant protein p22phox(T132A)
ADP + phosphorylated mutant protein p22phox(T132A)
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
ATP + Na,K-ATPase
ADP + phosphorylated Na,K-ATPase
show the reaction diagram
ATP + NADPH oxidase
ADP + phosphorylated NADPH oxidase
show the reaction diagram
ATP + Par-3
ADP + phosphorylated Par-3
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 + poly(ADP-ribose) polymerase-1
ADP + phosphorylated poly(ADP-ribose) polymerase-1
show the reaction diagram
-
-
-
-
?
ATP + protein
ADP + phosphoprotein
show the reaction diagram
ATP + protein p22phox
ADP + phosphorylated protein p22phox
show the reaction diagram
-
threonine 147 of protein p22phox is phosphorylated by PKC-alpha and PKC-delta isoforms in vitro
-
-
?
ATP + RalB
ADP + phosphorylated RalB
show the reaction diagram
-
PKCalpha phosphorylates RalB on Ser-192 and Ser-198 in the hypervariable sequence and Ser-198 phosphorylation promotes activation of RalB and causes RalB relocalization from the plasma membrane to late endosomes
-
-
?
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 + ribosomal protein S6-(229-239) peptide analogue
ADP + phosphorylated ribosomal protein S6-(229-239) peptide analogue
show the reaction diagram
-
-
-
-
?
ATP + serine racemase
ADP + phosphorylated serine racemase
show the reaction diagram
-
-
-
-
?
ATP + serotonin N-acetyltransferase
ADP + phosphorylated serotonin N-acetyltransferase
show the reaction diagram
ATP + sodium channel
ADP + phosphorylated sodium channel
show the reaction diagram
ATP + store-operated channel
ADP + phosphorylated store-operated channel
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 + transient receptor potential vanilloid 5
ADP + phosphorylated transient receptor potential vanilloid 5
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 + vasodilator-stimulated phosphoprotein
ADP + phosphorylated vasodilator-stimulated phosphoprotein
show the reaction diagram
-
phosphorylation at Ser157
-
-
?
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 + Akt
ADP + phosphorylated Akt
show the reaction diagram
-
phosphorylation by PKC isozymes at Ser473, regulation of the phosphorylation activity by PKCbetaII in mast cells stimulated by stem cell factor or interaleukin-3, and in serum-stimulated fibroblasts, and in antigen-receptor stimulated T- or B-lymphocytes, overview
-
-
?
ATP + Btk
ADP + phosphorylated Btk
show the reaction diagram
-
specific phosphorylation leads to inhibition of Btk membrane translocation and activation and the downstream events that promote PKCbeta activation, mechanism, overview
-
-
?
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 + 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 + endothelial nitric oxide synthase
ADP + phosphorylated endothelial nitric oxide synthase
show the reaction diagram
-
the enzyme is responsible for the negative regulation of endothelial nitric oxide synthase, a key enzyme in nitric oxide-mediated signal transduction, phosphorylation reduces the affinity of nitric oxide synthase for calmodulin
-
-
?
ATP + histone H1-IIIS
ADP + phosphorylated histone H1-IIIS
show the reaction diagram
Q1H8W8
isozyme PKCbeta
-
-
?
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 + insulin receptor substrate 1
ADP + phosphorylated insulin receptor substrate 1
show the reaction diagram
-
phosphorylation of insulin receptor substrate proteins on serine residues is an important posttranslational modification that is linked to insulin resistance, 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 + myristoylated alanine-rich C kinase substrate
ADP + phosphorylated myristoylated alanine-rich C kinase substrate
show the reaction diagram
ATP + Na,K-ATPase
ADP + phosphorylated Na,K-ATPase
show the reaction diagram
-
-
-
-
?
ATP + NADPH oxidase
ADP + phosphorylated NADPH oxidase
show the reaction diagram
-
-
-
-
?
ATP + phosphoinositide-dependent kinase
ADP + phosphorylated phosphoinositide-dependent kinase
show the reaction diagram
ATP + serotonin N-acetyltransferase
ADP + phosphorylated serotonin N-acetyltransferase
show the reaction diagram
-
PKC regulates the activity and stability of serotonin N-acetyltransferase in vivo, recombinant enzyme expressed in COS-7 cells
-
-
?
ATP + sodium channel
ADP + phosphorylated sodium channel
show the reaction diagram
-
PKC mediates inhibition of sodium channels and tetrodotoxin-sensitive transient sodium current by phosphorylation by topiramate, overview
-
-
?
ATP + vasodilator-stimulated phosphoprotein
ADP + phosphorylated vasodilator-stimulated phosphoprotein
show the reaction diagram
-
phosphorylation at Ser157
-
-
?
ATP + [low density lipoprotein receptor-related protein]
ADP + phosphorylated [low density lipoprotein receptor-related protein]
show the reaction diagram
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Cd2+
-
cell exposure to 0.020 mM cadmium for 24 h results in PKC activation
Mn2+
-
-
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-(5-isoquinolinesulfonyl)-2-methylpiperazine
-
-
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
angiotensin II type 2-receptor
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%
betaIIV5.3
-
0.01 mM, peptide translocation inhibitor of isozyme PKC betaII
-
BIM-I
inhibits encystment in vivo
bisindolylmaleimide
bisindolylmaleimide derivatives
bisindolylmaleimide I
bromoerol lactone
-
slight inhibition of PKCgamma oscillation at 0.1 mM
calphostin C
calphostin-C
-
inhibition of triiodothyronine-activation in forebrain, overview, can be partially reversed by triiodothyronone, i.e. T3
CG53353
chelerythrine
-
-
Chelerythrine chloride
interacts with the catalytic domain of PKC, inhibits encystment in vivo
cheletrytrine
-
complete inhibition at 0.05 mM
-
compound 48/80
-
complete inhibition of PKCgamma oscillation at 0.1 mM
CRLVLASC
-
targets isozyme PKCgamma, blocks formalin-induced pain response
curcumin
-
inhibits or activates PKC dependent on Ca2+ and the presence of membranes or phosphatidylserine, respectively, in presence of phosphatidylserine curcumin activates PKC, in presence of membranes with phosphatidylserine the enzyme is inhibited, Ca2+ competes with curcumin at the regulatory domainbinding site, overview, effects on different isozymes, overview
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
epsilonV1.2
-
0.01 mM, peptide translocation inhibitor of isozyme PKC epsilon
-
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
Go6976
Go6979
-
-
-
G 6976
G 6983
-
-
G-6976
G6983
-
an inhibitor of isozyme PKCbeta, but not of PKCmy
H-7
-
specific PKC inhibitor
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
KLFIMNL
-
targets isozyme PKCbetaI, inhibits cardiomyocyte hypertrophy
KQKTKTIK T
LEPEGK
-
-
LY333531
-
specific inhibition of PKCbeta
LY379196
-
highly specific for PKCbeta, inhibits amphetamine-stimulated dopamine efflux in striatum in vivo
-
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
-
-
N6-Dimethylaminopurine
-
-
NGRKI
-
-
NKMKSRLRKGALKKNV
-
autoregulatory pseudosubstrate sequence, residues 24-40
PAWHD
-
-
phenyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate
-
0.03 mM, inhibition: 48%
phorbol 12,13-dibutyrate
-
activates Na+,K+-ATPase activity at low concentration, but inhibits it at high concentration, the inhibitory effect can be reversed by preincubation with ethoxyresorufin, 17-octadecynoic acid, wortmannin, LY294002, cytochlasin D, or latrunculin B
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
QLMGGLHRHGAIINRKE
-
autoregulatory pseudosubstrate sequence, residues 391-407
RACK1 peptide I homologue
-
-
-
Ro 31-8220
-
i.e., 2-[1-[3-(amidinothio)propyl]-1H-indol-3-yl]-3-(1-methylindol-3-yl)-maleimide
Ro-31-7549
-
specific inhibitor for isozyme PKCalpha
Ro-31-8220
-
strong inhibition of PKCalpha
Ro-31-8425
-
-
Ro-32-0432
Ro318220
-
-
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
thymeleatoxin
-
activates Na+,K+-ATPase activity at low concentration, but inhibits it at high concentration
Tween 80
[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-dioctanoyl-sn-glycerol
-
-
1,2-diolein
activates, required
1,2-dioleoyl-sn-glycerol
-
activates
1-Oleoyl-2-acetyl-sn-glycerol
1-oleoyl-acetyl-sn-glycerol
-
0.01 mM
1-stearoyl-2-arachidonoyl-sn-glycerol
-
-
12-O-Tetradecanoylphorbol 13-acetate
12-O-tetradecanoylphorbol-13-acetate
13-O-acetylphorbol 12-myristate
-
-
4beta-phorbol 12-myristate 13-acetate
acetyl-beta-methylcholine
-
-
adenosine
-
-
Anionic phospholipids
-
isozymes alpha, betaI, betaII, and gamma require anionic phospholipids for activity, isozymes delta, epsilon, eta, and theta do not
-
arachidonic acid
-
alone or a combination of gamma-linolenic acid and phosphatidylserine slightly enhances PKC zeta activity; slightly enhances PKC zeta activity
ATP
-
-
cardiolipin
-
activates
CSF-1
-
CSF-1 increases PKCgamma Thr 410 phosphorylation and kinase activity in 32D.R cells
-
curcumin
-
inhibits or activates PKC dependent on Ca2+ and the presence of membranes or phosphatidylserine, respectively, in presence of phosphatidylserine curcumin activates PKC, in presence of membranes with phosphatidylserine the enzyme is inhibited, Ca2+ competes with curcumin at the regulatory domainbinding site, overview, effects on different isozymes, overview
diacylglycerol
Diacylglycerols
-
activate PKC isozymes
dioleoylglycerol
-
-
Epidermal growth factor
-
EGF, activates isozyme PKCalpha in the fetal lung during signaling involved in lung maturation, overview
fatty acids
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
hydrogen peroxide
-
-
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
IGF-1
-
-
-
Insulin
ionomycin
-
-
Kainic acid
-
phosphorylation of MARCKS by PKC isozymes is dramatically upregulated specifically in microglial cells after kainic acid-induced seizures, but not in other types of glial cells, overview, upregulation of isozymes PKCalpha, PKCbetaI, PKCbetaII, and PKCdelta
kenpaullone
-
20% activation of PKCalpha at 0.01 mM
mezerein
-
stimulates classical, but not novel PKC isozymes
palmitate
-
activates isozyme PKCtheta, but not isozymes PKCalpha and PKCepsilon
phorbol 12,13-dibutyrate
phorbol 12-myristate 13-acetate
phorbol 12-myristate-13-acetate
-
activation of protein kinase C significantly attenuates starvation- or rapamycin-induced LC3 processing. Activation of protein kinase C inhibits autophagy
phorbol dibutyrate
-
activates
phorbol ester
-
-
Phorbol esters
phorbol myristate acetate
-
-
phorbol-ester-12-13-dibutyrate
-
-
phosphatidylserine
phosphatidylserine-diolein
-
-
Phospholipid
Phospholipids
R59949
-
increases isofom PKCdelta and PKCepsilon activities in both membrane and cytosolic fractions
thymeleatoxin
transforming growth factor alpha
-
TGFalpha, activates isozyme PKCalpha in the fetal lung during signaling involved in lung maturation, overview
-
zileuton
-
zileuton acts as a PKC delta activator, causing it to translocate from the cytosol to nucleus, the activation is inhibited by rottlerin
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
0.0036
S6-(229-239) peptide
-
enzyme activated by cardiolipin
-
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
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