protein kinase C gamma | Alpha subfamily | IUPHAR Guide to IMMUNOPHARMACOLOGY

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protein kinase C gamma

  Target has curated data in GtoImmuPdb

Target id: 1484

Nomenclature: protein kinase C gamma

Abbreviated Name: PKCγ

Family: Alpha subfamily

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 697 19q13.4 PRKCG protein kinase C gamma
Mouse - 697 7 Prkcg protein kinase C, gamma
Rat - 697 1q12 Prkcg protein kinase C, gamma
Previous and Unofficial Names
PKCC | SCA14 | PKC-gamma | PKCI | Prkcc | protein kinase C, gamma | protein kinase C
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Solution structure of the phorbol esters/diacylglycerol binding domain of protein kinase C gamma
PDB Id:  2E73
Resolution:  0.0Å
Species:  Human
Enzyme Reaction
EC Number:

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
ingenol mebutate Hs Activation 9.8 pKi 8
pKi 9.8 (Ki 1.62x10-10 M) [8]
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
Gö 6983 Hs Inhibition 8.2 pIC50 6
pIC50 8.2 (IC50 6x10-9 M) [6]
balanol Hs Inhibition 8.0 pIC50 3
pIC50 8.0 (IC50 1x10-8 M) [3]
GF109203X Bt Inhibition 7.7 pIC50 10
pIC50 7.7 (IC50 2x10-8 M) [10]
7-hydroxystaurosporine Hs Inhibition 7.5 pIC50 9
pIC50 7.5 (IC50 3x10-8 M) [9]
Ro-32-0432 Bt Inhibition 7.4 – 7.4 pIC50 2,11
pIC50 7.4 – 7.4 (IC50 3.7x10-8 – 3.65x10-8 M) [2,11]
ruboxistaurin Hs Inhibition 6.5 pIC50 7
pIC50 6.5 (IC50 3x10-7 M) [7]
enzastaurin Hs Inhibition 5.7 pIC50 4
pIC50 5.7 (IC50 2x10-6 M) [4]
View species-specific inhibitor tables
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

Reference: 1,5

Key to terms and symbols Click column headers to sort
Target used in screen: PKCγ/PKCg
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition -3.2 1.5 1.0
Ro-32-0432 Hs Inhibitor Inhibition 6.9
GF109203X Hs Inhibitor Inhibition 17.6 1.0 1.0
SB 218078 Hs Inhibitor Inhibition 32.8 92.0 96.0
midostaurin Hs Inhibitor Inhibition 35.6 15.0 6.0
K-252a Hs Inhibitor Inhibition 40.2 19.0 2.0
PKCbeta inhibitor Hs Inhibitor Inhibition 51.6 8.0 2.0
Gö 6983 Hs Inhibitor Inhibition 54.0 3.0 0.0
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 59.3 113.0 95.0
Gö 6976 Hs Inhibitor Inhibition 72.1 9.0 16.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
PKCγ is included in GtoImmuPdb based on the involvement of other PKC isozymes in immune processes.
Immuno Process Associations
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 1 GO processes
GO:0031397 negative regulation of protein ubiquitination IDA
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0050764 regulation of phagocytosis IEA
Clinically-Relevant Mutations and Pathophysiology
Disease:  Spinocerebellar ataxia 14; SCA14
Synonyms: Spinocerebellar ataxia [Disease Ontology: DOID:1441]
Disease Ontology: DOID:1441
OMIM: 605361
Orphanet: ORPHA98763


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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1039-45. [PMID:22037377]

2. Birchall AM, Bishop J, Bradshaw D, Cline A, Coffey J, Elliott LH, Gibson VM, Greenham A, Hallam TJ, Harris W et al.. (1994) Ro 32-0432, a selective and orally active inhibitor of protein kinase C prevents T-cell activation. J. Pharmacol. Exp. Ther., 268 (2): 922-9. [PMID:8114006]

3. Defauw JM, Murphy MM, Jagdmann Jr GE, Hu H, Lampe JW, Hollinshead SP, Mitchell TJ, Crane HM, Heerding JM, Mendoza JS et al.. (1996) Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A. J. Med. Chem., 39 (26): 5215-27. [PMID:8978850]

4. Faul MM, Gillig JR, Jirousek MR, Ballas LM, Schotten T, Kahl A, Mohr M. (2003) Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta. Bioorg. Med. Chem. Lett., 13 (11): 1857-9. [PMID:12749884]

5. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J., 451 (2): 313-28. [PMID:23398362]

6. Gschwendt M, Dieterich S, Rennecke J, Kittstein W, Mueller HJ, Johannes FJ. (1996) Inhibition of protein kinase C mu by various inhibitors. Differentiation from protein kinase c isoenzymes. FEBS Lett., 392 (2): 77-80. [PMID:8772178]

7. Jirousek MR, Gillig JR, Gonzalez CM, Heath WF, McDonald JH, Neel DA, Rito CJ, Singh U, Stramm LE, Melikian-Badalian A et al.. (1996) (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. J. Med. Chem., 39 (14): 2664-71. [PMID:8709095]

8. Kedei N, Lundberg DJ, Toth A, Welburn P, Garfield SH, Blumberg PM. (2004) Characterization of the interaction of ingenol 3-angelate with protein kinase C. Cancer Res., 64 (9): 3243-55. [PMID:15126366]

9. Seynaeve CM, Kazanietz MG, Blumberg PM, Sausville EA, Worland PJ. (1994) Differential inhibition of protein kinase C isozymes by UCN-01, a staurosporine analogue. Mol. Pharmacol., 45 (6): 1207-14. [PMID:8022414]

10. Toullec D, Pianetti P, Coste H, Bellevergue P, Grand-Perret T, Ajakane M, Baudet V, Boissin P, Boursier E, Loriolle F et al.. (1991) The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J. Biol. Chem., 266 (24): 15771-81. [PMID:1874734]

11. Wilkinson SE, Parker PJ, Nixon JS. (1993) Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem. J., 294 ( Pt 2): 335-7. [PMID:8373348]

How to cite this page

Alpha subfamily: protein kinase C gamma. Last modified on 22/03/2017. Accessed on 16/07/2020. IUPHAR/BPS Guide to PHARMACOLOGY,