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

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protein kinase C beta

  Target has curated data in GtoImmuPdb

Target id: 1483

Nomenclature: protein kinase C beta

Abbreviated Name: PKCβ

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 - 673 16p12 PRKCB protein kinase C beta
Mouse - 673 7 Prkcb protein kinase C
Rat - 671 1q36 Prkcb protein kinase C
Gene and Protein Information Comments
The human PKCβ listed here is the longer isoform 2 (aka PKCβ2). A shorter isoform, PKCβ1, with 671 amino acids exists (isoform 1) and has RefSeq protein ID NP_997700.
Previous and Unofficial Names
PRKCB1 | PRKCB2 | PKC-beta | protein kinase C beta I | protein kinase C beta II | protein kinase C
Database Links
BRENDA
CATH/Gene3D
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.11.13

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

Activators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Parameter Reference
ingenol mebutate Hs Activation 10.0 pKi 9
pKi 10.0 (Ki 1.05x10-10 M) [9]
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Parameter Reference
sotrastaurin Hs Inhibition 8.7 pIC50 14
pIC50 8.7 (IC50 2x10-9 M) [14]
PKCbeta inhibitor Hs Inhibition 8.3 pIC50 12
pIC50 8.3 (IC50 5x10-9 M) [12]
ruboxistaurin Hs Inhibition 8.2 pIC50 8
pIC50 8.2 (IC50 5.9x10-9 M) [8]
Gö 6983 Hs Inhibition 8.1 pIC50 7
pIC50 8.1 (IC50 7x10-9 M) [7]
balanol Hs Inhibition 8.0 pIC50 4
pIC50 8.0 (IC50 1x10-8 M) [4]
GF109203X Bt Inhibition 7.8 pIC50 13
pIC50 7.8 (IC50 1.6x10-8 M) [13]
7-hydroxystaurosporine Hs Inhibition 7.5 pIC50 11
pIC50 7.5 (IC50 3.4x10-8 M) [11]
enzastaurin Hs Inhibition 7.5 pIC50 5
pIC50 7.5 (IC50 3x10-8 M) [5]
Ro-32-0432 Bt Inhibition 7.5 – 7.5 pIC50 2,15
pIC50 7.5 – 7.5 (IC50 3.1x10-8 – 3x10-8 M) [2,15]
bisindolylmaleimide IV Hs Inhibition 6.7 pIC50 12
pIC50 6.7 (IC50 2.12x10-7 M) [12]
Description: PKCβ2 isoform
CGP53353 Hs Inhibition 6.4 pIC50 3
pIC50 6.4 (IC50 3.98x10-7 M) [3]
View species-specific inhibitor tables
Inhibitor Comments
Bisindolylmaleimide IV also inhibits the shorter isoform of PKCβ, PKCβ1 with an IC50 value of 304nM [12].
Gö 6976 inhibits human PKCβ1 with an IC50 value of 6.2nM [10].
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.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx


Reference: 1,6

Key to terms and symbols Click column headers to sort
Target used in screen: PKCβI/PKCb1
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
GF109203X Hs Inhibitor Inhibition 3.2 4.0 1.0
Ro-32-0432 Hs Inhibitor Inhibition 3.7
staurosporine Hs Inhibitor Inhibition 4.1 1.0 1.0
PKCbeta inhibitor Hs Inhibitor Inhibition 9.8 19.0 2.0
Gö 6976 Hs Inhibitor Inhibition 18.7 6.0 6.0
Gö 6983 Hs Inhibitor Inhibition 19.3 4.0 -1.0
midostaurin Hs Inhibitor Inhibition 22.4 66.0 14.0
SB 218078 Hs Inhibitor Inhibition 22.5 95.0 91.0
bisindolylmaleimide IV Hs Inhibitor Inhibition 26.1 66.0 23.0
K-252a Hs Inhibitor Inhibition 26.3 53.0 13.0
Target used in screen: PKCβII/PKCb2
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Ro-32-0432 Hs Inhibitor Inhibition 2.3
staurosporine Hs Inhibitor Inhibition 3.0 3.5 2.0
PKCbeta inhibitor Hs Inhibitor Inhibition 4.3 27.0 6.0
SB 218078 Hs Inhibitor Inhibition 6.4 112.0 108.0
midostaurin Hs Inhibitor Inhibition 9.5 61.0 45.0
Gö 6976 Hs Inhibitor Inhibition 9.7 23.0 29.0
GF109203X Hs Inhibitor Inhibition 12.6 9.0 2.0
K-252a Hs Inhibitor Inhibition 13.8 67.0 18.0
Gö 6983 Hs Inhibitor Inhibition 14.2 4.0 3.0
CGP53353 Hs Inhibitor Inhibition 15.5 93.0 103.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
PKCβ is included in GtoImmuPdb based on its GO immune process associations.
Immuno Process Associations
Immuno Process:  Immune system development
GO Annotations:  Associated to 1 GO processes
GO:0045637 regulation of myeloid cell differentiation TAS
Immuno Process:  B cell (activation)
GO Annotations:  Associated to 2 GO processes
GO:0042113 B cell activation ISS
click arrow to show/hide IEA associations
GO:0002250 adaptive immune response IEA
Immuno Process:  Immune regulation
GO Annotations:  Associated to 3 GO processes
GO:0045637 regulation of myeloid cell differentiation TAS
GO:0050853 B cell receptor signaling pathway ISS
GO:0050861 positive regulation of B cell receptor signaling pathway ISS
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 3 GO processes
GO:0042113 B cell activation ISS
GO:0050853 B cell receptor signaling pathway ISS
GO:0050861 positive regulation of B cell receptor signaling pathway ISS
Immuno Process:  T cell (activation)
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0002250 adaptive immune response IEA

References

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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. Chalfant CE, Ohno S, Konno Y, Fisher AA, Bisnauth LD, Watson JE, Cooper DR. (1996) A carboxy-terminal deletion mutant of protein kinase C beta II inhibits insulin-stimulated 2-deoxyglucose uptake in L6 rat skeletal muscle cells. Mol. Endocrinol., 10 (10): 1273-81. [PMID:9121494]

4. 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]

5. 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]

6. 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]

7. 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]

8. 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]

9. 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]

10. Martiny-Baron G, Kazanietz MG, Mischak H, Blumberg PM, Kochs G, Hug H, Marmé D, Schächtele C. (1993) Selective inhibition of protein kinase C isozymes by the indolocarbazole Gö 6976. J. Biol. Chem., 268 (13): 9194-7. [PMID:8486620]

11. 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]

12. Tanaka M, Sagawa S, Hoshi J, Shimoma F, Matsuda I, Sakoda K, Sasase T, Shindo M, Inaba T. (2004) Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors. Bioorg. Med. Chem. Lett., 14 (20): 5171-4. [PMID:15380221]

13. 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]

14. Wagner J, von Matt P, Sedrani R, Albert R, Cooke N, Ehrhardt C, Geiser M, Rummel G, Stark W, Strauss A et al.. (2009) Discovery of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a potent and selective inhibitor of protein kinase C isotypes. J. Med. Chem., 52 (20): 6193-6. [PMID:19827831]

15. 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 beta. Last modified on 22/03/2017. Accessed on 16/02/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1483.