Proteins involved in PKC signaling pathways Chemical Reagents for PKC research    
  PKC kinases    PKC activators   PKC chromosomal Location
  PKC phosphatases   PKC inhibitors   PKC structure
  PKC interacting proteins        PKC transgenic mice
  PKC substrates       PKC knockout mice
PKC inhibitors    
PKC Inhibitor Year Title Web link
13-HODE 1999 The lipoxygenase product 13-hydroxyoctadecadienoic acid (13-HODE) is a selective inhibitor of classical PKC isoenzymes http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=10079174 
Annexin V 1995 Inhibitory effect of annexin V on protein kinase C activity in mesangial cell lysates http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=7588728 
Aprinocarsen 2004 The role of protein kinase C-alpha in malignancies of the nervous system and implications for the clinical development of the specific PKC-alpha inhibitor aprinocarsen (Review) http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=14719093
Bisindolylmaleimide GF 109203X 1991 The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=1874734 
Bryostatin-1 2003 Bryostatin-1: a novel PKC inhibitor in clinical development http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=14735696
BSP-A1/-A2 2003 The inhibitory effect of BSP-A1/-A2 on protein kinase C and tyrosine protein kinase http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=12736909
Butein 1998 Butein, a specific protein tyrosine kinase inhibitor http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=9571170 
Calphostin C 1992 Irreversible oxidative inactivation of protein kinase C by photosensitive inhibitor calphostin C http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=1281116 
Calphostin C 1997 Isoform specificity of activators and inhibitors of protein kinase C gamma and delta http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=9326378 
Chelerythrine 1990 Chelerythrine is a potent and specific inhibitor of protein kinase C http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=2244923 
Chelerythrine chloride 2001 Investigation of the inhibitory effects of chelerythrine chloride on the translocation of the protein kinase C betaI, betaII, zeta in human neutrophils http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=11765038
Curcumin 1993 Inhibitory effects of curcumin on protein kinase C activity induced by 12-O-tetradecanoyl-phorbol-13-acetate in NIH 3T3 cells http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=8504477 
Daphnetin 1999 Daphnetin, one of coumarin derivatives, is a protein kinase inhibitor http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=10403826 
Erbstatin 1990 Inhibition of protein kinase C by the tyrosine kinase inhibitor erbstatin http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=2242040 
H-7 1992 The structure and biological activities of the widely used protein kinase inhibitor, H7, differ depending on the commercial source http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=1530623 
Hispidin 1997 Synthetic hispidin, a PKC inhibitor, is more cytotoxic toward cancer cells than normal cells in vitro http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=9088624 
Hypocrellin A 2003 Inhibitory effect of hypocrellin A on protein kinase C in liver and skeletal muscle of obese Zucker rats http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=14992539
LY333531 2003 Selective protein kinase C inhibitors and their applications http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=14683472
Midostaurin 2001 Protein kinase C inhibitors as novel anticancer drugs http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=11772309
N-myristyl-Lys-Arg-Thr-Leu-Arg 1990 N-myristyl-Lys-Arg-Thr-Leu-Arg: a novel protein kinase C inhibitor http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=2153382 
NPC 15437 1991 2,6-Diamino-N-([1-oxotridecyl)-2-piperidinyl]methyl)hexanamide (NPC 15437): a selective inhibitor of protein kinase C http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=1793019 
PAP 1996 Phenylamino-pyrimidine (PAP) derivatives: a new class of potent and selective inhibitors of protein kinase C (PKC) http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=8764886 
PKC412 2000 PKC412--a protein kinase inhibitor with a broad therapeutic potential http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=8764886 
PKC412 2008 Inhibition of PKCalpha activation in human bone and soft tissue sarcoma cells by the selective PKC inhibitor PKC412 http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=18507025;
R8605 1991 [The inhibitory effect of a third generation retinoid, R8605, on protein kinase C activity in vitro] http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=1839520 
RK-286C 1990 A new inhibitor of protein kinase C, RK-286C (4'-demethylamino-4'-hydroxystaurosporine). I. Screening, taxonomy, fermentation and biological activity http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=2312404 
Ro 31-8220 1996 Atypical isoforms of pKc and insulin secretion from pancreatic beta-cells: evidence using Go 6976 and Ro 31-8220 as Pkc inhibitors http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=8885992 
Rottlerin 1994 Rottlerin, a novel protein kinase inhibitor http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=8123051 
Rottlerin 2003 Isoform-selectivity of PKC inhibitors acting at the regulatory and catalytic domain of mammalian PKC-alpha, -betaI, -delta, -eta and -zeta http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=15008511
Staurosporine 1989 The protein kinase inhibitor staurosporine, like phorbol esters, induces the association of protein kinase C with membranes http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=3408497 
Staurosporine 1992 Protein kinase C-dependent and -independent actions of a potent protein kinase C inhibitor, staurosporine http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=1426027 
UCN-01 1995 UCN-01, an anti-tumor drug, is a selective inhibitor of the conventional PKC subfamily http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=7867810 
UCN-01 and UCN-02 1989 UCN-01 and UCN-02, new selective inhibitors of protein kinase C. I. Screening, producing organism and fermentation http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=2722672 
UCN-01 and UCN-02 1989 UCN-01 and UCN-02, new selective inhibitors of protein kinase C. II. Purification, physico-chemical properties, structural determination and biological activities http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=2656615 
Vanicosides A and B 1994 Vanicosides A and B, protein kinase C inhibitors from Polygonum pensylvanicum http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=8176400 
Verbascoside 1991 Verbascoside isolated from Lantana camara, an inhibitor of protein kinase C http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=1812212 

 

Isozyme-Specific Protein Kinase C Inhibitors (IC50 values are in mM)                                                                                          Reference: Calbiochem Catalog
Product Calbiochem Cat. No.  PKCa PKCb PKCbI PKCbII PKCg PKCd PKCe PKCx PKCh PKCm Ref.
Bisindolylmaleimide I 203290 0.008 - 0.018 - - 0.21 0.132 5.8 - - 1
CGP41251 N/A 0.024 - 0.017 0.032 0.018 0.36 4.5 >1000 0.06 - 2
Gö 6976 365250 0.0023 - 0.006 - - - - - - 0.02 1