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ζ-Stat (1,3,6-Naphthalenetrisulfonic acid) is a novel PKC-zeta (PKC-ζ) specific inhibitor with IC50 of 5 uM, showed only 13% inhibition on PKC-I at 20 uM; downregulates TNF-α induced NF-κB translocation to the nucleus there by inducing apoptosis, significantly decreases melanoma cell proliferation of SK-MEL-2 and MeWo.




BJE6-106 (B106) is a potent, selective PKCδ inhibitor with IC50 of 50 nM, displays excellent selectivity over classical PKC isozymes (a 1,000-fold PKCδ selectivity over PKCα); induces cell growth inhibition in melanoma cell lines with NRAS mutations at nanomolar concentrations; induces phosphorylation (activation) of JNK1/2 (T183/Y185) most strongly after two hr of exposure in SBcl2 cells, induces phosphorylation of MKK4, JNK and H2AX in NRAS mutant melanoma WM1366 cells.




AS2521780 is a potent, selective, orally bioavailable PKCθ inhibitor that inhibits combinant human PKCθ enzyme with IC50 of 0.48 nM, >30-fold higher than other PKC isoforms; also displays >100-fold selectivity over a panel of 27 protein kinases (100-fold over CDK2, IC50=84 nM); suppresses CD3/CD28-induced IL-2 gene transcription (IC50=14 nM) in Jurkat T cells and proliferation of human primary T cells (IC50=17 nM), also suppresses concanavalin A-induced cytokine production by rat splenocytes and monkey PBMCs with similar potency; potentially ameliorate T cell-mediated autoimmune diseases in vivo models.



1132609-87-0 PZ09 (PKC-zeta inhibitor 9, PKC-ζ inhibitor PZ9) is a potent, isoform selective PKC-zeta (PKC-ζ) inhibitor with IC50 of 5.18 nM, displays excellent selectivity (>200-fold) over other PKC isoforms with exception of PKC-i (10-fold); also shows high selectivity for CDK-2 (>200-fold), as well as a broader range of other kinases (<50% inhibition at 10 uM); PZ09 is a small-molecule inhibitor, the first tool to successfully interrogate aPKC signaling in cells.

Bryostatin 1

83314-01-6 Bryostatin 1 (NSC 339555) is a macrocyclic lactone derived from a marine invertebrate, fuctions as an activator of PKC with high binding affinity (Ki=1.35 nM); functions like the phorbol esters biochemically in binding to and activating protein kinase C; inhibits tumor promotion by phorbol esters in SENCAR mouse skin, induces differentiation of B-chronic lymphocytic leukemia cells; blocks phorbol ester action in Friend cells, restores the differentiation respons with EC50 of 15 nM.

Alzheimer Disease

Phase 2 Clinical



742038-81-9 ICA-1 is a potent, specific inhibitor of Protein Kinase C-iota (PKC-ι) with IC50 of 0.1 uM, does not inhibit PKC-ζ, the closely related atypical PKC family member; potently inhibits the phosphorylation of Cdk7 by PKC-ι, inhibits PKC-ι/Cdk7/cdk2 cell signaling pathway and exhibits antiproliferative effects in neuroblastoma cells, also induces apoptosis; significantly reduces migration and melanoma cell invasion, downregulates TNF-α induced NF-κB translocation to the nucleus there by inducing apoptosis.


PKCiota-IN-49 is a potent and selective inhibitor of Protein Kinase C iota (PKC-ι) with IC50 of 2.8 nM, >20-fold selectivity over PKC-α (IC50=71 nM) and PKC-β (IC50=350 nM); inhibits PKC-ι on the phosphorylation of substrate ECT2 in HCCLM3 cells with IC50 of 3.0 uM.

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