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PKC Protein Kinase C

Inhibitors

Cat.No.  Name Information
M1861 Silmitasertib (CX-4945) CX-4945 (Silmitasertib) is a potent small molecule protein kinase inhibitor that selectively binds to and inhibits the enzyme casein kinase II (CK2).
M3629 LY333531 hydrochloride LY333531 hydrochloride competitively and reversibly inhibits PKCβI and PKCβII (IC50 values are 4.7 and 5.9 nM respectively).
M2066 Staurosporine Staurosporine (AM-2282) is a potent ATP-competitive kinase inhibitor with IC50 of 0.7, 7, 8.5, 6, 20 nM for PKC, PKA,PKG, p60v-src tyrosine protein kinase, CaM kinase II, respectively.
M2850 Midostaurin Midostaurin (pkc412) is a multi-targeted kinase inhibitor, including PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50 ranging from 80-500 nM.
M4647 Phorbol 12-myristate 13-acetate Phorbol 12-myristate 13-acetate (PMA) is a PKC-activating phorbol ester, increases the intracellular Ca2+ concentration ([Ca2+]i) in a dose-dependent manner, with an EC50 of 11.7 nM.
M11271 (-)-Indolactam V (-) -IndolacTAM V is an activator of PKC, and the Ki values of η -CrD2 (PKCγ -substituted peptide) and γ -CrD2 (PKCγ -substituted peptide) are 3.36 nM and 1.03 μM, respectively. The Kd values for C1A and C1B domains of PKC were 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), respectively. At 137 nM (β-C1B), 138 nM (γ-C1A) and 213 nM (γ-C1B), it has antitumor activity.
M10995 Daphnoretin Daphnoretin (Dephnoretin) is extracted from Wikstroemia indica and has antiviral activity. Daphnoretin acts similarly to PMA in that it can directly activate protein kinase C, thereby activating NADPH oxidase.
M10490 Delcasertib Delcasertib (KAI-9803) is a potent and selective δ-protein kinase C (δPKC) inhibitor, it could ameliorate injury associated with ischemia and reperfusion in animal models of acute myocardial infarction (MI).
M9547 VTX-27 VTX-27 is a novel potent and selective PKCθ inhibitor, with Kis of 0.08 nM and 16 nM for PKC θ and PKC δ.
M9484 PKCβ inhibitor PKCβ inhibitor is a potent and selective inhibitor of PKCβ isozymes (IC50 = 5 nM and 21 nM for human PKCβII and βI).
M5319 Chelerythrine Chloride Chelerythrine is potent, cell-permeable inhibitor of protein kinase C (IC50 = 660 nM); competitive with respect to the phosphate acceptor and non-competitive with respect to ATP.
M5303 1-Naphthyl PP1 1-Naphthyl PP1(1-NA-PP 1) is a selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl (IC50 values are 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively).
M5032 Zoledronic acid monohydrate Zoledronic acid monohydrate(CGP 42446; ZOL 446) is an activator of protein kinase C with apoptotic effects on multiple myeloma cell lines. It inhibited proliferation of human foetal osteoblastic cell line (hFOB) with an IC50 of 40 uM.
M5030 Ingenol Mebutate Ingenol Mebutate is a substance found in the sap of the plant Euphorbia peplus and an inducer of cell death.
M4661 Chelerythrine Chelerythrine
M4647 Phorbol 12-myristate 13-acetate Phorbol 12-myristate 13-acetate (PMA) is a PKC-activating phorbol ester, increases the intracellular Ca2+ concentration ([Ca2+]i) in a dose-dependent manner, with an EC50 of 11.7 nM.
M4450 acteoside Verbascoside 是从 Lantana camara 中得到的糖苷类物质,为 ATP 竞争性的 PKC 抑制剂,IC50 值为 25 µM,具有抗肿瘤,抗炎,抗神经性疼痛等作用。
M3974 Ingenol Ingenol is a extremely weak protein kinase C (PKC) activator. Starting material for synthesis of ingenol derivatives.
M3804 Ro 31-8220 Ro 31-8220 is a protein kinase C inhibitor, with activity at other protein kinases (IC50 values are 33, 3, 8, 15 and 38 nM for PKCα, MAPKAP-K1b, MSK1, GSK3β and S6K1 respectively).
M3803 Sotrastaurin Sotrastaurin is a potent and orally-active pan-PKC inhibitor, with Kis of 0.22 nM, 0.64nM, 0.95 nM, 1.8 nM, 2.1 nM and 3.2 nM for PKCθ, PKCβ, PKCα, PKCη, PKCδ and PKCε, respectively.
M3802 GF 109203X GF 109203X is a very potent and selective inhibitor of protein kinase C, selective for the α and β1 isoforms (IC50 values are 0.0084, 0.0180, 0.210, 0.132, and 5.8 μM for α, β1, δ, ε and ζ isoforms respectively).
M3799 UCN-02 UCN-02 is an inhibitor of PKC and PKA with IC50 values of 0.062 and 0.25 microM, respectively.
M3756 Oncrasin-1 Oncrasin-1 is a small molecule RNA polymerase II inhibitor that kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations.
M3694 arcyriarubin A arcyriarubin A is a cell permeable protein kinase C (PKC) inhibitor.
M3629 LY333531 hydrochloride LY333531 hydrochloride competitively and reversibly inhibits PKCβI and PKCβII (IC50 values are 4.7 and 5.9 nM respectively).



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