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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