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PKC
| Cat. No. | Product Name | CAS No. | Information |
|---|---|---|---|
| CSN16722 | Zoledronic acid monohydrate | 165800-06-6 | Zoledronic acid is an activator of protein kinase C with apoptotic effects on multiple myeloma cell lines. |
| CSN23775 | VTX-27 | 1321924-70-2 | VTX-27 is an inhibitor of protein kinase C θ (PKC θ) and PKC δ with Kis of 0.08 nM and 16 nM, respectively. |
| CSN26523 | Verosudil | 1414854-42-4 | Verosudil, also known as AR-12286, is a potent and selective Rho kinase inhibitor. AR-12286 was well tolerated and provided statistically significant reduction in IOP (intraocular pressure) in patients with XFS (exfoliation syndrome) and OHT (ocular hypertension) or XFG (exfoliative glaucoma). This drug may represent an additional therapeutic paradigm for the treatment of XFG. |
| CSN21991 | TPPB | 497259-23-1 | TPPB is a cell-permeable benzolactam-derived protein kinase C (PKC) activator with Ki of 11.9 nM. |
| CSN18071 | TAS-301 | 193620-69-8 | TAS-301 is an inhibitor of smooth muscle cell migration and proliferation, inhibits intimal thickening after balloon injury to rat carotid arteries. |
| CSN11980 | Staurosporine | 62996-74-1 | Staurosporine is a prototypical potent ATP-competitive multikinase 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. |
| CSN17145 | Sotrastaurin | 425637-18-9 | Sotrastaurin is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM and inactive to PKCζ. |
| CSN23069 | Ro 32-0432 | 151342-35-7 | Ro 32-0432 is a selective and orally active inhibitor of protein kinase C prevents T-cell activation. It displays slight selectivity for conventional PKC isoforms over Ca2+ and atypical PKC isoforms; binding affinities for rat isoforms are 9, 28, 31, 37 and 108 nM for PKC's α, βΙ, βΙΙ, γ and ε respectively. Ro 32-0432 is orally available and prevents T cell chronic inflammation in vivo. ). |
| CSN11854 | Ro 31-8220 mesylate | 138489-18-6 | Ro 31-8220 mesylate is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-, PKC-I, PKC-II, PKC-, and PKC-, respectively. |
| CSN26383 | R 59-022 | 93076-89-2 | R 59-022 is a diacylglycerol kinase inhibitor with IC50 of 2.8 μM. R 59-022 is a 5-HTR antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils[1][2][3][4]. |
| CSN24744 | PKC-theta inhibitor | 736048-65-0 | Protein kinase C theta (PKCθ) is a serine/threonine kinase that belongs to the calcium-independent protein kinase C family. It is a key enzyme in T cell activation, differentiation and survival. |
| CSN23246 | Ro 32-0432 hydrochloride | 1781828-85-0 | Potent, orally active PKC inhibitor |
| CSN25616 | PKCβ inhibitor 1 | 257879-35-9 | PKCβ Inhibitor is a potent, reversible and ATP-competitive PKCβ inhibitor with IC50 values of 5nM and 21nM for PKCβII and βI, respectively. |
| CSN15884 | Midostaurin | 120685-11-2 | PKC412 is a broad spectrum protein kinase inhibitor and inhibits conventional PKC isoforms (α, β, γ), PDFRβ, VEGFR2, Syk, PKCη, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1 and EGFR. |
| CSN27692 | PKC-iota inhibitor 1 | 2328094-11-5 | PKC-iota inhibitor 1 PKC-ι ℩ inhibitor with IC50 value of 0.34μM. |
| CSN11701 | Phorbol 12-myristate 13-acetate | 16561-29-8 | Phorbol 12-myristate 13-acetate is a PKC-activating phorbol ester, increases the intracellular Ca2 concentration (Ca2i) in a dose-dependent manner, with an EC50 of 11.7 nM. |
| CSN26933 | O-Desmethyl Midostaurin | 740816-86-8 | O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) via cytochrome P450 liver enzyme metabolism. O-Desmethyl Midostaurin can be used as an indicator for Midostaurin metabolism in vivo[1]. Midostaurin is a multi-targeted protein kinase inhibitor with IC50 ranging from 22-500 nM. |
| CSN16767 | Miltefosine | 58066-85-6 | Miltefosine is a mult-target inhibitor which can inhibit Akt, PI3K and PKC. |
| CSN12991 | Ruboxistaurin hydrochloride | 169939-93-9 | LY333531 is a -specific protein kinase C inhibitor. It competitively and reversibly inhibits PKC1 and PKC2 with IC50 values of 4.7 and 5.9 nM respectively. |
| CSN26193 | KT5823 | 126643-37-6 | KT 5823 is a selective inhibitor of the cGMP-dependent protein kinase (PKG) (Ki values are 0.23, 4 and > 10 μM for inhibition of PKG, PKC and PKA respectively). KT 5823 inhibits SNP-stimulated PKG activity with an IC50 of 60 nM in dispersed smooth muscle cells and has little effect on PKA activity at concentrations of up to 10 μM. |
| CSN26395 | K-252c | 85753-43-1 | K-252c, a staurosporine analog isolated from Nocardiopsis sp., is a cell-permeable PKC inhibitor, with an IC50 of 2.45 µM. K-252c induces apoptosis in human chronic myelogenous leukemia cancer cells. K-252c also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase, with IC50 values of 8, 8 and 10 μM respectively[1][2][3]. |
| CSN19714 | Juglone | 481-39-0 | Juglone significantly inhibits the proliferation and induce the apoptosis of SiHa cells and Caski cells, stimulates suicidal erythrocyte death or eryptosis at least in part by upregulation of ceramide abundance, energy depletion and activation of PKC, and prevents high-fat diet-induced liver injury and nerve inflammation in mice through inhibition of inflammatory cytokine secretion, NF-kappa B activation and endotoxin production. Its a natural product isolated and purified from the barks of Juglans regia L.. |
| CSN14537 | 6,10,11-Trihydroxy-3,3-dimethylpyrano[2,3-c]xanthen-7(3H)-one | 50597-93-8 | Isojacareubin, a natural product isolated and purified from the roots of Garcinia fusca Pierre., is a potent inhibitor of protein kinase C (PKC), suppresses hepatocellular carcinoma metastasis and induces apoptosis in vitro and in vivo, thus, it as a promising lead compound for the development of antihepatoma agents, and displays potent activity against H. |
| CSN11206 | Ingenol | 30220-46-3 | Ingenol is a diterpenoid with unique architecture and has derivatives possessing important anticancer activity. |
| CSN27678 | HA-100 dihydrochloride | 210297-47-5 | HA-100 is an isoquinoline compound with an added piperazinylsulfonyl group that acts as an inhibitor of protein kinases (PKs), including PKA, PKC, and PKG (IC50s = 8, 12, and 4 µM, respectively). |
| CSN26207 | HA-100 | 84468-24-6 | HA-100 is an inhibitor of cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase (IC50 values are 4, 8, 12 and 240 μM, respectively). |
| CSN19160 | H-89 dihydrochloride | 130964-39-5 | H 89 2HCl is a potent and selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) with IC50 of 48 nM. It also shows weak inhibition on PKG, PKC, CK1, CK2 and others kinases. |
| CSN19160 | H-89 dihydrochloride | 130964-39-5 | H 89 2HCl is a potent and selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) with IC50 of 48 nM. It also shows weak inhibition on PKG, PKC, CK1, CK2 and others kinases. |
| CSN10464 | Bisindolylmaleimide I | 133052-90-1 | GF109203X is a potent PKC inhibitor with IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKC, PKCI, PKCII, and PKC in cell-free assays, respectively, showing more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor. |
| CSN16571 | Go6976 | 136194-77-9 | G6976 is a pan inhibitor of Casup2sup-dependent PKC isozymes, PKC and PKC1, with IC50 values of 2.3nM and 6.2nM, respectively, but has no effect on Casup2sup-independent PKC isozymes PKC, and . |
| CSN10984 | Fasudil Hydrochloride | 105628-07-7 | Fasudil HCl is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with Ki of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and 36 μM, respectively. |
| CSN10772 | Dequalinium Chloride | 522-51-0 | Dequalinium Chloride is a PKC inhibitor with IC50 of 7-18 M, and also a selective blocker of apamin-sensitive K channels with IC50 of 1.1 M. |
| CSN21985 | Decursinol angelate | 130848-06-5 | Decursinol angelate (DA) blocks PGE2-induced activation of the EP2 receptor signaling pathway, including the activation of PKA and the phosphorylation of CREB. |
| CSN10745 | Daphnetin | 486-35-1 | Daphnetin is an inhibitor of EGFR, PKA and PKC with IC50 of 7.67 M, 9.33 M and 25.01 M respectively. It derives from plants of the genus Daphne. |
| CSN26161 | D-erythro-Sphingosine | 123-78-4 | D-Sphingosine inhibits protein kinase C. |
| CSN26558 | CRT0066854 hydrochloride | 2250019-91-9 | CRT0066854 hydrochloride is a potent and selective atypical PKCs inhibitor. CRT0066854 is against full-length (FL) PKCι, PKCζ, and ROCK-II kinases with IC50 values of 132 nM, 639 nM, and 620 nM, respectively[1]. |
| CSN10607 | Chelerythrine chloride | 3895-92-9 | Chelerythrine Chloride is a potent, cell-permeable inhibitor of protein kinase C (IC50 = 660 nM) and competitive with respect to the phosphate acceptor and non-competitive with respect to ATP. |
| CSN23664 | HA-100 hydrochloride | 141543-63-7 | C-1 HCl is a Protein kinase C and cyclic nucleotide dependent protein kinase inhibitor. |
| CSN20021 | Bryostatin 1 | 83314-01-6 | Bryostatin 1 is a Protein kinase C (PKC) activator that binds with high affinity (Ki = 1.35 nM). |
| CSN26742 | Bisindolylmaleimide VIII acetate | 138516-31-1 | Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively[1]. Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases[2]. |
| CSN25331 | Bisindolylmaleimide IV | 119139-23-0 | Bisindolylmaleimide IV is an inhibitor of protein kinase C. |
| CSN24270 | Bisindolylmaleimide X hydrochloride | 145317-11-9 | Bisindolylmaleimide is a potent PKC inhibitor and also a potent nAChR antagonist. |
| CSN12210 | α-Vitamin E | 59-02-9 | -Tocopherol is a type of vitamin E and an antagonist of PKC. |
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