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PKC
| 货号 | 产品名 | CAS号 | 信息 |
|---|---|---|---|
| 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. |
| CSN23871 | UCN-01 | 112953-11-4 | UCN-01 is a selective inhibitor of protein kinase C. |
| 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. |
| 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. ). |
| CSN17625 | Ro 31-8220 | 125314-64-9 | Ro 31-8220 is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, 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. |
| CSN23052 | Prostratin | 60857-08-1 | Prostratin is a PKC and NF-κB activator. |
| 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. |
| CSN27692 | PKC-iota inhibitor 1 | 2328094-11-5 | PKC-iota inhibitor 1 PKC-ι ℩ inhibitor with IC50 value of 0.34μM. |
| CSN26392 | Phorbol 12,13-dibutyrate | 37558-16-0 | Phorbol 12,13-dibutyrate is a PKC activator and a potent skin tumor promoter[1][2]. |
| CSN13863 | Phellopterin | 2543-94-4 | Phellopterin, a natural product isolated and purified from the roots of Saposhnikovia divaricata, is a partial agonist of the central benzodiazepine receptors in vitro, shows cytotoxic effect on RAW264.7 cell at the concentration from 40 to 400 μM, and reduces TNF-alpha-induced VCAM-1 expression through regulation of the Akt and PKC pathway, which contributes to inhibit the adhesion of monocytes to endothelium. |
| 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. |
| CSN18434 | (2-(Adamantan-1-yl)-6,8-dichloroquinolin-4-yl)(piperidin-2-yl)methanol | 785718-37-8 | NSC305787 is a small molecule inhibitor of PKC, with IC50 of 8.3 μM, 9.4 μM, 55 μM for PKCΙ phosphorylation of recombinant ezrin, of moesin, and of radixin. |
| CSN18323 | (Rac)-NSC305787 hydrochloride | 53868-26-1 | NSC305787 HCl is a small molecule inhibitor of PKC, with IC50 of 8.3 μM, 9.4 μM, 55 μM for PKCΙ phosphorylation of recombinant ezrin, of moesin, and of radixin. |
| CSN16767 | Miltefosine | 58066-85-6 | Miltefosine is a mult-target inhibitor which can inhibit Akt, PI3K and PKC. |
| CSN20625 | Darovasertib | 1874276-76-2 | LXS196 is a potent and orally active protein kinase C (PKC) inhibitor used for the treatment of uveal melanoma. |
| 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. |
| CSN21408 | Delcasertib | 949100-39-4 | KAI-9803 is a potent and selective δ protein kinase C (δ PKC) inhibitor. |
| 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. It's 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. |
| CSN16020 | Ingenol Mebutate | 75567-37-2 | Ingenol mebutate is a substance found in the sap of the plant Euphorbia peplus and an inducer of cell death. |
| 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. |
| CSN22823 | DCP-LA | 28399-31-7 | FR 236924 is a selective PKCε activator. |
| 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 μM, and also a selective blocker of apamin-sensitive K+ channels with IC50 of 1.1 μM. |
| 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 μM, 9.33 μM and 25.01 μM 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]. |
| CSN19868 | Chelerythrine | 34316-15-9 | Chelerythrine, a natural product isolated and purified from the herbs of Chelidonium majus with potent antimanic, antiproliferatvie and antitumor effect, can inhibit telomerase activity, and is a well-known protein kinase C inhibitor. |
| CSN17986 | CGP60474 | 164658-13-3 | CGP60474 is a promising inhibitor of PKC with a high degree of selectivity versus other serine/threonine and tyrosine kinases and show competitive kinetics relative to ATP. |
| CSN22738 | Calphostin C | 121263-19-2 | Calphostin C is a potent, selective and photo-dependent inhibitor of protein kinase C that targets the regulatory domain with IC50 of 50 nM. |
| 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). |
| CSN24270 | Bisindolylmaleimide X hydrochloride | 145317-11-9 | Bisindolylmaleimide xHCl is a potent protein kinase C (PKC) inhibitor. |
| 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. |
| CSN22715 | Bisindolylmaleimide II | 137592-45-1 | Bisindolylmaleimide II is a potent, ATP-competitive protein kinase C (PKC) inhibitor with IC50 of 0.01 μM, and also a potent nAChR antagonist. |
| CSN64509 | (±)-1,2-Diolein | 2442-61-7 |
