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| 品牌 | absin | CAS | 1342278-01-6 |
|---|---|---|---|
| 分子式 | C16H14N4O2S | 純度 | ＞98% |
| 分子量 | 326.37 | 貨號 | abs810410 |
| 規格 | 5mg | 供貨周期 | 現貨 |
| 主要用途 | is a potent small molecule inhibitor of | 應用領域 | 化工,生物產業,農林牧漁,制藥/生物制藥,綜合 |
RKI-1447 1342278-01-6
| 產品描述 | |
| 描述 | RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2. |
| 純度 | >98% |
| 儲存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 別名 | RKI 1447; RKI1447 |
| 外觀 | Powder |
| 可溶性/溶解性 | DMSO 65 mg/mL (199.16 mM) |
| 生物活性 | |
| 靶點 | ROCK2 ,ROCK1 |
| In vitro(體外研究) | RKI-1447 is a cell-permeable pyridylthiazolyl-urea that acts as a potent, ATP site-targeting Rho Kinase inhibitor, displaying much reduced potency against PKA, PKN1/PRK1, p70S6K/RPS6kB1, AKT1, MRCKa/CDC42BPA (85.5%, 80.5%, 61.9%, 56.0%, and 50.4% inhibition, respectively, by 1 µM RKI-1447) or 15 other kinases. Crystal structures of the RKI-1447/ROCK1 complex reveals that RKI-1447 is a Type I kinase inhibitor that binds the ATP binding site through interactions with the hinge region and the DFG motif. RKI-1447 suppresses phosphorylation of the ROCK substrates MLC-2 and MYPT-1 in human cancer cells, but had no effect on the phosphorylation levels of the AKT, MEK, and S6 kinase at concentrations as high as 10 μM. RKI-1447 is also highly selective at inhibiting ROCK-mediated cytoskeleton re-organization (actin stress fiber formation) following LPA stimulation, but does not affect PAK-meditated lamellipodia and filopodia formation following PDGF and Bradykinin stimulation. RKI-1447 inhibits migration, invasion and anchorage-independent tumor growth of breast cancer cells. |
| In vivo(體內研究) | RKI-1447 is highly effective at inhibiting the outgrowth of mammary tumors in a transgenic mouse model. Tumors from mice treated with the RKI-1447 increases in size with an average percent change in tumor volume of only 8.8%. Thus, RKI-1447 inhibited mammary tumor growth by 87%, and on average the mammary tumors from Compared with those tumors from mice treated with the vehicle control, RKI-1447 treated mice are 7.7-fold smaller. RKI-1447 treatments does not result in mouse weight loss. |
| 研究領域 | |
| 研究領域 | CancerSignal transductionProtein phosphorylationSerine/threonine kinasesOther ApoptosisIntracellularKinases Signal TransductionProtein PhosphorylationSer / Thr KinasesOther Kinases Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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