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S6K1 Inhibitor, PF-4708671-Calbiochem
| 产品编号： | 4168898 |
| 规格： | The S6K1 Inhibitor, PF-4708671 controls the biological activity of S6K1. This small molecule/inhibitor is primarily used for Cancer applications. |
| 包装规格： | 10 MG |
| 产品类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
产品别名
S6K1 Inhibitor, PF-4708671-Calbiochem
(2-((4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl)methyl)-5-(trifluoromethyl)-1H-benzo[d]imidazole, p70 Ribosomal S6 Kinase 1 Inhibitor
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C19H21F3N6 |
| Molecular weight | 390.41 |
| MDL number | MFCD18086922 |
| General description【一般描述】 | A cell-permeable piperazinyl-pyrimidine compound that acts as an inhibitor against S6K1 (Ki = 20 nM; IC50 = 160 nM) and MSK1 (IC50 = 950 nM) kinase activity, exhibiting little or much reduced potency against 85 other protein and lipid kinases (IC50 = 4.7, 9.2, 65 µM, respectively, against RSK1, RSK2, and S6K2; ≤27% inhibition of the rest at 1 µM). Shown to selectively inhibit IGF1- and PMA-stimulated S6K1 substrates phosphorylation in HEK-293 cells in a dose-dependent manner (up to 10 µM) in vitro and alleviate heart remodeling and functional damage in a MI (myocardial infarction) model in mice in vivo (75/mg/kg/daily i.p.). A cell-permeable piperazinyl-pyrimidine compound that acts as an inhibitor against S6K1 (Ki = 20 nM; IC50 = 160 nM) and MSK1 (IC50 = 950 nM) kinase activity, exhibiting little or much reduced potency against a panel of 75 other protein kinases (IC50 = 4.7, 9.2, 65 µM, respectively, against RSK1, RSK2, and S6K2; ≤27% inhibition of the rest at 1 µM) and 10 lipid kinases (≤6% inhibition at 10 µM). Inhibits IGF1-induced phosphorylation of cellular S6K1 substrates S6 (Ser235/236 and Ser240/244), mTOR (Ser2448), and Rictor (Thr1135) in serum-starved HEK-293 cultures, but not the phoshorylation of MSK or RSK cellular substrates (CREB Ser133 and GSK3α/β Ser21/ Ser9, respectively) upon PMA stimulation even at concentrations as high as 10 µM. Inhibition of S6K1 activation by rapamycin (Cat. Nos. 553210, 553211, & 553212) or S6K1 activity by PF-4708671 (75/mg/kg/daily i.p.) are both shown to alleviate heart remodeling and functional damage following left coronary artery ligation-induced MI (myocardial infarction) in mice in vivo. Cellular PF-4708671 treatment is also reported to result in increased S6K1 phosphorylation, likely due to a blockage of down-stream negative feedback mechanism. |
| Warning【警告】 | Toxicity: Standard Handling (A) |
| Reconstitution【重悬】 | Following reconstitution, aliquot and freeze (-20°C.) Stock solutions are stable for up to 6 months at -20°C. |
| Other Notes【其他说明】 | Di, R., et al. 2012. Biochem. J.441, 199. Pearce, L.R., et al. 2010. Biochem. J.431, 245. |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze protect from light |
| color【颜色】 | off-white |
| solubility【溶解性】 | DMSO: 50 mg/mL, pale yellow |
| shipped in【运输】 | ambient |
| storage temp.【储存温度】 | 2-8℃ |
| packaging【包装】 | 10 mg in Glass bottle Packaged under inert gas |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
