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S6K1 Inhibitor, PF-4708671
(2-((4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl)methyl)-5-(trifluoromethyl)-1H-benzo[d]imidazole, p70 Ribosomal S6 Kinase 1 Inhibitor
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.).
产品信息
Form Off-white solid
Molar mass 390.4
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥98% by HPLC
Solubility DMSO
Chemical formula C19H21F3N6
商店和运输信息
Storage +2°C to +8°C
Ship Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Standard Handling |