A cell-permeable piperazinyl-pyrimidine compound that acts as an inhibitor against S6K1 (Ki=20nM, IC50=160nM) and MSK1 (IC50=950nM) kinase activity, exhibiting little or much reduced potency against 85 other protein and lipid kinases ( IC50=4.7, 9.2, 65uM, respectively, against RSK1, RSK2, and S6K2, <27% inhibition of the rest at 1uM). Shown to selectively inhibit IGF1- and PMA-stimulated S6K1 substrates phosphorylation in HEK-293 cells in a dose-dependent manner (up to 10uM) 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.). Synonyms: (2-((4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl)methyl)-5-(trifluoromethyl)-1H-benzo[d]imidazole, p70 Ribosomal S6 Kinase 1 Inhibitor Molecular Formula: C19H21F3N6 Molecular Weight: 390.4 Solubility: DMSO (50mg/ml, pale yellow solution) Storage and Stability: Store at -20C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
Molecular Weight:
390.4
Purity:
98% (HPLC)
Form:
Supplied as an off-white solid.
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