S6K1 Inhibitor, PF-4708671 - Calbiochem

General Description

A cell-permeable piperazinyl-pyrimidine compound that acts as an inhibitor against S6K1 (K_i = 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.).