SGK1 Inhibitor

SGK1 inhibitor is an inhibitor of serum- and glucocorticoid-regulated kinase 1 (SGK1) and SGK2 (IC50s = 4.8 and 2.8 nM, respectively). It is selective for SGK1 and SGK2 over SGK3 in the presence of a high concentration of ATP (IC50s = 0.442, 0.924, and 23.3 μM, respectively) and only inhibits AMPK by more than 50% in a panel of 60 additional kinases when used at a concentration of 1 μM. SGK1 inhibitor prevents phosphorylation of GSK3β in U2OS cells with an IC50 value of 1.4 μM. It decreases cell viability in BYL719-insensitive HCC1954 cells when used in combination with the PI3Kα inhibitor BYL719 . SGK1 inhibitor (50 mg/kg) reduces tumor growth in an HCC1954 mouse xenograft model when administered in combination with BYL719.