SGK1 inhibitor is an inhibitor of serum- and glucocorticoid-regulated kinase 1 (SGK1) and SGK2. It is selective for SGK1 and SGK2 over SGK3 in the presence of a high concentration of ATP. SGK1 inhibitor prevents phosphorylation of GSK3β in U2OS cells and decreases cell viability in BYL719-insensitive HCC1954 cells when used in combination with the PI3Kα inhibitor BYL719. SGK1 inhibitor reduces tumor growth in an HCC1954 mouse xenograft model when administered in combination with BYL719.
ERK1 2 inhibitor 1 is a potent, orally bioavailable ERK1 2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively.