serum-glucocorticoid regulated kinase

CKI-7 is a potent, ATP-competitive inhibitor of casein kinase 1 (CK1; IC50: 6 μM; Ki: 8.5 μM) and a selective Cdc7 kinase inhibitor. It also inhibits SGK, ribosomal S6 kinase-1 (S6K1), and MSK1.

SGK1-IN-1 (compound 14n) is a highly potent SGK1 (Serum Glucocorticoid Regulated Kinase 1) inhibitor, with inhibitory activities of 41 nm, 128 nm, and 310 nm against hSGK1 2 3 at 500 μM ATP, respectively, and can be used for studying SGK1-related cancers and metabolic diseases.

SGK1-IN-2 (14h) is a selective inhibitor of serum and glucocorticoid-regulated kinase 1 (SGK1), with an IC50 of 5 nM at a 10 μM ATP concentration.

GSK 650394 is an inhibitor of serum- and glucocorticoid-regulated kinases (SGK) that inhibits SGK1 and SGK2 (IC50=62 103 nM). GSK 650394 has antitumor activity and also inhibits osteoclast differentiation and prevents bone loss.

EMD638683,a novel SGK inhibitor with antihypertensive potency(with an IC50 of 3 μM).

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.

SGK1-IN-4 is a selective inhibitor of SGK1 and can be used in studies about osteoarthritis.