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 GSK3beta 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 PI3Kalpha inhibitor BYL719 (Cay-16986). SGK1 inhibitor (50 mg/kg) reduces tumor growth in an HCC1954 mouse xenograft model when administered in combination with BYL719.Formal Name: N-[4-(3-amino-1H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]-2,3-dichloro-benzenesulfonamide. CAS Number: 1426214-51-8. Molecular Formula: C17H12Cl2N6O2S. Formula Weight: 435.3. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. SMILES: ClC1=CC=CC(S(NC2=CC=C(C3=CN=C(C(N)=NN4)C4=N3)C=C2)(=O)=O)=C1Cl. InChi Code: InChI=1S/C17H12Cl2N6O2S/c18-11-2-1-3-13(14(11)19)28(26,27)25-10-6-4-9(5-7-10)12-8-21-15-16(20)23-24-17(15)22-12/h1-8,25H,(H3,20,22,23,24). InChi Key: MBNNXCKHRKSGSU-UHFFFAOYSA-N.