EMD 638683

EMD 638683 is an inhibitor of serum- and glucocorticoid-regulated kinase 1 (SGK1) that inhibits SGK1 by 85% when used at a concentration of 1 µM. It is greater than 27-fold selective for SGK1 over a panel of 11 kinases but does inhibit SGK2, SGK3, PRK2, and MSK1 by greater than 50% at 1 µM. EMD 638683 inhibits phosphorylation of the SGK1 target NDRG1 in HeLa cells (IC50 = 3.35 µM). It increases radiation-induced apoptosis of Caco-2 colon carcinoma cells when used at a concentration of 50 µM. Dietary administration of EMD 638683 (600 mg/kg) reduces the number of tumors in a mouse model of chemical carcinogenesis. It prevents fructose and saline consumption-induced increases in systolic blood pressure in mice. EMD 638683 decreases body weight, fasting blood glucose and hemoglobin A1c (HbA1C) levels, and food intake in db/db diabetic mice. It also reduces angiotensin II-induced collagen deposition and cardiac fibrosis in mice.Formal Name: 3,5-difluoro-alpha-hydroxy-benzeneacetic acid, 2-(2-ethyl-4-hydroxy-3-methylbenzoyl)hydrazide. CAS Number: 1181770-72-8. Molecular Formula: C18H18F2N2O4. Formula Weight: 364.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml, Ethanol: 25 mg/ml. SMILES: FC1=CC(F)=CC(C(O)C(NNC(C2=CC=C(O)C(C)=C2CC)=O)=O)=C1. InChi Code: InChI=1S/C18H18F2N2O4/c1-3-13-9(2)15(23)5-4-14(13)17(25)21-22-18(26)16(24)10-6-11(19)8-12(20)7-10/h4-8,16,23-24H,3H2,1-2H3,(H,21,25)(H,22,26). InChi Key: SSNAPUUWBPZGOY-UHFFFAOYSA-N.