产品描述:
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.{59340} 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.{59341} 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.{59340} EMD 638683 decreases body weight, fasting blood glucose and hemoglobin A1c (HbA1C) levels, and food intake in db/db diabetic mice.{59342} It also reduces angiotensin II-induced collagen deposition and cardiac fibrosis in mice.{59343}