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.¹ 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.² 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.¹ EMD 638683 decreases body weight, fasting blood glucose and hemoglobin A1c (HbA1C) levels, and food intake in db/db diabetic mice.³ It also reduces angiotensin II-induced collagen deposition and cardiac fibrosis in mice.⁴

WARNING This product is not for human or veterinary use.

1. Ackermann, T.F., Boini, K.M., Beier, N., et al. EMD638683, a novel SGK inhibitor with antihypertensive potency. Cell. Physiol. Biochem. 28(1), 137-146 (2011).

2. Towhid, S.T., Liu, G.-L., Ackermann, T.F., et al. Inhibition of colonic tumor growth by the selective SGK inhibitor EMD638683. Cell. Physiol. Biochem. 32(4), 838-848 (2013).

3. Li, P., Hao, Y., Pan, F.-H., et al. SGK1 inhibitor reverses hyperglycemia partly through decreasing glucose absorption. J. Mol. Endocrinol. 56(4), 301-309 (2016).

4. Gan, W., Ren, J., Li, T., et al. The SGK1 inhibitor EMD638683, prevents angiotensin II-induced cardiac inflammation and fibrosis by blocking NLRP3 inflammasome activation. Biochim. Biophys. Acta Mol. Basis Dis. 1864(1), 1-10 (2018).