EMD638683 is an orally active and highly selective serum/glucocorticoid-regulated kinase 1 (SGK1) inhibitor (IC50 = 3 μM against HeLa cellular NDRG1 phosphorylation) that significantly decreased blood pressure in fructose-treated mice but not in control saline-treated or in SGK1-knockout animals (4460 ppm in chow, ~600 mg/kg/day). EMD638683 promotes radiation-induced suicidal death of CaCo-2 colon tumor cells in vitro (50 μM) and decreases the number of colonic tumors following chemical carcinogenesis in vivo (4460 ppm in chow).
Orally active and highly selective serum/glucocorticoid-regulated kinase 1 (SGK1) inhibitor with anti-cancer and anti-hypertensive efficacy in vitro and in vivo.
International journal of molecular sciences, 21(19) (2020-10-03)
In diabetes mellitus, hyperglycemia promotes the osteogenic transdifferentiation of vascular smooth muscle cells (VSMCs) to enhance medial vascular calcification, a common complication strongly associated with cardiovascular disease and mortality. The mechanisms involved are, however, still poorly understood. Therefore, the present
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