HS56 is a highly selective and potent dual Pim/DAPK3 inhibitor that significantly reduces contractile intensity and phosphorylation levels of myosin light chain (LC20) in rat caudal arterial smooth muscle strips. HS56 decreases blood pressure in spontaneously hypertensive mice without affecting heart rate.
highly selective and potent dual Pim/DAPK3 inhibitor that significantly reduces contractile intensity and phosphorylation levels of myosin light chain (LC20)
Cell chemical biology, 25(10), 1195-1207 (2018-07-24)
Sustained vascular smooth muscle hypercontractility promotes hypertension and cardiovascular disease. The etiology of hypercontractility is not completely understood. New therapeutic targets remain vitally important for drug discovery. Here we report that Pim kinases, in combination with DAPK3, regulate contractility and
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