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HS56 is an ATP-competitive dual Pim/DAPK3 inhibitor with Ki values of 0.26, 0.208, 2.94, and ＞100 μM for DAPK3, Pim-3, Pim-1, and Pim-2, respectively. HS56 inhibits LC20 phosphorylation and smooth muscle contraction. HS56 decreases blood pressure in spontaneously hypertensive mice. HS56 can be used in research of hypertension[1].

HS56 is a highly selective and potent dual Pim/DAPK3 inhibitor th at significantly reduces contractile intensity and phosphorylation levels of myosin light chain (LC20) in r at caudal arterial smooth muscle strips. HS56 decreases blood pressure in spontaneously hypertensive mice without affecting heart rate.

PIM3: 0.208 μM (Ki); PIM1: 2.94 μM (Ki); PIM2: ＞100 μM (Ki)

[1] Carlson DA, et, al. Targeting Pim Kinases and DAPK3 to Control Hypertension. Cell Chem Biol. 2018 Oct 18;25(10):1195-1207.e32. DOI:10.1016/j.chembiol.2018.06.006