GSK269962A hydrochloride (GSK 269962 hydrochloride) is a highly potent inhibitor of ROCK1 and ROCK2, with IC50 values of 1.6 nM and 4 nM, respectively, for recombinant human isoforms. This compound exhibits both anti-inflammatory and vasodilatory properties.

Akt3:1510 nM (IC50), MSK1:49 nM (IC50), ROCK1:1.6 nM (IC50), ROCK2:4 nM (IC50), CDK2:3500 nM (IC50), Akt2:1350 nM (IC50), GSK-3α:1260 nM (IC50), Akt1:955 nM (IC50), RSK1:132 nM (IC50)

GSK269962A has an IC 50 of 1.6 nM toward recombinant human ROCK1. GSK269962A exhibits more than 30-fold selectivity against a panel of serine/threonine kinases[1]. GSK269962A induces vasorelaxation in preconstricted rat aorta with an IC 50 of 35 nM[1].

GSK269962A is a potent antihypertensive agent. GSK269962A (0.3, 1, and 3 mg/kg; oral gavage) induces a dose-dependent reduction in blood pressure in spontaneously hypertensive rat (SHR). The reduction of blood pressure is acute and substantial[1]. Animal Model: Male Sprague-Dawley rats (350-400g)[1]Dosage: 0.3, 1, and 3 mg/kg Administration: Oral gavage; 12 hours Result: Induced a dose-dependent reduction in blood pressure.