GSK269962

Description	GSK 269962 is a potent ROCK inhibitor with IC50 values are 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively, which displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases. It may be used in OAB treatment. It has been shown to block the generation of inflammatory cytokines in lipopolysaccharide-stimulated monocytes and to induce vasorelaxation in preconstricted rat aorta (IC50 = 35 nM). It lowers blood pressure in a rat model of hypertension. It induced a reduction in blood pressure of approximately 10, 20, and 50 mm Hg at doses of 1, 3, and 30 mg/kg. It represent a novel class of ROCK inhibitors that have profound effects in the vasculature, which may enable us to further evaluate the potential beneficial effects of ROCK inhibition in animal models of cardiovascular as well as other chronic diseases.
Pathways	Cell Cycle/DNA Damage TGF beta/Smad Wnt/Stem Cell
Targets	ROCK

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