Two Rho-associated kinases (ROCKS), ROCK1 and ROCK2, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. GSK269962 is a selective ROCK inhibitor with IC50 values of 1.6 and 6 nM for ROCK1 and ROCK2, respectively. It displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases. GSK269962 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). Oral administration of 1-30 mg/kg GSK269962 can dose-dependently lower blood pressure in spontaneously hypertensive rats.
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