850664-21-0

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.

GSK 269962 is a potent and selective Rho kinase (ROCK) inhibitor.

ROCK1: 1.6 nM (IC₅₀); ROCK2: 4 nM (IC₅₀); RSK1: 132 nM (IC₅₀); MSK1: 49 nM (IC₅₀); AKT1: 955 nM (IC₅₀); AKT2: 1350 nM (IC₅₀); AKT3: 1510 nM (IC₅₀); CDK2: 3500 nM (IC₅₀); GSK3α: 1260 nM (IC₅₀)

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[1] CHRIS DOE. Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.[J]. Journal of Pharmacology and Experimental Therapeutics, 2007, 320 1: 89-98. DOI: 10.1124/jpet.106.110635