GSK-269962 is a potent and selective Rho kinase (ROCK) inhibitor (IC₅₀ values are 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively). It displays >30-fold selectivity for ROCK against a panel of serine/threonine kinases. Induces vasorelaxation in preconstricted rat aorta (IC₅₀ = 35 nM) and lowers blood pressure in a rat model of hypertension.