Rho Kinase Inhibitor V

General Description

A cell-permeable pyrazolyl carboxamide compound that acts as a potent, ATP-binding pocket-targeting inhibitor of ROCK-II (IC₅₀ = 1.5 nM) and effectively inhibits the myosin light chain 2 phosphorylation on Thr18/Ser19 in A7r5 cells (IC₅₀ = 72 nM). It afftects the activities of PKA, MRCK, Akt1 (IC₅₀ = 0.186, 1.19, and 1.41 μM, respectively) and CYP-450 enzymes (% inhibition of 2C9/2D6/3A4/1A2 at 10 μM = 87/40/1/20, respectively) only at much higher concentrations.