H-1152

H-1152 is a membrane-permeable and selective ROCK inhibitor, with a K_i value of 1.6 nM, and an IC₅₀ value of 12 nM for ROCK2. IC50 & Target: IC50: 12 nM (ROCK2)^[1]
Ki: 1.6 nM (ROCK)^[2] In Vitro: H-1152 is an inhibitor of Rho-kinase, with an IC₅₀ of 12 nM for ROCK2. H-1152 (H-1152P) also shows less inhibitory activities against CaMKII, PKG, AuroraA, PKA, Src, PKC, MLCK, Abl, EGFR, MKK4, GSK3α, AMPK, and P38α, with IC₅₀s of 0.180, 0.360, 0.745, 3.03, 3.06, 5.68, 28.3, 7.77, 50.0, 16.9, 60.7, 100, and 100 μM, respectively^[1]. H-1152 potently inhibits Rho kinase, with a K_i of 1.6 nM, and slightly suppresses PKA, PKC and MLCK, with K_is of?0.63, 9.27, and 10.1 μM, respectively. H-1152 (0.1-10 μM) highly inhibits MARCKS phosphorylation, with an IC₅₀ value of 2.5 μM in LPA-treated cells, but shows no such obvious effects in PDBu-treated cells^[2]. H-1152 (0.5-10 μM) cuases no decreased neuronal survival. H-1152 (1, 5 or 10 μM) also exerts no alterations in the ratios of different neuronal morphologies. Furthermore, H-1152 (10 μM) increases neurite length in both BMP4 and LIF cultures^[3].