H-1152 is a cell membrane-permeable and selective ROCK (Rho-kinase) inhibitor (Ki=1.6 nM) that increases neurite length in neuron-rich cultures and inhibits MARCKS Ser159 phosphorylation in LPA-stimulated neuronal cells.

ROCK2:12 nM, PKA:3.03 μM, Aurora A:0.745 μM, EGFR:50 μM, MLCK:28.3 μM, Src:3.06 μM, Abl:7.77 μM, PKC:5.68 μM, PKG:0.36 μM, GSK3α:60.7 μM, AMPK:100 μM, MKK4:16.9 μM, CaMK II:0.18 μM, P38α:100 μM

H-1152 potently inhibits Rho kinase (Ki = 1.6 nM) while exhibiting only mild inhibitory effects on PKA, PKC, and MLCK with Ki values of 0.63 μM, 9.27 μM, and 10.1 μM, respectively. In LPA-treated cells, H-1152 (0.1-10 μM) significantly suppresses MARCKS protein phosphorylation with an IC₅₀ of 2.5 μM, whereas no such pronounced effect was observed in PDBu-treated cells [2].
H-1152 (0.5-10 μM) does not reduce neuronal viability. Neither does H-1152 (1, 5, or 10 μM) alter the proportion of different neuronal morphologies. Furthermore, in both BMP4 and LIF culture systems, H-1152 (10 μM) enhances neurite outgrowth length [3].