H-1152, an isoquinolinesulfonamide derivative, is a more specific, stronger and membrane-permeable inhibitor of Rho-kinase with a Ki value of 1.6 nM, but poor inhibitor of other serine/threonine kinases.

IC50 Value: 1.6 nM (Ki Value) [1]

Target: ROCK

in vitro: H-1152 dose-dependently inhibited the phosphorylation of MARCKS in human neuroteratoma (NT-2) cells stimulated by Rho-activator lysophosphatidic acid (LPA), which was determined by phosphorylation site-specific antibody against phospho-Ser159 in MARCKS, wheras it hardly inhibited the phosphorylation stimulated by phorbol-12,13-dibutyrate (PDBu) [1].
 

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