H-1152
H-1152P
(S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]homopiperazine, 2HCl
ROCK Inhibitor White solid. PROTECT FROM LIGHT. HYGROSCOPIC. PACKAGED UNDER INERT GAS. A cell-permeable isoquinolinesulfonamide compound that acts as a highly specific, potent, and ATP-competitive inhibitor of G-protein Rho-associated kinase (ROCK; Ki = 1.6 nM). Exhibits a much weaker affinity for other serine/threonine kinases (Ki = 630 nM for PKA, 9.27 mM for PKC, and 10.1 mM for MLCK). Shown to selectively block lysophosphatidic acid-induced, but not PDBu-induced, phosphorylation of myristoylated alanine-rich C kinase substrate MARCKS (IC50 = 2.5 mM) in NT-2 cells. Reported to be more potent and selective than Y-27632 (Cat. Nos. 688000 and 688001). Purity: ≥95% by HPLC. Ref.: Ikenoya, M., et al. 2002. J. Neurochem. 81, 9. Sasaki, Y., et al. 2002. Pharmacol. Ther. 93, 225. |
