Description General description A cell-permeable isoquinolinesulfonamide compound that acts as a highly specific, reversible, 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 μM for PKC, and 10.1 μM 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 μM) in NT-2 cells. Reported to be more potent and selective than Y-27632 (Cat. Nos. 688000 and 688001). Mainly targets Aurora Kinase A, and induces polyploidization of acute megakaryocytic leukemia cells (AMKL). At 10 mM (500 µg/128 µl) solution of Rho Kinase Inhibitor (Cat. No. 555552) in H2O is also available. A cell-permeable isoquinolinesulfonamide compound that acts as a highly specific, reversible, potent, and ATP-competitive inhibitor of G-protein Rho-associated kinase (ROCK; Ki = 1.6 nM). Inhibits other serine/threonine kinases only at higher concentrations (Ki = 630 nM for PKA, 9.27 µM for PKC, and 10.1 µM for MLCK). Shown to selectively block lysophosphatidic acid-induced, but not PDBu-induced, phosphorylation of myristoylated alanine-rich C kinase substrate (MARCKS) in NT-2 cells (IC50 = 2.5 µM). Reported to be a more potent and selective inhibitor than Y-27632 (Cat. No. 688000 & 688001). Mainly targets Aurora Kinase A, and induces polyploidization of acute megakaryocytic leukemia cells (AMKL). Packaging 1 mg in Plastic ampoule Packaged under inert gas 5 mg in Glass bottle Biochem/physiol Actions Cell permeable: yes Primary Target ROCK Product competes with ATP. Reversible: yes Target Ki: 1.6 nM against G-protein Rho-associated kinase Warning Toxicity: Harmful (C) Reconstitution Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. Other Notes Wen, Qiang, et al. 2012. Cell150, 575. Ikenoya, M., et al. 2002. J. Neurochem.81, 9. Sasaki, Y., et al. 2002. Pharmacol. Ther.93, 225.