Biochem/physiol Actions
Cell permeable: no
Product competes with ATP.
Primary TargetROCK
Target Ki: 1.6 nM against Rho-associated kinase (ROCK)
General description
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). 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).
The InSolution™ Rho Kinase Inhibitor controls the biological activity of Rho Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Ikenoya, M., et al. 2002. J. Neurochem.81, 9.Sasaki, Y., et al. 2002. Pharmacol. Ther.93, 225.
Packaging
500 µg in Plastic ampoule
Physical form
A 10 mM (500 µg/128 µl) solution of Rho Kinase Inhibitor (Cat. No. 555550) in H2O.
Reconstitution
Following initial thaw, aliquot and freeze (-20°C).
Warning
Toxicity: Harmful (C)
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