Rho Kinase Inhibitor

A cell-permeable isoquinolinesulfonamide compound that acts as a highly specific, potent, and ATP-competitive inhibitor of G-protein Rho-associated kinase (ROCK; K_i = 1.6 nM). Inhibits other serine/threonine kinases only at higher concentrations (K_i = 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.

Cell permeable: no

Primary Target
ROCK

Product competes with ATP.

Target K_i: 1.6 nM against Rho-associated kinase (ROCK)

A 10 mM (500 µg/128 µl) solution of Rho Kinase Inhibitor (Cat. No. 555550) in H₂O.

Following initial thaw, aliquot and freeze (-20°C).

Ikenoya, M., et al. 2002. J. Neurochem.81, 9.
Sasaki, Y., et al. 2002. Pharmacol. Ther.93, 225.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Harmful (C)