Rho Kinase Inhibitor

Biochem/physiol Actions

Reversible: yes

Product competes with ATP.

Target K_i: 1.6 nM against G-protein Rho-associated kinase

Primary TargetROCK

Cell permeable: yes

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; 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). Mainly targets Aurora Kinase A, and induces polyploidization of acute megakaryocytic leukemia cells (AMKL).

A cell-permeable isoquinolinesulfonamide compound that acts as a highly specific, reversible, potent, and ATP-competitive inhibitor of G-protein Rho-associated kinase (ROCK; K_i = 1.6 nM). Exhibits a much weaker affinity for other serine/threonine kinases (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 (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.

Legal Information

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

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.

Packaging

1 mg in Plastic ampoule

5 mg in Glass bottle

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Harmful (C)