Biochem/physiol Actions

Reversible: yes

Product competes with ATP.

Primary TargetROCK

Target IC₅₀: 25 µM against ROCK

Cell permeable: yes

General description

A cell-permeable indolopyridine compound that acts as a selective, reversible, and ATP-competitive inhibitor of Rho kinase activity with an IC₅₀ of 25 µM. Does not inhibit the activation of Rho kinase nor does it affect the in vitro activities of MLCK, PKCα, and SAPK2a/p38α. Shown to be 5-fold less potent than Y-27632 (Cat. No. 688000; IC₅₀ = ~5 µM), and display a similar specificity profile as H-89 (Cat. No. 371963). Affects cell migration, inhibits blebbing (IC₅₀ = ~ 12 µM in M2 cells), and decreases stress fibers in Bulb 3T3 cells at 50 µM.

A cell-permeable, selective, reversible, and ATP-competitive inhibitor of Rho kinase activity (IC₅₀ = 25 µM). Does not inhibit the activation of Rho kinase nor does it affect the in vitro activities of MLCK, PKCα, and SAPK2a/p38α. Shown to be 5-fold less potent than Y-27632 (Cat. No. 688000; IC₅₀ ~5 µM), and display a similar specificity profile as H-89 (Cat. No. 371963). Affects cell migration, inhibits blebbing (IC₅₀ ~12 µM in M2 cells), and decreases stress fibers in Bulb 3T3 cells at 50 µM.

Legal Information

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

Other Notes

Yarrow, J.C., et al. 2005. Chem. Biol.12, 385.

Packaging

Packaged under inert gas

10 mg in Plastic ampoule

Reconstitution

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

Warning

Toxicity: Standard Handling (A)