Biochem/physiol Actions

Primary TargetRho-kinase

Reversible: yes

Product competes with ATP.

Cell permeable: yes

Target IC₅₀: 0.9 and 1.8 µM against Rho-kinase using a peptide and MLC as substrate, respectively

General description

A cell-permeable, hydroxylated metabolite of HA 1077 (Fasudil; Cat. No. 371970) that displays anti-anginal properties. Acts as an ATP-competitive and a reversible inhibitor of Rho-kinase (IC₅₀ = 0.9 and 1.8 µM using a peptide and MLC as substrate, respectively) with ~100-fold greater selectivity over MLCK, MRCKβ, and PKC. Reported to inhibit the Rho kinase-mediated contraction both in vitro and in vivo.

Legal Information

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

Other Notes

Ito, K., et al. 2003. J. Physiol.546, 823.Takemoto, M., et al. 2002. Circulation106, 57.Shimokawa, H., et al. 1999. Cardiovasc. Res.43, 1029.

Packaging

2 mg in Plastic ampoule

Packaged under inert gas

Physical form

A 10 mM (2 mg/582 µl) solution in H₂O.

Warning

Toxicity: Harmful (C)