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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target Rho-kinase
Product competes with ATP.
Reversible: yes
Target IC50: 0.9 and 1.8 µM against Rho-kinase using a peptide and MLC as substrate, respectively
Packaging
Packaged under inert gas
Warning
Toxicity: Harmful (C)
Physical form
A 10 mM (2 mg/582 µl) solution in H₂O.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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