Chemical Name:1-[(1,2-Dihydro-1-oxo-5-isoquinolinyl)sulfonyl]hexahydr
o-1H-1,4-diazepine
Biological Activity:
Cell-permeable active metabolite of
Fasudil (HA 1077; Cat. No. 0541). Produces ATP-competitive and reversible
inhibition of Rho-kinase and is ~ 100-fold selective over a range of other
protein kinases. Inhibits neutrophil migration and produces potent vasodilatory
effects in vivo.
Araiet
al (1993) Inhibition by the protein kinase inhibitor HA1077 of the
activation of NADPH oxidase in human neutrophils. Biochem.Pharmacol. 46
1487. Shimokawaet al (1999) Rho-kinase-mediated pathway induces
enhanced myosin light chain phosphorylations in a swine model of coronary
artery spasm. Cardiovasc.Res. 43 1029. Utsunomiya et al
(2001) Antianginal effects of hydroxyfasudil, a Rho-kinase inhibitor, in a
canine model of effort angina. Br.J.Pharmacol. 134 1724.