hydroxyfasudil

Hydroxyfasudil is a small molecule inhibitor of Rho-associated protein kinase (ROCK), specifically targeting both ROCK1 and ROCK2 isoforms with IC50 values of approximately 0.73 μM and 0.72 μM respectively[1][6]. It is the hydroxylated active metabolite of fasudil (HA-1077)[3], which itself is a clinically used vasodilator in some countries for cerebral vasospasm and other vascular conditions[5]. Hydroxyfasudil also inhibits cAMP-dependent protein kinase (PKA) at much higher concentrations (IC50 ~37 μM), indicating selectivity for ROCK over PKA[1][6]. The drug has been studied experimentally for its effects on vascular tone, cytoskeletal dynamics, apoptosis regulation, and potential neuroprotective properties. It has not been approved for clinical use in the US or other major markets as of June 2025[2].

Other names

5-((1,4-Diazepan-1-yl)sulfonyl)isoquinolin-1(2H)-one1-(1-Hydroxy-5-isoquinolinesulfonyl)homopiperazineHydroxy-fasudil