Rho kinase inhibitor

Rho kinase inhibitors (rho-associated protein kinase inhibitor or ROCK inhibitor) are a series of compounds that target rho kinase (ROCK). Clinical trials have found that inhibition of the ROCK pathway contributes to the cardiovascular benefits of statin therapy. Furthermore, ROCK inhibitors may have clinical applications for anti-erectile dysfunction, antihypertension, and tumor metastasis inhibition.^[1]

Examples

Chemical structure of fasudil

• Fasudil, its hydrochloride salt is a drug approved by the U.S. Food and Drug Administration (FDA) used for improvement and prevention of cerebral vasospasm and the cerebral ischemic symptoms caused by it after subarachnoid hemorrhage surgery.
• Ripasudil, used in Japan for the treatment of glaucoma and ocular hypertension
• RKI-1447, a potent small molecule inhibitor of ROCK1 and ROCK2. Studies show that RKI-1447 could function conspicuous anti-invasive and anti-tumor activities.
• Y-27632, the first small molecule ROCK inhibitor. It selectively inhibits ROCK1 with K_i of 140 nM.^[2]
• GSK429286A
• Y-30141

References

1. James K. Liao et al. (Jul 2007). "Rho Kinase (ROCK) Inhibitors". J Cardiovasc Pharmacol 50 (1): 17–24. doi:10.1097/FJC.0b013e318070d1bd.
2. "information of different kinds of ROCK inhibitor". selleckchemicals.