RKI-1447 is a drug which acts as a potent and selective inhibitor of the

enzyme An enzyme () is a protein that acts as a biological catalyst by accelerating chemical reactions. The molecules upon which enzymes may act are called substrate (chemistry), substrates, and the enzyme converts the substrates into different mol ...

Rho kinase Rho-associated protein kinase or Rho-associated coiled-coil kinase (ROCK) is a kinase belonging to the AGC (PKA/ PKG/PKC) family of serine-threonine specific protein kinases. It is involved mainly in regulating the shape and movement of cells by ...

, with an IC₅₀ of 14.5 nM at

ROCK1 ROCK1 is a protein serine/threonine kinase also known as rho-associated, coiled-coil-containing protein kinase 1. Other common names are ROKβ and P160ROCK. ROCK1 is a major downstream effector of the small GTPase RhoA and is a regulator of the ...

and 6.2 nM at

ROCK2 Rho associated coiled-coil containing protein kinase 2 is a protein that in humans is encoded by the ROCK2 gene. Fasudil is an inhibitor of ROCK protein. Function The protein encoded by this gene is a serine/threonine kinase that regulates cyt ...

. It has been investigated for applications in

cancer Cancer is a group of diseases involving Cell growth#Disorders, abnormal cell growth with the potential to Invasion (cancer), invade or Metastasis, spread to other parts of the body. These contrast with benign tumors, which do not spread. Po ...

treatment, as well as

glaucoma Glaucoma is a group of eye diseases that can lead to damage of the optic nerve. The optic nerve transmits visual information from the eye to the brain. Glaucoma may cause vision loss if left untreated. It has been called the "silent thief of ...

, and nonalcoholic fatty liver disease.

References

{{pharm-stub Enzyme inhibitors Thiazoles 4-Pyridyl compounds 3-Hydroxyphenyl compounds Ureas

See also

References