RKI-1447 explained

RKI-1447 is a drug which acts as a potent and selective inhibitor of the enzyme Rho kinase, with an IC₅₀ of 14.5 nM at ROCK1 and 6.2 nM at ROCK2. It has been investigated for applications in cancer treatment,^{[1] [2] [3]} as well as glaucoma,^[4] and nonalcoholic fatty liver disease.^[5]

See also

• Rho kinase inhibitor

Notes and References

1. Patel RA, Forinash KD, Pireddu R, Sun Y, Sun N, Martin MP, Schönbrunn E, Lawrence NJ, Sebti SM . 6 . RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer . Cancer Research . 72 . 19 . 5025–34 . October 2012 . 22846914 . 10.1158/0008-5472.CAN-12-0954 . 3463757 .
2. Dyberg C, Andonova T, Olsen TK, Brodin B, Kool M, Kogner P, Johnsen JI, Wickström M . 6 . Inhibition of Rho-Associated Kinase Suppresses Medulloblastoma Growth . Cancers . 12 . 1 . December 2019 . 73 . 31888022 . 10.3390/cancers12010073 . 7016943 . free .
3. Li L, Chen Q, Yu Y, Chen H, Lu M, Huang Y, Li P, Chang H . 6 . RKI-1447 suppresses colorectal carcinoma cell growth via disrupting cellular bioenergetics and mitochondrial dynamics . Journal of Cellular Physiology . 235 . 1 . 254–266 . January 2020 . 31237697 . 10.1002/jcp.28965 . 195356540 .
4. Dang Y, Wang C, Shah P, Waxman S, Loewen RT, Loewen NA . RKI-1447, a Rho kinase inhibitor, causes ocular hypotension, actin stress fiber disruption, and increased phagocytosis . Graefe's Archive for Clinical and Experimental Ophthalmology. 257 . 1 . 101–109 . January 2019 . 30456419 . 10.1007/s00417-018-4175-6 . 51691810 . 7818579 .
5. Wang J, Jiang W . The Effects of RKI-1447 in a Mouse Model of Nonalcoholic Fatty Liver Disease Induced by a High-Fat Diet and in HepG2 Human Hepatocellular Carcinoma Cells Treated with Oleic Acid . Medical Science Monitor . 26 . e919220 . February 2020 . 32026851 . 10.12659/MSM.919220 . 7020744 .