Chemistry:RKI-1447

From HandWiki
Short description: Chemical compound
RKI-1447
RKI-1447 structure.png
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC16H14N4O2S
Molar mass326.37 g·mol−1
3D model (JSmol)

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

References

  1. "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. doi:10.1158/0008-5472.CAN-12-0954. PMID 22846914. 
  2. "Inhibition of Rho-Associated Kinase Suppresses Medulloblastoma Growth". Cancers 12 (1): 73. December 2019. doi:10.3390/cancers12010073. PMID 31888022. 
  3. "RKI-1447 suppresses colorectal carcinoma cell growth via disrupting cellular bioenergetics and mitochondrial dynamics". Journal of Cellular Physiology 235 (1): 254–266. January 2020. doi:10.1002/jcp.28965. PMID 31237697. 
  4. "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. doi:10.1007/s00417-018-4175-6. PMID 30456419. 
  5. "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. doi:10.12659/MSM.919220. PMID 32026851.