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Chemical compound
RKI-1447
1-[(3-hydroxyphenyl)methyl]-3-(4-pyridin-4-yl-1,3-thiazol-2-yl)urea
CAS Number
PubChem
CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (
EPA )
Formula C 16 H 14 N 4 O 2 S
Molar mass 326.37 g·mol−1 3D model (
JSmol )
C1=CC(=CC(=C1)O)CNC(=O)NC2=NC(=CS2)C3=CC=NC=C3
InChI=1S/C16H14N4O2S/c21-13-3-1-2-11(8-13)9-18-15(22)20-16-19-14(10-23-16)12-4-6-17-7-5-12/h1-8,10,21H,9H2,(H2,18,19,20,22)
Key:GDVRVPIXWXOKQO-UHFFFAOYSA-N
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
^ Patel RA, Forinash KD, Pireddu R, Sun Y, Sun N, Martin MP, et al. (October 2012).
"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.
doi :
10.1158/0008-5472.CAN-12-0954 .
PMC
3463757 .
PMID
22846914 .
^ Dyberg C, Andonova T, Olsen TK, Brodin B, Kool M, Kogner P, et al. (December 2019).
"Inhibition of Rho-Associated Kinase Suppresses Medulloblastoma Growth" . Cancers . 12 (1): 73.
doi :
10.3390/cancers12010073 .
PMC
7016943 .
PMID
31888022 .
^ Li L, Chen Q, Yu Y, Chen H, Lu M, Huang Y, et al. (January 2020). "RKI-1447 suppresses colorectal carcinoma cell growth via disrupting cellular bioenergetics and mitochondrial dynamics". Journal of Cellular Physiology . 235 (1): 254–266.
doi :
10.1002/jcp.28965 .
PMID
31237697 .
S2CID
195356540 .
^ Dang Y, Wang C, Shah P, Waxman S, Loewen RT, Loewen NA (January 2019).
"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.
doi :
10.1007/s00417-018-4175-6 .
PMC
7818579 .
PMID
30456419 .
S2CID
51691810 .
^ Wang J, Jiang W (February 2020).
"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.
doi :
10.12659/MSM.919220 .
PMC
7020744 .
PMID
32026851 .