RKI-1447

RKI-1447
Identifiers
	IUPAC name 1-[(3-hydroxyphenyl)methyl]-3-(4-pyridin-4-yl-1,3-thiazol-2-yl)urea;
CAS Number	1342278-01-6 ;
PubChem CID	60138149;
ChemSpider	29315066;
UNII	F8GZ6C9MKZ;
ChEMBL	ChEMBL3218011;
CompTox Dashboard (EPA)	DTXSID501336679 ;
Chemical and physical data
Formula	C16H14N4O2S
Molar mass	326.37 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1=CC(=CC(=C1)O)CNC(=O)NC2=NC(=CS2)C3=CC=NC=C3;
	InChI 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]

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.

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[1] 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.

[2] 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.

[3] 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.

[4] 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.

[5] 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.

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See also

References