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'''RKI-1447''' is a drug which acts as a potent and selective inhibitor of the [[enzyme]] [[Rho kinase]], with an IC<sub>50</sub> of 14.5 nM at [[ROCK1]] and 6.2 nM at [[ROCK2]]. It has been investigated for applications in [[cancer]] treatment,<ref>{{cite journal | vauthors = Patel RA, Forinash KD, Pireddu R, Sun Y, Sun N, Martin MP, Schönbrunn E, Lawrence NJ, Sebti SM | display-authors = 6 | title = RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer | journal = Cancer Research | volume = 72 | issue = 19 | pages = 5025–34 | date = October 2012 | pmid = 22846914 | doi = 10.1158/0008-5472.CAN-12-0954 }}</ref><ref>{{cite journal | vauthors = Dyberg C, Andonova T, Olsen TK, Brodin B, Kool M, Kogner P, Johnsen JI, Wickström M | display-authors = 6 | title = Inhibition of Rho-Associated Kinase Suppresses Medulloblastoma Growth | journal = Cancers | volume = 12 | issue = 1 | date = December 2019 | pmid = 31888022 | doi = 10.3390/cancers12010073 }}</ref><ref>{{cite journal | vauthors = Li L, Chen Q, Yu Y, Chen H, Lu M, Huang Y, Li P, Chang H | display-authors = 6 | title = RKI-1447 suppresses colorectal carcinoma cell growth via disrupting cellular bioenergetics and mitochondrial dynamics | journal = Journal of Cellular Physiology | volume = 235 | issue = 1 | pages = 254–266 | date = January 2020 | pmid = 31237697 | doi = 10.1002/jcp.28965 }}</ref> as well as [[glaucoma]],<ref>{{cite journal | vauthors = Dang Y, Wang C, Shah P, Waxman S, Loewen RT, Loewen NA | title = RKI-1447, a Rho kinase inhibitor, causes ocular hypotension, actin stress fiber disruption, and increased phagocytosis | journal = Graefe's Archive for Clinical and Experimental Ophthalmology = Albrecht Von Graefes Archiv Fur Klinische Und Experimentelle Ophthalmologie | volume = 257 | issue = 1 | pages = 101–109 | date = January 2019 | pmid = 30456419 | doi = 10.1007/s00417-018-4175-6 }}</ref> and [[nonalcoholic fatty liver disease]].<ref>{{cite journal | vauthors = Wang J, Jiang W | title = 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 | journal = Medical Science Monitor | volume = 26 | pages = e919220 | date = February 2020 | pmid = 32026851 | doi = 10.12659/MSM.919220 }}</ref>
'''RKI-1447''' is a drug which acts as a potent and selective inhibitor of the [[enzyme]] [[Rho kinase]], with an IC<sub>50</sub> of 14.5 nM at [[ROCK1]] and 6.2 nM at [[ROCK2]]. It has been investigated for applications in [[cancer]] treatment,<ref>{{cite journal | vauthors = Patel RA, Forinash KD, Pireddu R, Sun Y, Sun N, Martin MP, Schönbrunn E, Lawrence NJ, Sebti SM | display-authors = 6 | title = RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer | journal = Cancer Research | volume = 72 | issue = 19 | pages = 5025–34 | date = October 2012 | pmid = 22846914 | doi = 10.1158/0008-5472.CAN-12-0954 | pmc = 3463757 }}</ref><ref>{{cite journal | vauthors = Dyberg C, Andonova T, Olsen TK, Brodin B, Kool M, Kogner P, Johnsen JI, Wickström M | display-authors = 6 | title = Inhibition of Rho-Associated Kinase Suppresses Medulloblastoma Growth | journal = Cancers | volume = 12 | issue = 1 | date = December 2019 | page = 73 | pmid = 31888022 | doi = 10.3390/cancers12010073 | pmc = 7016943 }}</ref><ref>{{cite journal | vauthors = Li L, Chen Q, Yu Y, Chen H, Lu M, Huang Y, Li P, Chang H | display-authors = 6 | title = RKI-1447 suppresses colorectal carcinoma cell growth via disrupting cellular bioenergetics and mitochondrial dynamics | journal = Journal of Cellular Physiology | volume = 235 | issue = 1 | pages = 254–266 | date = January 2020 | pmid = 31237697 | doi = 10.1002/jcp.28965 | s2cid = 195356540 }}</ref> as well as [[glaucoma]],<ref>{{cite journal | vauthors = Dang Y, Wang C, Shah P, Waxman S, Loewen RT, Loewen NA | title = RKI-1447, a Rho kinase inhibitor, causes ocular hypotension, actin stress fiber disruption, and increased phagocytosis | journal = Graefe's Archive for Clinical and Experimental Ophthalmology = Albrecht von Graefes Archiv Fur Klinische und Experimentelle Ophthalmologie | volume = 257 | issue = 1 | pages = 101–109 | date = January 2019 | pmid = 30456419 | doi = 10.1007/s00417-018-4175-6 | s2cid = 51691810 }}</ref> and [[nonalcoholic fatty liver disease]].<ref>{{cite journal | vauthors = Wang J, Jiang W | title = 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 | journal = Medical Science Monitor | volume = 26 | pages = e919220 | date = February 2020 | pmid = 32026851 | doi = 10.12659/MSM.919220 | pmc = 7020744 }}</ref>


== See also ==
== See also ==

Revision as of 22:34, 29 December 2020

RKI-1447
Identifiers
  • 1-[(3-hydroxyphenyl)methyl]-3-(4-pyridin-4-yl-1,3-thiazol-2-yl)urea
CAS Number
PubChem CID
ChemSpider
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC16H14N4O2S
Molar mass326.37 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

  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.{{cite journal}}: CS1 maint: unflagged free DOI (link)
  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 = Albrecht von Graefes Archiv Fur Klinische und Experimentelle Ophthalmologie. 257 (1): 101–109. doi:10.1007/s00417-018-4175-6. 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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