Catalog Number: 5061
Chemical Name: N-[(3-Hydroxyphenyl)methyl]-N'-[4-(4-pyridinyl)-2-thiazolyl]urea dihydrochloride
Biological Activity
Potent and selective ROCK inhibitor (IC50 values are 6.2 and 14.5 nM for ROCK2 and ROCK1 respectively); suppresses phosphorylation of ROCK substrates MLC-2 and MYPT-1 in human cancer cells, but has no effect on the phosphorylation levels of Akt, MEK, and S6 kinase. Displays anti-invasive and antitumor activities in breast cancer cells.
Technical Data
  • M.Wt:
    399.29
  • Formula:
    C16H14N4O2S.2HCl
  • Solubility:
    Soluble to 10 mM in water with gentle warming and to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at -20°C
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer.
    Patel et al.
    Cancer Res., 2012;72:5025
  2. Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2)
    Pireddu et al.
    Med.Chem.Comm., 2013;3:699

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