RKI 1447 dihydrochloride

Cat. No. 5061

RKI 1447 dihydrochloride C16H14N4O2S.2HCl

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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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Pireddu et al (2013) Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2) Med.Chem.Comm. 3 699. PMID: 23275831.

Patel et al (2012) RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer. Cancer Res. 72 5025. PMID: 22846914.

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Keywords: RKI 1447 dihydrochloride, supplier, RKI1447, dihydrochloride, Potent, and, selective, ROCK, inhibitors, inhibits, anti-invasive, antitumor, breast, cancer, ROCK1, ROCK2, MLC-2, MYPT-1, Tocris Bioscience, Rho-Kinases Inhibitor products

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