RKI 1447 dihydrochloride

Biological Activity

RKI 1447 dihydrochloride is a 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. RKI 1447 dihydrochloride enhances the efficacy of BET inhibitors on the downregulation of N-Myc in vitro and in vivo.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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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