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RKI 1447 dihydrochloride

Chemical Structure : RKI 1447 dihydrochloride

CAS No.: 1782109-09-4

RKI 1447 dihydrochloride (RKI-1447)

Catalog No.: PC-38731Not For Human Use, Lab Use Only.

RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC50 of 14.5 nM and 6.2 nM, respectively, suppresses phosphorylation of the ROCK substrates MLC-2 and MYPT-1 in human cancer cells.

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Biological Activity

RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC50 of 14.5 nM and 6.2 nM, respectively, suppresses phosphorylation of the ROCK substrates MLC-2 and MYPT-1 in human cancer cells.
RKI-1447 binds the ATP binding site through interactions with the hinge region and the DFG motif.
RKI-1447 shows no effect on the phosphorylation levels of the AKT, MEK, and S6 kinase.
RKI-1447 inhibited migration, invasion and anchorage-independent tumor growth of breast cancer cells (MDA-MB-231 cells, IC50=709 nM).
RKI-1447 is highly effective at inhibiting the outgrowth of mammary tumors in a transgenic mouse model.

Physicochemical Properties

M.Wt 399.290
Formula C16H16Cl2N4O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-[(3-Hydroxyphenyl)methyl]-N'-[4-(4-pyridinyl)-2-thiazolyl]urea dihydrochloride

References

1. Patel RA, et al. Cancer Res. 2012 Oct 1;72(19):5025-34.

2. Pireddu R, et al. Med Chem Commun. 2012;3(6):699–709.

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