RKI-1447


Catalog No. size PriceQuantity
M60415-2S 2 mg solid $129
M60415-10S 10mg solid $510

Description

Product Information
Molecular Weight: 326.37
Formula: C16H14N4O2S
Purity: >98%
CAS#: 1342278-01-6
Solubility: 10 mM in DMSO
Chemical Name: 1-(3-Hydroxybenzyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea
Storage: Powder -20oC 3 years 4oC 2 years In solvent -80oC 6 months -20oC 1 month

 

Biological Activity:


RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC50 values of 14.5 nM and 6.2 nM, respectively.

How to use:

In Vitro: RKI-1447 is a Type I kinase inhibitor that binds the ATP binding site through interactions with the hinge region and the DFG motif. RKI-1447 suppresses phosphorylation of the ROCK substrates mLC-2 and MYPT-1 in human cancer cells, but has no effect on the phosphorylation levels of the AKT, MEK and S6 kinase at concentrations as high as 10 μM. RKI-1447 is also highly selective at inhibiting ROCK-mediated cytoskeleton re-organization. RKI-1447 inhibits migration, invasion and anchorage-independent tumor growth of breast cancer cells[1].

In Vivo: RKI-1447 is highly effective at inhibiting the outgrowth of mammary tumors in a transgenic mouse model. RKI-1447 inhibits mammary tumor growth by 87% and on average the mammary tumors from RKI-1447 treated mice are 7.7 fold smaller compared to those tumors from mice treated with the vehicle control[1].

Reference:

[1]. Patel RA, et al. RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer. Cancer Res. 2012 Oct 1;72(19):5025-34.

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