RKI-1447是高效的 ROCK1 和 ROCK2 的小分子抑制剂，IC₅₀ 值分别为14.5 nM 和 6.2 nM。

RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC 50 values of 14.5 nM and 6.2 nM, respectively.

Solid

ROCK2 6.2 nM (IC50) ROCK1 14.5 nM (IC

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : ≥ 50 mg/mL (153.20 mM)配制储备液