RKI-1447

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

RKI-1447是ROCK1和ROCK2的有效抑制剂，IC50分别为14.5 nM和6.2 nM，具有抗侵袭和抗肿瘤活性。

RKI-1447 is a potent inhibitor of ROCK1 and ROCK2, with IC50 of 14.5 nM and 6.2 nM, respectively, has anti-invasive and antitumor activities.(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.(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.

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.

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.

RKI-1447 | RKI1447 | RKI 1447. ROCK Inhibitor XIII

Cell Cycle/DNA Damage

ROCK

ROCK1| ROCK2

Cancer

——

1342278-01-6

326.37

C16H14N4O2S

>98% (HPLC)

DMSO: 65 mg/mL (199.16 mM)

O=C(NC1=NC(C2=CC=NC=C2)=CS1)NCC3=CC=CC(O)=C3

1-(3-Hydroxybenzyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea

(-20℃)

With Ice Pack

≥ 2 years