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RKI-1447

CAS No. : 1342278-01-6

MCE 站：RKI-1447

产品活性：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。

研究领域：Cell Cycle/DNA Damage  |  Stem Cell/Wnt  |  Cytoskeleton  |  TGF-beta/Smad

作用靶点：ROCK

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.

相关产品：Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  Stem Cell Signaling Compound Library  |  TGF-beta/Smad Compound Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Reprogramming Compound Library  |  Cytoskeleton Compound Library  |  Anti-Breast Cancer Compound Library  |  Y-27632 dihydrochloride  |  Chroman 1  |  Fasudil Hydrochloride  |  Narciclasine  |  Ripasudil  |  GSK429286A  |  Y-33075  |  CMPD101  |  H-1152 dihydrochloride  |  Hydroxyfasudil  |  BDP5290  |  SR-3677  |  SB-772077B dihydrochloride  |  Pentanoic acid  |  ZINC00881524  |  Verosudil  |  ROCK-IN-1  |  ROCK2-IN-2

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