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产品价格:电议      采购度:1604      原产地:美洲
发布时间:2021/7/24 5:38:10 所属地区:上海 上海市
简要描述:
RKI-1447是高效的ROCK1和ROCK2的小分子抑制剂, nM nM。
标签:rki
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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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更新时间:2024/1/2 10:14:41
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