Aurora A Inhibitor I is a selective Aurora A inhibitor (Aurora A: IC50 at 0.0034 μM; Aurora B: IC50 at 3.4 μM), (B / A ratio=1000). Aurora A Inhibitor I belongs a class of 2,4-dianilinopyrimidine inhibitors. Its selectivity for Aurora A is 1000 folds over Aurora B, both in enzymatic assays and in cellular phenotypic assays. Thr217 of Aurora A is the critical residue as a “gating” binding to this agent, which is responsible for the enhanced selectivity over Aurora B.[1]
参考文献
A Class of 2,4-Bisanilinopyrimidine Aurora A Inhibitors with Unusually High Selectivity against Aurora B Ignacio Aliagas-Martin,Dan Burdick,et al J. Med. Chem 2009;52:3300–3307
[1] Aliagas-Martin I, et al. J Med Chem, 2009, 52(10), 3300-3307.
[2] Yuan H, et al. Carcinogenesis, 2012, 33(2), 285-293.
客户反馈数据
Western blot analysis of Histone and p-Histone. 0-10μM Aurora inhibitor I was added.
如果需要长期保存,请于零下二十度低温保存。
禁止用于人体及ZL!
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