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Eg5-I
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Eg5-I图片
CAS NO:1338701-15-7
规格:98%
分子量:379.5
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
potent inhibitor of Eg5
CAS:1338701-15-7
分子式:C23H25NO2S
分子量:379.5
纯度:98%
存储:Store at -20°C

Background:

IC50: 127 and 190 nM for enzyme and cell, respectively


Eg5-I is a potent inhibitor of Eg5.


The kinesin-like spindle protein Eg5, also known as KSP and Kif11, is a motor protein that is essential for establishing a bipolar spindle during mitosis.


In vitro: Previous study found that the interphase microtubule morphology was normal after the treatment of Eg5-I, whereas spindle morphology mirrored that of the parent compound. Eg5-I was tested for inhibitory activity against a selected panel of mitotic kinesins with no measurable inhibition detected. To determine whether Eg5-I had a similar effect on KSP dynamics, cells were treated with Eg5-I and probed for KSP localization with anti-KSP antibodies. Eg5-I showed a dose-dependent depletion of KSP from the spindle, with a 1.63-fold increase in clearance of KSP over its parent compound, consistent with the biochemical-and cell-based assays. Eg5-I blocked bipolar spindle formation, whereas the parent compound was weakly active. Eg5-I was also evaluated for anti-proliferative activity against the NCI60 tumor panel and the growth inhibitory concentration anged from 10 nM to 3 μM across the panel, respectively [1].


In vivo: Up to now, there is no animal in vivo data reported for Eg5-I.


Clinical trial: So far, no clinical study has been conducted for Eg5-I.


Reference:
[1] Rodriguez, D. ,Ramesh, C.,Henson, L.H., et al. Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity. Bioorganic & Medicinal Chemistry 19(18), 5446-5453 (2011).