CAS NO: | 1338701-15-7 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 379.5 |
Cas No. | 1338701-15-7 |
Formula | C23H25NO2S |
Solubility | ≤1mg/ml in ethanol;25mg/ml in DMSO;5mg/ml in dimethyl formamide |
Chemical Name | (2R)-2-amino-3-[[(4-methoxyphenyl)diphenylmethyl]thio]-1-propanol |
Canonical SMILES | OC[C@@H](N)CSC(C1=CC=C(OC)C=C1)(C2=CC=CC=C2)C3=CC=CC=C3 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
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).