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Eg5-I

Catalog No.GC10681

potent inhibitor of Eg5

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Eg5-I Chemical Structure

Cas No.: 1338701-15-7

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1mg
$68.00
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5mg
$252.00
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10mg
$437.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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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).

Chemical Properties

Cas No. 1338701-15-7 SDF
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
Formula C23H25NO2S M.Wt 379.5
Solubility ≤1mg/ml in ethanol;25mg/ml in DMSO;5mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.635 mL 13.1752 mL 26.3505 mL
5 mM 0.527 mL 2.635 mL 5.2701 mL
10 mM 0.2635 mL 1.3175 mL 2.635 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 32 reference(s) in Google Scholar.)

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