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Merck
CN

324631

Eg5 Inhibitor VII - CAS 912953-25-4 - Calbiochem

别名:

KSP Inhibitor VII; 6-(4-Trifluoromethyl)phenyl)-3,4-dihydro-2(1H)-quinolinone, GSK-1

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assay

≥97% (HPLC)

form

powder

color

off-white

solubility

DMSO: 10 mg/mL

General description

A cell-permeable quinolinone compound that acts as a highly potent and selective Eg5/KSP inhibitor (Ki = 1.4, 2.1, 2.2, and 1.7 nM for the mutant A133D, KHC-L5, D130V, and the wild-type KSP, respectively) by antagonizing ATP binding via an allosteric site. Effectively induces monopolar spindles in ovarian adenocarcinoma SKOV3 cells and inhibits the proliferation of colorectal carcinoma HCT116 cells (IC50 = 36 and 0.5 nM againt the parental and the ispinesib-resistant D130V mutant line, respectively). It is uncompetitive with respect to microtubule and exhibits little activity against a panel of 7 other mitotic kinesins.
The Eg5 Inhibitor VII controls the biological activity of Eg5. This small molecule/inhibitor is primarily used for Cell Structure applications.

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.


存储类别

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

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Lusong Luo et al.
Nature chemical biology, 3(11), 722-726 (2007-10-09)
The mitotic kinesin KSP (kinesin spindle protein, or Eg5) has an essential role in centrosome separation and formation of the bipolar mitotic spindle. Its exclusive involvement in the mitotic spindle of proliferating cells presents an opportunity for developing new anticancer