324631
Eg5 Inhibitor VII - CAS 912953-25-4 - Calbiochem
Synonym(s):
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.
Storage Class
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
新产品
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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