GSK-1
KSP Inhibitor VII; 6-(4-Trifluoromethyl)phenyl)-3,4-dihydro-2(1H)-quinolinone Off-white powder. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. 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. Purity: ≥97% by HPLC. Ref.: Luo, L., et al. 2007. Nat. Chem. Biol. 3, 722. |
