KSP Inhibitor VI
N-(4′-(Trifluoromethyl)-4-biphenyl)sulfamide Off-white solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable biphenylsulfamide compound that acts as a potent, reversible, and ATP-competitive inhibitor of Eg5/KSP ATPase activity (IC50 = 18 nM) with reactivity against both wild-type and the D130V mutant (Ki = 6.2 nM and 7 nM, respectively) in cell-free assays. Due to a higher ATP binding affinity of the WT enzyme, the inhibitor exhibits a much weaker antiproliferative activity against WT-expressing cells in cultures (IC50 = 5.4 and 403 nM, using HCT116 D130V and HCT116, respectively) and its in vivo antitumor efficacy has only been demonstrated in HCT116 D130V xenografed mice, but not mice with WT KSP-bearing Colo205. Purity: ≥97% by HPLC. Ref.: Parrish, C.A., et al. 2007. J. Med. Chem. 50, 4939.
R: 22-36/38; S: 26-36-45 |
