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A cell-permeable biphenylsulfamide compound that acts as a potent, reversible, and ATP-competitive inhibitor of Eg5/KSP ATPase activity (IC50 = 18 nM). Has 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.
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Eg5 Inhibitor VI, 5 mg | sc-281686 | 5 mg | $398.00 |