Eg5 Inhibitor VI - Calbiochem

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 (K_i = 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.

The Eg5 Inhibitor VI controls the biological activity of Eg5. This small molecule/inhibitor is primarily used for Cell Structure applications.

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