324629
Eg5 Inhibitor VI - Calbiochem
Synonym(s):
N-(4ʹ-(Trifluoromethyl)-4-biphenyl)sulfamide, KSP Inhibitor VI
Assay
≥97% (HPLC)
form
solid
color
off-white
solubility
ethanol: 15 mg/mL
DMSO: 20 mg/mL
General description
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.
The Eg5 Inhibitor VI 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.
Regulatory Information
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Cynthia A Parrish et al.
Journal of medicinal chemistry, 50(20), 4939-4952 (2007-08-30)
Kinesin spindle protein (KSP), an ATPase responsible for spindle pole separation during mitosis that is present only in proliferating cells, has become a novel and attractive anticancer target with potential for reduced side effects compared to currently available therapies. We
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