Eg5 Inhibitor VI

$200.00$650.00

Product Specification

  • Appearance
    :

    Off-white solid.

  • CAS Number
    :

    N/A

  • Cat.number
    :

    VD-OEIA-1019

  • Formula
    :

    C13H11F3N2O2S

  • MW
    :

    316.3

  • Purity
    :

    ≥97% by HPLC

  • Solubility
    :

    DMSO or EtOH.

  • Storage
    :

    +2°C to +8°C. Protect from light.

  • Synonyms
    :

    N-(4′-(Trifluoromethyl)-4-biphenyl)sulfamide, KSP Inhibitor VI

  • Size
    :

    25mg, 5mg

Product Variations

Product # Price Quantity  
VD-OEIA-1019-0005-5mg $200
VD-OEIA-1019-0025-25mg $650

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.

1.Parrish, C.A., et al. 2007. J. Med. Chem. 50, 4939.

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