Catalog Number: 2435
Chemical Name: 4-[4-(2,3-Dihydro-1,4-benzodioxin-6-yl)-5-methyl-1H-pyrazol-3-yl]-6-ethyl-1,3-benzenediol
Biological Activity
Novel inhibitor of heat shock protein 90 (Hsp90) ATPase activity (IC50 = 5.7 μM) that displays selectivity over human Hsp72 and topoisomerase II. Inhibits proliferation of HCT116 human colon tumor cells and produces upregulation of Hsp70 and downregulation of c-Raf and cdk4. More soluble than 17-AAG (Cat. No. 1515) and is independent of NQO1/DT-diaphorase and P-glycoprotein expression.
Technical Data
  • M.Wt:
    352.39
  • Formula:
    C20H20N2O4
  • Solubility:
    Soluble to 5 mM in water and to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    171009-07-7
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors.
    Cheung et al.
    Bioorg.Med.Chem.Lett., 2005;15:3338
  2. Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design.
    Dymock et al.
    J.Med.Chem., 2005;48:4212
  3. In vitro biological characterization of a novel, synthetic diaryl pyrazole resorcinol class of heat shock protein 90 inhibitors.
    Sharp et al.
    Cancer Res., 2007;67:2206

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