Chemical Name: 4-[4-(2,3-Dihydro-1,4-benzodioxin-6-yl)-5-methyl-1H-pyrazol-3-yl]-6-ethyl-1,3-benzenediol
Biological ActivityNovel 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors.
Cheung et al.
Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design.
Dymock et al.
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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