Novel inhibitor of heat shock protein 90 (Hsp90) ATPase activity (IC50
= 5.7 μ
M) 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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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