Chemical Name:4-[4-(2,3-Dihydro-1,4-benzodioxin-6-yl)-5-methyl-1H-pyr
azol-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 tumour 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.
Cheunget al
(2005) The identification, synthesis, protein crystal structure and in vitro
biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors.
Bioorg.Med.Chem.Lett. 15 3338. Dymock et al (2005)
Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90
discovered through structure-based design. J.Med.Chem. 48 4212. Sharpet al (2007) In vitro biological characterization of a novel,
synthetic diaryl pyrazole resorcinol class of heat shock protein 90 inhibitors.
Cancer Res. 67 2206.
“I am grateful for your honesty and courtesy. The principles of Tocris are very different to that of your competitors who, in fact, have put our inhibitor on the market without any approval, exhibiting a pirate policy and a total absence of ethics..”
