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CCT 018159Cat. No. 2435 |
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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.Certificate of Analysis / Safety Data Sheet
References
Cheung et 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. PMID: 15955698.
Dymock et al (2005) Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design. J.Med.Chem. 48 4212. PMID: 15974572.
Sharp et al (2007) In vitro biological characterization of a novel, synthetic diaryl pyrazole resorcinol class of heat shock protein 90 inhibitors. Cancer Res. 67 2206. PMID: 17332351.
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Keywords: CCT 018159, supplier, Hsp90, inhibitors, Heat, Shock, Protein, 90, CCT018159
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