CCT 018159

Cat. No. 2435

CCT 018159 C20H20N2O4 [171009-07-7]

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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.

Technical Data

Soluble to 5 mM in water and to 100 mM in DMSO
>98 %
Store at +4°C

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.

Certificate of Analysis / Safety Data Sheet

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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, Hsp90 Inhibitors

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