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.
|Storage||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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 352.39. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.84 mL||14.19 mL||28.38 mL|
|5 mM||0.57 mL||2.84 mL||5.68 mL|
|10 mM||0.28 mL||1.42 mL||2.84 mL|
|50 mM||0.06 mL||0.28 mL||0.57 mL|
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for CCT 018159, please let us know.
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Keywords: CCT 018159, CCT 018159 supplier, Hsp90, inhibitors, inhibits, Heat, Shock, Protein, 90, CCT018159, 2435, Tocris Bioscience
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Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.