Cat. No. 1368
Chemical Name: 9,13-Dihydroxy-8,14,19-trimethoxy-4
Biological ActivitySelectively inhibits heat shock protein 90 (Hsp90). Binds to the ATP site of Hsp90 (Kd = 1.2 μM) and inhibits its chaperone activity. Consequently inhibits activities of oncogenic kinases (e.g. src, Raf), p53 and steroid receptors. Demonstrates antiproliferative effect on breast cancer stem-like cells.
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 / Product Datasheet / Safety Datasheet
Lee et al (2012) Inhibition of heat shock protein (Hsp) 27 potentiates the suppressive effect of Hsp90 inhibitors in targeting breast cancer stem-like cells. Biochimie. 94 1382. PMID: 22445681.
Roe et al (1999) Structural basis for inhibition of the Hsp90 molecular chaperone by the antitumor antibiotics radicicol and geldanomycin. J.Med.Chem. 42 260. PMID: 9925731.
Cardenas et al (1998) Signal-transduction cascades as targets for therapeutic intervention by natural products. Trends Biotechnol. 16 427. PMID: 9807840.
Whitesell et al (1994) Inhibition of heat shock protein HSP90-pp60v-src heteroprotein complex formation by benzoquinone ansamycins: essential role for stress proteins in oncogenic transformation. Proc.Natl.Acad.Sci.U.S.A. 91 8324. PMID: 8078881.
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Citations are publications that use Tocris products. Selected citations for Geldanamycin include:
Chung-Davidson et al (2015) Hsp90 and hepatobiliary transformation during sea lamprey metamorphosis. Nucleic Acids Res 15 47. PMID: 26627605.
Young et al (2015) A novel mechanism of autophagic cell death in dystrophic muscle regulated by P2RX7 receptor large-pore formation and HSP90. BMC Dev Biol 11 113. PMID: 25700737.
Barker et al (2006) Inhibition of Hsp90 acts synergistically with topoisomerase II poisons to increase the apoptotic killing of cells due to an increase in topoisomerase II mediated DNA damage. Neuroscience 34 1148. PMID: 16504968.
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Keywords: Geldanamycin, supplier, Selective, Hsp90, inhibitors, inhibits, Heat, Shock, Protein, 90, antibiotics, Tocris Bioscience, Hsp90 Inhibitor products