Chemical Name: 9,13-Dihydroxy-8,14,19-trimethoxy-4,10,12,16-tetramethyl-2-azabicyclo[16.3.1]docosa-4,6,10,18,21-pentaene-3,20,22-trione, 9-carbamate
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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Inhibition of heat shock protein (Hsp) 27 potentiates the suppressive effect of Hsp90 inhibitors in targeting breast cancer stem-like cells.
Lee et al.
Signal-transduction cascades as targets for therapeutic intervention by natural products.
Cardenas et al.
Trends Biotechnol., 1998;16:427
Structural basis for inhibition of the Hsp90 molecular chaperone by the antitumor antibiotics radicicol and geldanomycin.
Roe et al.
Inhibition of heat shock protein HSP90-pp60v-src heteroprotein complex formation by benzoquinone ansamycins: essential role for stress proteins in oncogenic transformation.
Whitesell et al.
Citations for Geldanamycin
The citations listed below are publications that use Tocris products. Selected citations for Geldanamycin include:
5 Citations: Showing 1 - 5
NudCL2 is an Hsp90 cochaperone to regulate sister chromatid cohesion by stabilizing cohesin subunits.
Authors: Yang Et al.
Cell Mol Life Sci 2018;
P2X7 receptor antagonism prevents IL-1β release from salivary epithelial cells and reduces inflammation in a mouse model of autoimmune exocrinopathy.
Authors: Khalafalla Et al.
J Biol Chem 2017;292:16626
Hsp90 and hepatobiliary transformation during sea lamprey metamorphosis.
Authors: Chung-Davidson Et al.
Nucleic Acids Res 2015;15:47
A novel mechanism of autophagic cell death in dystrophic muscle regulated by P2RX7 receptor large-pore formation and HSP90.
Authors: Young Et al.
BMC Dev Biol 2015;11:113
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.
Authors: Barker Et al.
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Geldanamycin was used in resistance experiments. We investigated the Hsp90 family protein (HtpG) of the organism that makes GdA, S. hygroscopicus.