17-AAG
Chemical Name: 17-Demethoxy-17-(2-propenylamino)geldanamycin
Purity: ≥98%
Biological Activity
17-AAG is an inhibitor of heat shock protein 90 (Hsp90) chaperone activity, and an analog of geldanamycin (Cat. No. 1368). Subsequently inhibits the activity of oncogenic proteins such as p185erbB-2 (IC50 = 31 nM), N-ras, Ki-ras and c-Akt. Antitumor in vivo. Also protects neuroprogenitor cells against stress-induced apoptosis at low concentrations (10 nM) in vitro.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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The hsp70 inhibitor VER155008 induces paraptosis requiring de novo protein synthesis in anaplastic thyroid carcinoma cells.
Kim S, Kang J, Kim C, Ihm S, Choi M, Yoo H, Lee S
Biochem Biophys Res Commun, 2014;454(1):36-41. -
Heat shock protein 90 (Hsp90) promotes opioid-induced anti-nociception by an ERK Mitogen Activated Protein Kinase (MAPK) mechanism in mouse brain
W Lei, N Mullen, S McCarthy, C Brann, P Richard, J Cormier, K Edwards, EJ Bilsky, JM Streicher
J. Biol. Chem., 2017;0(0):. -
Protection of murine neural progenitor cells by the Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin in the low nanomolar concentration range.
Wang et al.
J.Neurochem., 2011;117:703 -
Inhibition of signal transduction by the Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin results in cytostasis and apoptosis.
Hostein et al.
Cancer Res., 2001;61:4003 -
Inhibition of the oncogene product p185erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives.
Schnur et al.
J.Med.Chem., 1995;38:3806 -
Disruption of the EF-2 kinase/Hsp90 protein complex: a possible mechanism to inhibit glioblastoma by geldanamycin.
Yang et al.
Cancer Res., 2001;61:4010
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Citations for 17-AAG
The citations listed below are publications that use Tocris products. Selected citations for 17-AAG include:
6 Citations: Showing 1 - 6
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Heat Shock Protein 90 as a Prognostic Marker and Therapeutic Target for Adrenocortical Carcinoma.
Authors: Siebert Et al.
Front Endocrinol (Lausanne) 2019;10:487
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Hsp90 regulation of fibroblast activation in pulmonary fibrosis.
Authors: Sontake Et al.
JCI Insight 2017;2:e91454
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Quantitative proteomics of the yeast Hsp70/Hsp90 interactomes during DNA damage reveal chaperone-dependent regulation of ribonucleotide reductase.
Authors: Truman Et al.
J Proteomics 2015;112:285
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HSP90 regulates DNA repair via the interaction between XRCC1 and DNA polymerase β.
Authors: Fang Et al.
Nat Commun 2014;5:5513
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HSF1 deficiency and impaired HSP90-dependent protein folding are hallmarks of aneuploid human cells.
Authors: Donnelly Et al.
EMBO J 2014;33:2374
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Pertuzumab Increases 17-AAG-Induced Degradation of ErbB2, and This Effect Is Further Increased by Combining Pertuzumab with trastu.
Authors: Hughes Et al.
Pharmaceuticals (Basel) 2012;5:674
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