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Geldanamycin (CAS 30562-34-6)

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Application:
Geldanamycin is an inhibitor of HSP 90 and nuclear hormone receptor family
CAS Number:
30562-34-6
Purity:
>95%
Molecular Weight:
560.64
Molecular Formula:
C29H40N2O9
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Geldanamycin, a benzoquinone ansamycin, has been found to revert tyrosine kinase-induced oncogenic transformation. In the same study it was reported that Geldanamycin was able to bind elements of Hsp90 (heat shock protein 90) clients, such as HIF-1alpha (Hypoxia-inducible factor-1-alpha), and inhibit them. Geldanamycin binds in a specific and stable manner and as a result inhibits new protein maturation. Geldanamycin binds with high affinity into the ATP binding pocket of Hsp90. These heat shock proteins might positively impact cell proliferation by being a chaperone required for the assembly and activation of telomerase in cells. By binding them, Geldanamycin is thought to reduce new protein maturation and their downstream transcriptional activity. Geldanamycin has also displayed a capacity to bind to the endoplasmic reticulum homologue of the heat-shock protein, GP-96 and thus interferes with the cellular stress response. In addition, Geldanamycin has been reported as a potent inhibitor of the nuclear hormone receptor family. Other research has demonstrated Geldanamycin to be a protective agent against alpha-synuclein toxicity to dopaminergic neurons in Drosophila. Geldanamycin is an inhibitor of c-Src.


Geldanamycin (CAS 30562-34-6) References

  1. Geldanamycin as a potential anti-cancer agent: its molecular target and biochemical activity.  |  Neckers, L., et al. 1999. Invest New Drugs. 17: 361-73. PMID: 10759403
  2. Geldanamycin induces degradation of hypoxia-inducible factor 1alpha protein via the proteosome pathway in prostate cancer cells.  |  Mabjeesh, NJ., et al. 2002. Cancer Res. 62: 2478-82. PMID: 11980636
  3. Hsp90 inhibitor geldanamycin and its derivatives as novel cancer chemotherapeutic agents.  |  Miyata, Y. 2005. Curr Pharm Des. 11: 1131-8. PMID: 15853661
  4. Geldanamycin, radicicol, and chimeric inhibitors of the Hsp90 N-terminal ATP binding site.  |  Hadden, MK., et al. 2006. Curr Top Med Chem. 6: 1173-82. PMID: 16842154
  5. Low dose geldanamycin inhibits hepatocyte growth factor and hypoxia-stimulated invasion of cancer cells.  |  Koga, F., et al. 2007. Cell Cycle. 6: 1393-402. PMID: 17525527
  6. Geldanamycin and its anti-cancer activities.  |  Fukuyo, Y., et al. 2010. Cancer Lett. 290: 24-35. PMID: 19850405
  7. Synthesis and biological evaluation of heat-shock protein 90 inhibitors: geldanamycin derivatives with broad antiviral activities.  |  Li, YP., et al. 2010. Antivir Chem Chemother. 20: 259-68. PMID: 20710066
  8. Geldanamycin and its derivatives as Hsp90 inhibitors.  |  Gorska, M., et al. 2012. Front Biosci (Landmark Ed). 17: 2269-77. PMID: 22652777
  9. HSP90 inhibitor geldanamycin reverts IL-13- and IL-17-induced airway goblet cell metaplasia.  |  Pezzulo, AA., et al. 2019. J Clin Invest. 129: 744-758. PMID: 30640172
  10. Exosomes Based Geldanamycin Delivery to Cancer Cells with Increased Therapeutic Efficacy.  |  Dhayapulay, A. and Kanapathipillai, M. 2019. J Biomed Nanotechnol. 15: 2202-2208. PMID: 31847934
  11. Geldanamycin-Induced Morphological Changes Require Candida albicans Hyphal Growth Regulatory Machinery.  |  Saville, SP. and Cleary, IA. 2021. Mycopathologia. 186: 103-107. PMID: 33389485
  12. Nigericin and Geldanamycin Are Phytotoxic Specialized Metabolites Produced by the Plant Pathogen Streptomyces sp. 11-1-2.  |  Díaz-Cruz, GA., et al. 2022. Microbiol Spectr. 10: e0231421. PMID: 35225656
  13. Geldanamycin Enhances the Radioprotective Effect of Peroxyredoxin 6 in Irradiated 3T3 Fibroblasts.  |  Novoselova, EG., et al. 2022. Dokl Biochem Biophys. 506: 202-205. PMID: 36303052
  14. Inhibition of heat shock protein HSP90-pp60v-src heteroprotein complex formation by benzoquinone ansamycins: essential role for stress proteins in oncogenic transformation.  |  Whitesell, L., et al. 1994. Proc Natl Acad Sci U S A. 91: 8324-8. PMID: 8078881

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Geldanamycin, 100 µg

sc-200617B
100 µg
$39.00

Geldanamycin, 500 µg

sc-200617C
500 µg
$59.00

Geldanamycin, 1 mg

sc-200617
1 mg
$104.00

Geldanamycin, 5 mg

sc-200617A
5 mg
$206.00