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Geldanamycin

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Geldanamycin Basic information
Geldanamycin Chemical Properties
  • Melting point:255 °C
  • Boiling point:627.87°C (rough estimate)
  • Density 1.2443 (rough estimate)
  • refractive index 1.5800 (estimate)
  • Flash point:87℃
  • storage temp. −20°C
  • solubility DMSO: soluble
  • pka8.42±0.70(Predicted)
  • form powder
  • color yellow to orange
  • λmax305nm(MeOH)(lit.)
  • CAS DataBase Reference30562-34-6(CAS DataBase Reference)
Safety Information
MSDS
Geldanamycin Usage And Synthesis
  • Chemical PropertiesYellow to Orange Powder
  • UsesGeldanamycin is a potent antitumor antibiotic active at nanomolar concentration against 60 cell lines. It binds specifically to the heat shock protein Hsp90 and to its endoplasmic reticulum homologue GP96, and thus interferes with conformational maturation of proteins and the cellular stress response. In addition, it is a potent inhibitor of the nuclear hormone receptor family.
  • UsesGeldanamycin is benzoquinone ansamycin antibiotic isolated from Streptomyces hygroscopicus. It is a potent antitumour metabolite that acts by binding to the 90-kDa heat-shock protein (Hsp90) essential to maintain the conformation, stability, activity and cellular localisation of several key oncogenic proteins such as ERBB2, C-RAF, CDK4, AKT/PKB, steroid hormone receptors, mutant p53, HIF-1α, survivin and telomerase hTERT.
  • DefinitionChEBI: An ansamycin consisting of a 19-membered macrocyle incorporating a benzoquinone ring and a lactam functionality. It shows antimicrobial activity against many Gram-positive and some Gram-negative bacteria.
  • Biological ActivitySelectively inhibits heat shock protein 90 (Hsp90). Binds to the ATP site of Hsp90 (K d = 1.2 μ M) and inhibits its chaperone activity. Consequently inhibits activities of oncogenic kinases (e.g. src, Raf), p53 and steroid receptors.
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