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Geldanamycin Inhibitor

InhA 30562-34-6 (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-13-hydroxy-8,14,19-trimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1] docosa-1(21),4,6,10,18-pentaen-9-yl carbamate
Pubmed (2)
Catalog No. ABIN1027731
$156.00
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1 mg ABIN1027731
1 mg ABIN1027731
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  • Application
    Inhibition Assay (InhA)
    Purpose
    Hsp90 inhibitor
    Specificity
    Geldanamycin is a benzoquinoid ansamycin produced by Streptomyces hygroscopicus. It binds specifically to heat shock protein HSP90 and downregulates target proteins including tyrosine kinases, steroid receptors, transcription factors and cell cycle regulatory kinases. It induces the inactivation, destabilization and eventual degradation of HIF-1alpha. This is specifically a novel geldanamycin fluorescent probe that may be used in a fluorescence polarization assay for Hsp90 inhibitors. May also be used for detection of cell surface Hsp90. Other geldanamycin fluorophores (BODPY) have been reported and used in FP HTS assays.
    Characteristics
    Hsp90 inhibitor.
    Purification
    Produced by fermentation
    Purity
    >95 %
    Chemical Name
    (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-13-hydroxy-8,14,19-trimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1] docosa-1(21),4,6,10,18-pentaen-9-yl carbamate
    Formula
    C29H40N2O9
    Solubility
    Slightly soluble in methanol, chloroform or DMSO (10 mg/ml); insoluble in water
  • Comment

    Source: Produced by fermentation.
    Appearance: Yellow Solid

    Restrictions
    For Research Use only
  • Format
    Solid
    Precaution of Use
    Classification: Harmful. May be harmful if inhaled, swallowed or absorbed through skin. Safety Phrases: S22 - Do not breathe dust S24/25 - Avoid contact with skin and eyes S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection Risk Phrases: R68- Possible risk of irreversible effects
    Handling Advice
    Classification: Harmful. May be harmful if inhaled, swallowed or absorbed through skin. Safety Phrases: S22 - Do not breathe dust S24/25 - Avoid contact with skin and eyes S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection Risk Phrases: R68- Possible risk of irreversible effects
    Storage
    -20 °C
  • Cha, St Louis, Tradewell, Gentil, Minotti, Jaffer, Chen, Rubenstein, Durham: "A novel small molecule HSP90 inhibitor, NXD30001, differentially induces heat shock proteins in nervous tissue in culture and in vivo." in: Cell stress & chaperones, Vol. 19, Issue 3, pp. 421-35, 2014 (PubMed).

    Mori, Hitora, Nakamura, Yamagami, Horie, Nishimura, Yamamoto: "Hsp90 inhibitor induces autophagy and apoptosis in osteosarcoma cells." in: International journal of oncology, Vol. 46, Issue 1, pp. 47-54, 2014 (PubMed).

  • Molecular Weight
    560.6
    CAS-No
    30562-34-6
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