Geldanamycin
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- Application
- Inhibition (Inh)
- 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
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- Comment
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Source: Produced by fermentation.
Appearance: Yellow Solid - Restrictions
- For Research Use only
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- 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
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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).
: "Hsp90 inhibitor induces autophagy and apoptosis in osteosarcoma cells." in: International journal of oncology, Vol. 46, Issue 1, pp. 47-54, (2014) (PubMed).
: "
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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).
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- Molecular Weight
- 560.6
- CAS-No
- 30562-34-6
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