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Stock availabilitIn Stock
In Stock
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CAS number
30562-34-6
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Description
Hsp90 inhibitor
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Molecular weight
560,6 g/mol
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Primary research fields
Cancer, Heat Shock
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Other 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
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Product category
Small Molecules
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Product type
Inhibitor
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Chemical formula
C29H40N2O9
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Origin
Produced by fermentation
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Purity pourcentage
>95%
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Soluble in
Slightly soluble in methanol, chloroform or DMSO (10 mg/ml); insoluble in water
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Physical appearance
Yellow Solid
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Storage recommendations
-20ºC
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Shipping recommendations
Shipped Ambient
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Safety information
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
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PubChem number
5288382
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Scientific context
Glendanamycin (GA), a benzoquinone ansamycin antibiotic, interferes with the action of Hsp90 leading to degradation of Hsp90 client proteins. GA itself however has undesirable properties such as poor aqueous solubility and liver toxicity; therefore, numerous analogs have been synthesized, such as 17-AAG(1). 17-AAG is an HSP-90 inhibitor that displays a 100-fold higher affinity for HSP-90 derived from tumor cells compared to HSP-90 from normal cells(2). 17-AAG inhibits Akt activation and expression in tumors and synergizes with a number of antitumor agents such as taxol(3), cisplatin(4) and UCN-01 (400 nM 17-AAG, U937 cells)(5). Looking for more information on HSP90? Visit our new HSP90 Scientific Resource Guide at more.
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Bibliography
1. Whitesell L., et al. (1994) Proc. Natl. Acad. Sci. USA 91:8324. 2. Neckers L. (2002) Trends Mol. Med. 8: S55. 3. Mabjeesh N.J., et al. (2002) Cancer Res. 62: 2478. 4. Chavany C., et al. 1996) Amer. Society Biochem Mol Bio. 9: 4974-4977. 5. Villa R., et al. (2003) Carcinogenesis. 24(5): 851-9. 6. Yamaki H., Iguchi-Ariga S.M., and Ariga H. (1989) J Antibiot (Tokyo). 42(4): 604-10.
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PubMed number
Refer to PubMed
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Tested applications
To be tested
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Tested reactivity
To be tested
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Representative figure legend
Chemical structure of Geldanamycin (SIH-111), a Hsp90 inhibitor. CAS #: 30562-34-6. Molecular Formula: C29H40N2O9. Molecular Weight: 560.6 g/mol. Chemical structure of Geldanamycin, a Hsp90 inhibitor (SIH-111). CAS # 30562-34-6. Molecular Formula: C29H40N2O9.
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Warning information
Non-hazardous
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Country of production
Canada
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Total weight kg
0.25
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Net weight g
0.001
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Additional description
Tissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.