Product Type: Inhibitor
CAS No.: 75747-14-7
MolecularFormula: C31H43N3O8
Molecular Weight: 585,7
Source: Synthetic
Purity: >99% (HPLC); NMR (Conforms)
Solubility: Soluble in DMSO (>50 mg/ml) or ethanol (5 mg/ml)
Appearance: Red to dark red powder
PubChem CID: 6505803
Scientific Background: 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). It has also been found that 17-AAG is alo an effective inducer fo the autophagic pathway by which alpha synuclein can be removed. It may provide a means to modulate autophagy in neural cells (6).
References: 1. Neckers L. (2002) Trends Mol Med. 84: S55-61.2. Kamal A., et al.(2003) Nature. 425: 407.3. Solit D.B., et al.(2003) Cancer Res. 63: 2139.4. Vasilevskaya I.A., et al. (2003) Mol.Pharmacol. 65: 235.5. Jia W., et al.(2003) Blood. 102: 1824. 6. Riedel M., Goldbaum O., Schwarz L., Schmitt S., Richter-Landsberg C. (2010) PLOS ONE. 5(1): e8753. https://doi.org/10.1371/journal.pone.0008755
Field of Use: Not for use in humans. Not for use in diagnostics or therapeutics. For in vitro research use only.
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