Heat Shock Protein Inhibitors

Geldanamycin & Analogs

Heat shock protein 90 (Hsp90) is a ubiquitous molecular chaperone critical for the folding, assembly and activity of multiple mutated and overexpressed signaling proteins that promote the growth and/or survival of tumor cells.

Hsp90 client proteins include mutated p53, Raf-1, Akt, ErbB2 and hypoxia-inducible factor 1a (HIF-1a).

Geldanamycin (GA), a benzoquinone ansamycin antibiotic, selectively inhibits Hsp90 leading to the degradation of its client proteins. GA inhibits the proliferation of cancer cells and shows anti-cancer activity in experimental animals.

However due to poor aqueous solubility and liver toxicity, GA has not moved forward in clinical trials. To overcome these undesirable properties, numerous GA analogs have been synthesized which differ only in their 17-substituent.

These include 17-allylamino-demethoxygeldamycin (17-AAG) and 17-dimethylamino- geldanamycin (17-DMAG) that have completed phase I and are currently entering phase II clinical trials.

InvivoGen provides Geldanamycin and four of its more promising analogs as well as other derivatives.

Bulk quantity readily available - contact us

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