17-DMAG(17-Dimethylamino-ethylamino-17-demethoxygeldanamycin) a watersoluble geldanamycin analog belonging to the class of benzoquinones ??is a selective Hsp90 inhibitor. Geldanamycin analogs such as 17-DMAG bind to the N-terminal domain ATP binding site of Hsp90, inhibiting Hsp90 chaperone activity. Hsp90 client proteins include kinases and several known oncogenes, making inhibition of Hsp90 an attractive chemotherapeutic strategy. Disruption of Hsp90 client protein folding leads to their ubiquitination and subsequent proteolytic degradation by the proteasome. 17-DMAG demonstrates greater potency and water solubility than other geldanamycin analogs such as 17-AAG, while demonstrating anti-tumor activity and offering excellent oral bioavailability.

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