17-DMAG HCl (Alvespimycin), a watersoluble geldanamycin analog belonging to the class of benzoquinones, is a selective Hsp90 inhibitor. 17-DMAG HCl binds to the N-terminal domain ATP binding site of Hsp90, inhibiting Hsp90 chaperone activity. 17-DMAG HCl demonstrates greater potency and water solubility than other geldanamycin analogs such as 17-AAG (mean GI50 values are 53 and 123 nM for 17-DMAG HCl and 17-AAG respectively), while demonstrating anti-tumor activity and offering excellent oral bioavailability.
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