17-DMAG/

生物活性

17-DMAG, a watersoluble geldanamycin analog belonging to the class of benzoquinones, is a selective Hsp90 inhibitor. 17-DMAG binds to the N-terminal domain ATP binding site of Hsp90, inhibiting Hsp90 chaperone activity. 17-DMAG 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 and 17-AAG respectively), while demonstrating anti-tumor activity and offering excellent oral bioavailability. [1]

参考文献

[1] Smith V et al. Cancer Chemother Pharmacol. 2005 Aug;56(2):126-37