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Benzisoxazole Hsp90 inhibitor is an inhibitor of heat shock protein 90 (Hsp90; IC50 = 30 nM in a fluorescence polarization assay).1 It is selective for Hsp90 over a panel of kinases (IC50s = >20 µM). Benzisoxazole Hsp90 inhibitor inhibits the proliferation of HCT116, SK-BR-3, LNCaP, DU145, and H157 cancer cells (IC50s = 0.28, 0.37, 0.17, 0.29, and 0.23 µM, respectively). It also induces degradation of the Hsp90 targets HER2 and the androgen receptor in SK-BR-3 and LNCaP cells, respectively, with an IC50 value of 0.33 µM for both.
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1. Discovery of benzisoxazoles as potent inhibitors of chaperone heat shock protein 90. J. Med. Chem. 51, 373-375 (2008).