Heat shock protein 90 -Hsp90) is a molecular chaperone that modulates intracellular signaling and protein folding, trafficking, and turnover. Inhibitors of Hsp90, such as geldanamycin, have shown promise as anti-tumor agents. CAY10607 binds the N-terminal domain of Hsp90, efficiently displacing geldanamycin from the ATP binding site -IC50 = 30 nM). In addition, CAY10607 inhibits the proliferation of several cancer cell lines -IC50 ~ 0.28 uM), promotes the degradation of the Hsp90 client proteins Her-2 and androgen receptor, and has no effect on a variety of kinases.
產(chǎn)品描述
Binds the N-terminal domain of Hsp90, efficiently displacing geldanamycin from the ATP binding site -IC50 = 30 nM); inhibits the proliferation of several cancer cell lines -IC50 ~ 0.28 uM), promotes the degradation of Hsp90 client proteins, and has no effect on a variety of kinases