56632-39-4

BHPI is an antagonist of estrogen receptor α (ERα) that blocks 17β-estradiol-induced proliferation of drug-resistant breast, endometrial, and ovarian cancer cell lines at concentrations ranging from 10 to 1,000 nM. It is effective in vivo, driving tumor regression in mice bearing MCF-7 xenografts at a dose of 15 mg/kg daily. BHPI specifically inhibits ERα-dependent gene expression and protein synthesis by activating the unfolded protein response in cells.

BHPI is an antagonist of estrogen receptor α (ERα) that blocks 17β-estradiol-induced proliferation of drug-resistant breast, endometrial and ovarian cancer cell lines.

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[1] NEAL D ANDRUSKA. Estrogen receptor α inhibitor activates the unfolded protein response, blocks protein synthesis, and induces tumor regression.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2015, 112 15: 4737-4742. DOI: 10.1073/pnas.1403685112