35446-HCl

35446-HCl (also known as NSC35446.HCl) is a second-generation small molecule BRCA1 mimetic and estrogen receptor-alpha (ERα) antagonist developed by Georgetown University. It is designed to fit into a predicted BRCA1-binding cavity within ERα, mimicking the ability of BRCA1 to repress ERα activity. By disrupting the interaction of ERα with estrogen response elements (EREs), 35446-HCl inhibits ERα-dependent gene transcription, including the expression of the NF-κB activator IKKβ (IKKB). This downregulates NF-κB signaling and downstream anti-apoptotic genes, inducing apoptosis in antiestrogen-resistant breast cancer cells. 35446-HCl has demonstrated preclinical efficacy in inhibiting the growth of tamoxifen- and fulvestrant-resistant breast cancer cell lines and tumor xenografts.

Other names

35446 hydrochlorideBRCA1 mimetic 35446BRCA-1 mimetic 35446BRCA 1 mimetic 35446BRCA1 mimetic 35446-HClBRCA-1 mimetic 35446-HClBRCA 1 mimetic 35446-HClBRCA1-mimetic compound NSC35446.HClBRCA-1-mimetic compound NSC35446.HClBRCA 1-mimetic compound NSC35446.HCl