PROTAC AR Degrader-12

PROTACAR Degrader-12 is an effective PROTAC that targets the androgen receptor (AR) co-activator binding site (AR-CBS) . It induces AR degradation via the ubiquitin-proteasome system (UPS) pathway, inhibiting tumor cell growth by affecting DNA replication and cell division. Besides effectively degrading AR, it strongly inhibits the proliferation of MCF-7 cells and various mutant or drug-resistant breast cancer cells. PROTACAR Degrader-12 blocks the estrogen receptor α (ERα) signaling pathway through dual mechanisms of ERα protein downregulation and transcriptional activity inhibition, significantly suppressing mRNA expression of FOXA1, GREB1, SRC, and PELP1. It is applicable in breast cancer research.