protac er degrader 4

PROTAC ER Degrader-4 is a PROTAC degrader of the estrogen receptor (ER) with an IC50 of 0.8 nM.

PROTAC ERα Degrader-4, a highly potent and selective agent (K i: 5.08 μM), contains OBHSAs, a linker, and E3 ligase ligands. This compound demonstrates superb inhibitory effects and ERα degradation activity in both Tamoxifen-sensitive and -resistant ER+ breast cancer (BC) cells, as well as in ERα-mutated BC cells. Additionally, PROTAC ERα Degrader-4 can induce apoptosis, making it valuable for cancer research.

PROTAC ER Degrader-14 (compound 86) is a PROTAC-type estrogen receptor ERR degrader. It comprises an E3 ubiquitin ligase ligand (blue part) (S)-Deoxy-thalidomide, a PROTAC linker (black part) N-Boc-piperazine, and a target protein ligand (red part) ER ligand-6. The combination of the E3 ligase and linker forms tert-Butyl (S)-4-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)piperazine-1-carboxylate.

AZD9496 deacrylic acid phenol (AZD9496) represents a portion of the ligand that targets the protein for PROTAC ER Degrader-4 [1].