protac brd4 degrader 10

PROTAC BRD4 Degrader-10, also known as compound 8b, is a dual ligand-based PROTAC that combines ligands for von Hippel-Lindau and BRD4. To degrade the BRD4 protein in PC3 prostate cancer cells, PROTAC BRD4 Degrader-10 can be conjugated with STEAP1 and CLL1 antibodies, with respective DC 50 values of 1.3 nM and 18 nM.

QCA570 is an effective BET degrader based on PROTAC (IC50: 10 nM for BRD4 BD1 Protein).

PROTACBRD4-DCAF1 degrader-1 (I-907) is a PROTAC degrader targeting BRD4-DCAF1, exhibiting a DC50 range of 10~100 nM.

PROTAC BRD4 Degrader-45 (compound 2b) is a PROTAC degrader that targets BRD4. It demonstrates improved passive membrane permeability, stability in cell culture medium supplemented with 10% FBS, and higher intracellular concentration in cancer cells.

PROTAC BRD4 Degrader-44 (compound 2a) is a BRD4-targeted PROTAC degrader with passive membrane permeability. It remains stable for up to 6 hours in medium supplemented with 10% FBS. Additionally, PROTAC BRD4 Degrader-44 exhibits increased intracellular accumulation within 6 hours, indicating a reduction in efflux activity.

PROTAC BET Degrader-10 (WO2017007612A1, example 37) is a highly efficient and selective small molecule compound designed to degrade BET protein BRD4. PROTAC BET Degrader-10 functions by utilizing specific ligands that connect Cereblon and BRD4, with a DC 50 value of 49 nM.

XY-06-007, a potent and selective bump-and-hole (B&H) PROTAC BRD4 BD1 L94V degrader, exhibits a DC50, 6 h of 10 nM specifically against BRD4 BD1 L94V without degrading off-targets. It also demonstrates favorable pharmacokinetics for in vivo studies [1].