brd-4

PROTAC BRD4 ligand-1, a component of Protac GNE-987, is a ligand for BRD4 and acts as an inhibitor of BET.

FKBP12 PROTAC dTAG-13 (dTAG-13) is a heterobifunctional degrader that targets FKBP12F36V with FKBP12F36V expressed in-frame with a protein of interest, and selectively degrades the BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to the E3 ubiquitin ligase CRBN.

Tz-Thalidomide is a tetrazine-modified Thalidomide (E3 ligase ligand) with some affinity for BRD4.

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.

BRD4 Ligand-Linker Conjugate 1 is a compound consisting of a ligand and a linker, specifically designed to bind to the target protein BRD4. This conjugate serves as a valuable tool for synthesizing PROTACs, molecules utilized for targeted protein degradation.

PROTAC BRD4 Degrader-15 is a chemical compound consisting of a PROteolysis TArgeting Chimera (PROTAC) linked to ligands specific to von Hippel-Lindau and BRD4. It exhibits an IC50 of 7.2 nM for BRD4 BD1 and 8.1 nM for BRD4 BD2 and demonstrates potent degradation activity against the BRD4 protein in PC3 prostate cancer cells.

PROTAC BRD4 Degrader-5 is a PROTAC that efficiently degrades BRD4 in HER2-positive and -negative breast cancer cell lines, and is formed by linking von Hippel-Lindau ligand to BRD4 ligand.

PROTAC BRD4 Degrader-2 is an efficacious degrader of PROTAC BRD4(BRD4 BD1,IC50 of 14.2 nM).

PROTAC BRD4 Degrader-3 is an efficacious degrader of PROTAC BRD4.

HBL-4 is a PROTAC targeting BRD.

PROTAC BRD4 degrader for PAC-1 (compound 5) is a chimeric BET degrader GNE-987 conjugated with a disulfide-containing linker[1]. This PROTAC-linker conjugate specifically targets and degrades BRD4, enabling selective proteolysis of PAC-1.

PROTAC BRD4 Degrader-1 is an efficacious degrader of BRD4(BRD4 BD1,IC50 of 41.8 nM).

PROTAC BRD4 Degrader-9 (compound 8a) is a novel chemical compound comprising ligands for von Hippel-Lindau and BRD4, connected by a PROTAC moiety. This compound efficiently degrades the BRD4 protein in PC3 prostate cancer cells. When conjugated with STEAP1 and CLL1 antibodies, PROTAC BRD4 Degrader-9 exhibits potent activity, with respective DC50 values of 0.86 nM and 7.6 nM.

PROTAC BRD4 Degrader-8 is a potent BRD4 inhibitor with IC50 values of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively, effectively degrading the BRD4 protein in PC3 prostate cancer cells[1].

PROTAC BRD4 ligand-2 is a ligand for the target BRD4 protein used in the development of PROTAC CFT-2718.

PROTAC BRD4 Degrader-13 (compound 9d) is a bioactive compound functioning as a proteolysis targeting chimera (PROTAC) by linking ligands for von Hippel-Lindau and BRD4 proteins. In PC3 prostate cancer cells, it effectively degrades the BRD4 protein through conjugation with STEAP1 and CLL1 antibodies, exhibiting a DC50 of 0.025 nM and 6.0 nM, respectively.

PROTAC BRD4-binding moiety 1 is a BRD4 ligand that binds to the cereblon ligand via a linker, facilitating the formation of a PROTAC complex which efficiently degrades BRD4[1].

BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.