brd4

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.

JQ-1 (carboxylic acid) is a cell-permeable BRD4 inhibitor with IC50s of 77 nM for BRD4(1) and 33 nM for BRD4(2)

PROTAC BRD4 Ligand-3 serves as a ligand for target proteins in PROTACs (Ligands for Target Protein for PROTACs). It is utilized in the synthesis process.

PROTAC BRD4 Degrader-16 is a potent degrader of BRD4, with IC50 values of 34.58 nM for BRD4 (BD1) and 40.23 nM for BRD4 (BD2). It significantly reduces Cyclin B1 expression, impedes G2 M phase progression, and induces apoptosis in MV-4-11 cells [1].

PROTAC BRD4 Degrader-22 (Compd 44h) is a PROTAC-based degrader targeting BRD4, with a pDC50 of 9.2 in MOLT4 cells over 24 hours [1].

PROTAC BRD4 Ligand-2 Hydrochloride serves as a ligand targeting the BRD4 protein, specifically designed for use with PROTAC CFT-2718.

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 Degrader-27 is a selective PROTAC targeting BRD4, distinguished from BRD2 BRD3. This compound is composed of the E3 ubiquitinase ligand Thalidomide-4-OH, the PROTAC Linker γ-Aminobutyric acid, and the PROTAC target protein ligand PROTAC BRD4 ligand-3. The active control for this target protein ligand is Mivebresib, while the conjugate of the E3 ubiquitin ligase ligand and Linker is identified as Pomalidomide 4'-alkylC3-acid.

PROTAC BRD4 Degrader-14, a PROTAC (Proteolysis Targeting Chimera) linked by ligands to von Hippel-Lindau and BRD4, exhibits IC50 values of 1.8 nM and 1.7 nM for BRD4 BD1 and BD2, respectively. This compound effectively degrades the BRD4 protein in PC3 prostate cancer cells [1].

PROTAC BRD4 Degrader-12 (compound 9c) is a PROTAC that links von Hippel-Lindau and BRD4 ligands. When conjugated with STEAP1 and CLL1 antibodies, this compound effectively degrades BRD4 protein in PC3 prostate cancer cells, demonstrating potent activity with DC50 values of 0.39 nM and 0.24 nM, respectively [1].

PROTAC BRD4 Degrader-17 (compound 13i), a potent inhibitor, exhibits IC50 values of 29.54 nM (BRD4 (BD1)) and 3.82 nM (BRD4 (BD2)), effectively reducing Cyclin B1 expression linked with G2 M phase progression and significantly inducing apoptosis in MV-4-11 cells [1].

PROTAC BRD4 Degrader-28 (Compound 4) is a PROTAC degrader specifically targeting BRD4, and it holds potential for cancer research.

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-5-CO-PEG3-N3 (Compound 2) is a PROTAC-linker conjugate utilized in PAC, comprising the BRD4 degrader GNE-987 connected with a 3-PEG linker. This compound serves as a click chemistry reagent, featuring an Azide group capable of undergoing copper-catalyzed azide-alkyne cycloaddition reactions (CuAAc) with molecules containing an Alkyne group. Additionally, it can participate in strain-promoted alkyne-azide cycloaddition reactions (SPAAC) with molecules that possess DBCO or BCN groups.

PROTAC BRD4 Degrader-20 (compound 195) is a bifunctional degrader of BRD4 [1].

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.