brd4

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

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.

BETd-260, a PROTAC linked by a Cereblon ligand and a BET ligand, has an inhibitory effect on BRD4 protein in leukemic cell lines.

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

FKBP12 PROTAC dTAG-13 is a PROTAC and selective degrader that can be used for target validation during drug discovery by splicing FKBP12 F36V with CRBN and thereby degrading FKBP12 F36V.

ARV-825, a heterobifunctional PROTAC (Proteolysis Targeting Chimera) that recruits BRD4 to the E3 ubiquitin ligase cereblon leading to fast, efficient, and prolonged degradation of BRD4 in all BL cell lines tested.

MZ 1 is a BRD4 protein degrader based on PROTAC technology.

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

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.

PROTAC BRD2 BRD4 degrader-1 (compound 15) is a potent, selective degrader of BET proteins BRD4 and BRD2, achieving rapid, reversible, and unexpectedly selective elimination compared to BRD3. It effectively suppresses solid tumors with minimal cytotoxic effects and comprises a BET inhibitor, a connecting linker, and thalidomide as the ligand for cereblon (CRBN) cullin 4A[1].

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].

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.

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

PROTAC BRD4 Degrader-29 (compound 7a) is a potent BRD4 PROTAC degrader with a DC50 of 89.4 nM, playing a significant role in cancer research.

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

PROTACBRD4 degrader-30 is an ISOX-DUAL-based PROTAC degrader, targeting BRD4 with an IC50 value of 65 nM. It is used in research studies related to c-Myc oncoproteins and the pathophysiology of cancer cells.

BRD4 ligand 6 is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). It serves as a key component in synthesizing the PROTAC CBP/BRD4 degrader-1.

BRD4 degrader-6 is a dimeric BDR4PROTAC class degrader with a DC50 of less than 0.1 μM. It effectively induces the ubiquitination and degradation of BDR4, exhibiting anticancer properties.

PROTACBRD4 Degrader-32 (Compound 22) is a potent BRD4 PROTAC degrader with a DC50 of 0.20 nM. It employs a unique carbon-carbon linker to connect the BRD4 binding domain with the CRBN binding domain, forming a ternary complex that induces BRD4 ubiquitination and facilitates proteasomal degradation. PROTACBRD4 Degrader-32 holds promise for research into BRD4-related cancers, such as hematological malignancies.

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.

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.