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-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-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.

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

FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional compound that selectively degrades the BET bromodomain transcriptional co-activator BRD4 by linking BET bromodomains to the E3 ubiquitin ligase CRBN. It also functions as a degrader of FKBP12F36V when FKBP12F36V is expressed in-frame with a targeted protein.

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.

PROTAC BRD9 Degrader-1 is a leading PROTAC BRD9 chemical degrader with an IC50 of 13.5 nM.

I-BET762 carboxylic acid is an inhibitor of BRD4(pIC50 of 5.1).

TD-428 is a highly specific degrader of BRD4(DC50 of 0.32 nM). TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation.

Azido-PEG1-CH2CO2H, a PROTAC linker characterized by an alkyl/ether combination, can be utilized to synthesize PROTAC BRD4 Degrader-1[1].

SNIPER(BRD)-1 is a chemical compound composed of a derivative of the IAP antagonist LCL-161 and the BET inhibitor (+)-JQ-1, linked together. It promotes the degradation of BRD4 through the ubiquitin-proteasome pathway and effectively degrades cIAP1, cIAP2, and XIAP with IC50 values of 6.8 nM, 17 nM, and 49nM, respectively[1].

ZXH-3-26 is a PROTAC composed of a Cereblon ligand, an E3 ubiquitin ligase, and a BRD4 ligand that can be used to study cancer.

KB02-JQ1 is a potent and specific proteolysis targeting chimera (PROTAC) that specifically degrades BRD4, acting as a molecular glue. It does not degrade BRD2 or BRD3. The mechanism of action involves covalent modification of the E3 ligase DCAF16, thereby promoting BRD4 degradation. Importantly, KB02-JQ1 demonstrates enhanced stability and durability in facilitating protein degradation within biological systems. The compound forms a complex with the ubiquitin E3 ligase ligand KB02 through a linker, resulting in the formation of KB02-JQ1[1].

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.

A1874 is a nutlin-based and BRD4-degrading PROTAC which induces BRD4 degradation in cells. Effective in inhibiting many cancer cell lines proliferation.

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 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.