brd4 (2)

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

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].

BRD4 degrader-2 (Compound JP-2-197) is a covalent and monovalent molecule glue-type BRD4 degrader. It targets RNF126 (E3 ligase) to degrade both long and short isoforms of BRD4 in cells.

BRD4/FKBP12 degrader-2 (a1d) is a BRD4/FKBP12 degrader with anticancer activity.

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

BRD4 D1-IN-2 (compound 26) is a selective and potent inhibitor of BRD4 D1, exhibiting an IC50 value of less than 0.092 μM and a 15 nM affinity for BRD4 D1, with over 500-fold selectivity for BRD2 D1 and BRD4 D2.

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

PROTACFLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader targeting FLT3, JAK2, and BRD4, with DC50 values of 5.23 nM, 0.678 nM, and 1.17 nM, respectively. It exhibits potent antiproliferative activity against MV4;11 cells (IC50= 0.79 nM) and FLT3-mutated Ba/F3 cells. Additionally, PROTACFLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells and demonstrates significant antitumor efficacy in an MV4;11 xenograft model established in NOD SCID mice. This compound is applicable for research in acute myeloid leukemia (AML).

BRD4/CK2-IN-1 is a small molecule inhibitor targeting BRD4 and CK2, with an IC50 of 180nM for BRD4 and 230nM for CK2. It inhibits the proliferation of MDA-MB-231 and MDA-MB-468 cells, inducing apoptosis and autophagy-related cell death. It can be used in triple-negative breast cancer research.

CF53 is a highly potent, selective, and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM, and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, being very selective over non-BET bromodomain-containing proteins. CF53 exhibits potent anti-tumor activity both in vitro and in vivo.

ZEN-3411 is an orally available and potent BET inhibitor that inhibits BRD4(BD1), BRD4(BD2), and BRD4(BD1BD2) and suppresses the growth of tumor cells overproducing BET proteins.

(+)-JQ-1 (JQ1) is a specific, reversible BET bromine domain inhibitor that targets BRD4 (1/2) with IC50 values of 77/33 nM. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.

3-methyl-1,2,3,4-tetrahydroquinazolin-2-one is a inhibitor of BRD4 .

ZEN-3219 is a BET inhibitor, which has inhibitory effect on BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2). ZEN-3219 has inhibitory effect on BRD4(BD1), The IC50 values of BRD4(BD2) and BRD4(BD1BD2) were 0.48, 0.16 and 0.47 μM, respectively. ZEN-3219 is a component of PROTAC molecule and can induce BRD4 degradation.

BRD4-BD1-IN-2 is a selective and potent BRD4-BD1 inhibitor with an IC50 value of 2.51 µM, exhibiting 20-fold greater inhibitory activity against BRD4-BD1 compared to BRD4-BD2. [BRD4-BD1-IN-2] is applicable for research in cardiovascular and cancer-related diseases.

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

1-benzyl-2-ethyl-4,5,6,7-tetrahydro-1H-indol-4-one is an inhibitor Bromodomain-containing protein 4 (human).

CHEMBRDG-BB 7118966 is an inhibitor of Bromodomain-containing protein 4 (human).

BET-IN-2 is a BET inhibitor with an IC50 of 52 nM for BRD4-BD1.

MS645 is an inhibitor of bromodomain-containing protein 4 (BRD4) with a Ki of 18.4 nM for BRD4-BD1/BD2.

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

Lenalidomide-PEG1-azide is an E3 ligase ligand-linker complex comprising a cereblon ligand and linker, suitable for synthesising PROTACs and click chemistry reactions.

MS436 is a selective, small-molecule inhibitor for the BRD4 bromodomains.

(R)-(-)-JQ1 Enantiomer is the stereoisomer of (+)-JQ1, a BET bromodomain inhibitor, which acts on BRD4(1/2) with IC50 values of 77 nM and 33 nM in a cell-free assay.