brd4 (1)

PNZ5, an isoxazole-based pan-BET inhibitor, demonstrates potent activity and high selectivity comparable to the established (+)-JQ1, exhibiting a dissociation constant (KD) of 5.43 nM for BRD4(1).

(+)-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.

Y06036, a potent and selective BET inhibitor, can bind to the BRD4(1) bromodomain (Kd: 82 nM).

ZEN-2759 is a potent BET small molecule inhibitor of BRD4 (BD1), BRD4 (BD2), and BRD4 (BD1BD2).

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-1 is an efficacious degrader of BRD4(BRD4 BD1,IC50 of 41.8 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].

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.

HDAC3 BRD4-IN-1 (compound 26n) is an inhibitor of HDAC3 BRD4, exhibiting an IC50 of 8 nM for HDAC3, while its IC50 values for HDAC1 and HDAC2 are 220 nM and 120 nM, respectively. It displays anti-tumor and anti-proliferative effects by upregulating Ac-H3 and downregulating c-Myc. The half-life of HDAC3 BRD4-IN-1 in human liver microsomes is 29.36 minutes.

CDK4/6/BRD4-IN-1 (B15) is an inhibitor targeting CDK4, CDK6, and BRD4, with IC50 values of 220 nM for BRD4-BD2, 146 nM for BRD4-BD1, 106 nM for CDK6, and 85 nM for CDK4. This compound is applicable for research in non-small cell lung cancer (NSCLC) and can induce cell cycle arrest and apoptosis.

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.

BRD4-BD1 2-IN-1 is a highly effective inhibitor of BRD4, targeting the BRD4 BD-1 and BD-2 domains with IC50 values of <100 nM each (US20150148375A1, compound 5) [1].

BRD4-BD1-IN-1 (Compound 9a) is a BRD4-BD1 inhibitor with an IC50 of 38.20 μM.

PARP1 BRD4-IN-1 is a highly selective and potent inhibitor of PARP1 (IC50: 49 nM) and BRD4 (IC50: 202 nM), which inhibits the expression and activity of PARP1 and BRD4, thereby synergistically suppressing the malignant growth of pancreatic cancer cells.

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.

PLK1 BRD4-IN-1 (9b) is an orally active dual inhibitor of PLK1 (IC50: 22 nM) and BRD4 (IC50: 109 nM) that demonstrates significant anti-tumor efficacy in vivo.

BRD4 D1-IN-1 is a selective inhibitor of BRD4 D1 with an IC50 <0.092 μM, an affinity of 18 nM, and over 500-fold selectivity for BRD4 D1 and BRD4 D2.

HDAC JAK BRD4-IN-1 (compound 25ap) is a potent triple inhibitor targeting HDAC, JAK, and BRD4. This compound not only inhibits cell proliferation but also induces apoptosis in MDA-MB-231 cells and demonstrates in vivo anticancer efficacy [1].

GNE-049 is a highly selective and potent inhibitor designed to target the CREB-binding protein (CBP) with high affinity, exhibiting an IC50 of 1.1 nM for the suppression of BRET and BRD4 activity, which consequently blocks prostate cancer cell proliferation in both in vitro and in vivo models.

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.

Y06137 is an effective and selective BET inhibitor with a Kd of 81 nM for BRD4(1) bromodomain. Y06137 can be used for research on the treatment of castration-resistant prostate cancer.

CeMMEC1 is an inhibitor of BRD4, and also has a great affinity for TAF1(IC50=0.9 μM).