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).

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.

GNE-781 is a highly potent and selective inhibitor of CBP (IC50: 0.94 nM in TR-FRET assay). GNE-781 also inhibits BRET and BRD4(1) (IC50s: 6.2 nM and 5100 nM, respectively).

(+)-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).

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

OXF BD 02 is a potent and selective BRD4(1) inhibitor (IC50: 382 nM) with anticancer and anti-inflammatory activity.

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

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.

GNE-207 is a selective and orally bioavailable inhibitor of the bromodomain of CBP (IC50: 1 nM). It has a selective index of >2500-fold against BRD4 (1). GNE-207 displays excellent CBP potency (EC50: 18 nM for MYC expression in MV-4-11 cells).

PROTAC BRD4 ligand-1 is a PROTAC and a BRD4-targeted inhibitor with BET inhibitory activity. This ligand is cell-permeable and is used for the synthesis of PROTAC GNE-987, possessing antitumor potential.

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 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.

BRD4 degrader-1 (Compound ML 1-50) is a monovalent and covalent molecular glue-type degrader targeting BRD4. It specifically directs the degradation of BRD4 long and short isoforms in cells by targeting DCAF16 (E3 ligase).

BRD4/NAMPT-IN-1 (Compound A2) exhibits strong inhibitory effects on NAMPT and BRD4, with IC50 values of 35 nM (NAMPT) and 58 nM (BRD4). This compound significantly suppresses the growth and migration of liver cancer cells while promoting apoptosis. Additionally, BRD4/NAMPT-IN-1 demonstrates potent anticancer activity in HCCLM3 xenograft mouse models without noticeable toxicity.

BRD4/FKBP12 degrader-1 (a1d) is an anticancer agent that functions as a BRD4/FKBP12 degrader.

AR/BRD4 RIPTAC-1 (Compound II-5) is an orally active Regulatory-inducible proximity-targeting chimera (RIPTAC). AR/BRD4 RIPTAC-1 induces the formation of a stable ternary complex between the androgen receptor (AR) and BRD4, thereby blocking BRD4 function. AR/BRD4 RIPTAC-1 inhibits the growth and proliferation of tumor cells. AR/BRD4 RIPTAC-1 holds promise for use in prostate cancer research. AR/BRD4 RIPTAC-1 is additionally applicable in molecular oncology research for investigating androgen receptor–epigenetic regulator interactions and for studying proximity-induced protein complex formation mechanisms in tumor-associated transcriptional regulation systems.

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).

FLT3/JAK2/BRD4 ligand-1 is a ligand for FLT3, JAK2, and BRD4. It serves as a component for synthesizing PROTAC [FLT3/JAK2/BRD4 Degrader-1].

PROTACBRD4 ligand-1-NH-PEG-phenol-PEG-COOtBu is a Target Protein Ligand-Linker Conjugate that comprises a BRD4 ligand and a PROTAC linker. This compound is utilized in the synthesis of PROTACBRD4 Degrader-14.

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/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.

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.