2. Signaling Pathways
  3. Epigenetics
  4. Epigenetic Reader Domain
  5. BET Isoform

BET

BET (bromodomain and extraterminal domain) proteins are epigenetic reader proteins that recognize acetylated lysine residues through tandem bromodomains and recruit transcriptional regulatory complexes to chromatin, thereby controlling transcriptional activation and elongation programs[1][2]. BET family members, including BRD2, BRD3, BRD4, and BRDT, regulate RNA polymerase II-dependent gene expression and are important mediators of enhancer-associated transcriptional networks[1][3]. Mechanistically, BRD4 functions as a central transcriptional co-regulator by binding acetylated histones and facilitating recruitment of positive transcription elongation factor b (P-TEFb), which promotes productive transcriptional elongation[2][4]. Dysregulation of BET-dependent transcription has been implicated in cancer, inflammatory disorders, immune-mediated diseases, and viral infection models, where BRD4 contributes to disease-associated gene expression programs[1][3][5]. Compared with related BET isoforms, BRD4 is the most extensively characterized member and is distinguished by its prominent role in enhancer-driven transcription and broad involvement in oncogenic signaling pathways[3][6]. For experimental applications, BET bromodomains are highly druggable targets, and small-molecule inhibitors such as JQ1 as well as domain-selective BD1- or BD2-targeting compounds have been widely used to interrogate transcriptional regulation and evaluate therapeutic mechanisms in disease models[4][7][8]. These pharmacological tools have established BET proteins as key regulators of chromatin-dependent gene expression and valuable targets for mechanistic and translational research[5][7].

BET Related Products (11):

Cat. No. Product Name Effect Purity
  • HY-112588
    dBET6
    		Degrader 99.92%
    dBET6 is a highly potent, selective and cell-permeable PROTAC connected by ligands for Cereblon and BET, with an IC50 of 14 nM, and has antitumor activity.
  • HY-78695
    JQ-1 carboxylic acid
    		Inhibitor 99.69%
    JQ-1 carboxylic acid, a (+)-JQ-1 (HY-13030) derivative, is a potent BET bromodomain inhibitor. JQ-1 carboxylic acid can be used to synthesize PROTAC, which can target the degradation of BRD4.
  • HY-112429
    HJB97
    		Inhibitor 98.05%
    HJB97 is a high-affinity BET inhibitor with Ki values of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), and 1.0 nM (BRD4 BD2). HJB97 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC BET degraders with antitumor activity. HJB97 can be used for the synthesis of BETd-260 (HY-101519).
  • HY-145125
    SJ995973
    		Degrader 98.88%
    SJ995973 (PROTAC) is a uniquely potent degrader of bromodomain and extra-terminal (BET) proteins.
  • HY-185459
    PCIP-1
    PCIP-1 is a PARP2 inhibitor. PCIP-1 recruits BET proteins to PARP2 to inhibit DNA repair, acts via event-driven pharmacology, and does not inhibit PARP-catalyzed PARylation. PCIP-1 inhibits DNA repair, thereby inducing synthetic lethality in homologous recombination-deficient cancer cells and increasing the sensitivity of PARP1-knockout cells. PCIP-1 can be used in the research of homologous recombination-deficient cancers, T-cell acute lymphoblastic leukemia, and BRCA-mutant cancers.
  • HY-181003
    GSK785
    		Inhibitor
    GSK785 is a BRD2/4-selective, BRD3-sparing bivalent BET inhibitor. GSK785 inhibits production of the MCP1 cytokine in human whole blood. GSK785 can be used for the research of cancer.
  • HY-182036
    KWZL-7f15
    		Inhibitor
    KWZL-7f15 is a dual CDK6/BRD4 inhibitor with an IC50 of 31.81 nM against human CDK6. KWZL-7f15 inhibits the CDK6-RB axis and BRD4-Myc axis, and also acts as a pan-BET inhibitor. KWZL-7f15 exhibits antiproliferative activity against triple-negative breast cancer cells. KWZL-7f15 shows antitumor activity in xenograft mouse models. KWZL-7f15 can be used in studies related to triple-negative breast cancer.
  • HY-169980
    Mivebresib-alkyne
    		Control
    Mivebresib-alkyne (Compound 25), a Mivebresib (HY-100015) derivative, can be used for BRD4 targeted PROTAC synthesis through click reaction.
  • HY-122703
    BETi-211
    		Inhibitor
    BETi-211 is an orally active BET inhibitor (Ki: <1 nM). BETi-211 inhibits growth of triple-negative breast cancers (TNBC) cell lines with IC50 < 1 μM. BETi-211 degrades BET proteins and suppress tumor growth in xenograft breast tumors.
  • HY-177244
    EBET-1593
    		Degrader
    EBET-1593 is a BET PROTAC degrader. EBET-1593 can promote the ubiquitination and degradation of BET. EBET-1593 is a lead payload. EBET-1593 can be used to synthesize ADCs, such as 84-EBET. 84-EBET has antitumor effects against pancreatic ductal adenocarcinoma.
  • HY-161387
    EBET-590
    		Inhibitor
    EBET-590 is a BET inhibitor, and can be used for cancer research