2. シグナル伝達
  3. Epigenetics
  4. Epigenetic Reader Domain
  5. BRD4 Isoform

BRD4

BRD4 (Bromodomain Containing Protein 4) is a member of the BET (bromodomain and extra-terminal) protein family that recognizes acetylated histones and functions as a central regulator of chromatin-associated transcriptional programs[1][2]. Mechanistically, BRD4 promotes RNA polymerase II transcriptional elongation through functional interaction with positive transcription elongation factor b (P-TEFb), thereby facilitating productive gene expression and transcriptional pause release[3][4][5]. Beyond transcriptional control, BRD4 contributes to chromatin organization, DNA replication, and DNA damage response pathways, linking epigenetic regulation to genome stability[1][6]. BRD4 also supports efficient transcription elongation that limits R-loop accumulation and transcription-replication conflicts, processes that are important for maintaining cellular viability[6]. In disease contexts, aberrant BRD4 activity has been associated with cancer, inflammatory disorders, viral infection, and neurological disease, reflecting its broad influence on gene regulatory networks[1][7]. In multiple tumor models, BRD4 regulates transcriptional programs linked to oncogenic drivers and tumor cell survival, supporting its relevance as a therapeutic target[8][9]. Compared with related BET family members BRD2, BRD3, and the testis-restricted BRDT, BRD4 possesses a characteristic C-terminal domain that mediates interaction with P-TEFb and plays a distinct role in transcriptional elongation control[3][10]. For experimental applications, small-molecule BET inhibitors such as JQ1 and I-BET disrupt bromodomain-dependent chromatin interactions and have become widely used tools for investigating BRD4-dependent transcriptional mechanisms and target validation in disease models[1][8][9].

References:

BRD4 関連製品 (223):

製品番号 製品名 製品効果 純度
  • HY-13030
    (+)-JQ-1 Inhibitor 99.91%
    (+)-JQ-1 (JQ1), a chemical probe, is a potent, specific, CNS-penetrant and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy.
  • HY-100972
    ARV-771 Degrader 99.87%
    ARV-771 is a potent BET PROTAC based on E3 ligase von Hippel-Lindau with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively.
  • HY-101838
    dBET1 Inhibitor 99.24%
    dBET1 is a PROTAC connected by ligands for Cereblon and BRD4 with an EC50 of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to NSC 527179 (HY-14658) with a linker.
  • 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-12863
    Pelabresib Inhibitor 99.95%
    Pelabresib (CPI-0610) is a potent, selective, orally active and cell-active BET inhibitor. Pelabresib inhibits BRD4-BD1 with an IC50 of 39 nM, and with an EC50 value of 0.18 μM for MYC.
  • HY-181553A
    PROTAC BRD4 Degrader-45 Degrader
    PROTAC BRD4 Degrader-45 is a PROTAC degrader targeting BRD4, with a DC50 of 43 nM. PROTAC BRD4 Degrader-45 is applicable to studies on membrane-permeable PROTACs.
  • HY-181496
    (S)-JQ-35-Boc Ligand
    (S)-JQ-35-Boc is a BRD4 ligand. (S)-JQ-35-Boc can be used to synthesize BRD4 degrader RAJQ14 (HY-181495). RAJQ14 can be used for cancer research.
  • HY-183992
    CZL-149 Inhibitor
    CZL-149 is an orally active dual BET and p300/CBP bromodomains inhibitor with IC50s of 13 nM and 10.5 nM for BED4 BD1 and p300, respectively. CZL-149 reduces c-Myc and H3K27Ac levels. CZL-149 has good drug-like properties and metabolic characteristics, as well as good safety. CZL-149 can be used for the study of multiple myeloma.
  • HY-112090
    ABBV-744 Inhibitor 99.97%
    ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC50 values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with agent-like properties enable the investigation of its antitumor efficacy and tolerability.
  • HY-129937A
    GNE-987 Inhibitor 99.98%
    GNE-987 is a VHL-dependent BRD4 PROTAC degrader. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 can be used for the research of cancer.
  • HY-136570
    GSK778 Inhibitor 99.14%
    GSK778 (iBET-BD1), a chemical probe, is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models.
  • HY-122826
    ZXH-3-26 Inhibitor 99.53%
    ZXH-3-26 is a PROTAC connected by ligands for Cereblon and BRD4 with a DC50/5h of 5 nM. The DC50/5h refers to half-maximal degradation after 5 hours of treatment of ~ 5 nM.
  • HY-14443
    XMD8-92 Inhibitor 99.48%
    XMD8-92 is a potent ERK5 (BMK1)/BRD4 inhibitor with Kds of 80 and 190 nM, respectively. XMD8-92 inhibits DCAMKL2, PLK4 and TNK1 with Kds of 190, 600 and 890 nM, respectively. Anti-cancer activity.
  • HY-100482
    CPI-637 Inhibitor 99.94%
    CPI-637 is a selective and potent CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM, 0.051 μM and 11.0 μM for CBP, EP300 and BRD4 BD-1, respectively, and an EC50 of 0.3 μM for CBP.
  • HY-114305
    A1874 Inhibitor 99.77%
    A1874 is a nutlin-based (MDM2 ligand) and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation.
  • HY-123941
    FKBP12 PROTAC dTAG-7 Inhibitor 99.47%
    FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional PROTAC degrader. FKBP12 PROTAC dTAG-7 targets FKBP12F36V and BET BRD4. FKBP12 PROTAC dTAG-7 enables rapid and selective degradation of target proteins, and is suitable for cellular and in vivo studies to analyze protein functions and validate targets. (Pink: target protein ligand (HY-114420); Black: linker (HY-128844); Blue: CRBN Ligand (HY-103597); CRBN Ligand+linker: (HY-W722323))
  • HY-136571
    GSK046 Inhibitor 99.70%
    GSK046 (iBET-BD2), a chemical probe, is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins, with IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively. GSK046 has immunomodulatory activity.
  • HY-176521
    AR/BRD4 RIPTAC-1 Inhibitor 98.65%
    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.
  • HY-120028
    GNE-207 Inhibitor 99.94%
    GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells.
  • HY-107443
    I-BET762 carboxylic acid Inhibitor 99.55%
    I-BET762 carboxylic acid (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid (Molibresib carboxylic acid) is a BRD4 inhibitor with a pIC50 of 5.1.