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][2]. In multiple tumor models, BRD4 regulates transcriptional programs linked to oncogenic drivers and tumor cell survival, supporting its relevance as a therapeutic target[7][8]. 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][9]. 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][7][8].
References:
- [1]. Cheung KL, et al. The Functions of BET Proteins in Gene Transcription of Biology and Diseases. Front Mol Biosci. 2021 Sep 3;8:728777. [Content Brief]
- [2]. Liang Y, et al. BRD4 in physiology and pathology: ''BET'' on its partners. Bioessays. 2021 Dec;43(12):e2100180. [Content Brief]
- [3]. Zheng B, et al. Distinct layers of BRD4-PTEFb reveal bromodomain-independent function in transcriptional regulation. Mol Cell. 2023 Aug 17;83(16):2896-2910.e4. [Content Brief]
- [4]. Altendorfer E, et al. BRD4: a general regulator of transcription elongation. Transcription. 2022 Feb-Jun;13(1-3):70-81. [Content Brief]
- [5]. Kanno T, et al. BRD4 assists elongation of both coding and enhancer RNAs by interacting with acetylated histones. Nat Struct Mol Biol. 2014 Dec;21(12):1047-57. [Content Brief]
- [6]. Edwards DS, et al. BRD4 Prevents R-Loop Formation and Transcription-Replication Conflicts by Ensuring Efficient Transcription Elongation. Cell Rep. 2020 Sep 22;32(12):108166. [Content Brief]
- [7]. Jung M, et al. Targeting BET bromodomains for cancer treatment. Epigenomics. 2015;7(3):487-501. [Content Brief]
- [8]. Lucas X, et al. 4-Acyl pyrroles: mimicking acetylated lysines in histone code reading. Angew Chem Int Ed Engl. 2013 Dec 23;52(52):14055-9. [Content Brief]
- [9]. Kargbo RB. PROTAC Degradation of Bromodomain for the Treatment of Hyperplasia and Cancer. ACS Med Chem Lett. 2019 Sep 30;10(10):1372-1373. doi: 10.1021/acsmedchemlett.9b00424. PMID: 31620218; PMCID: PMC6792170. et al. PROTAC Degradation of Bromodomain for the Treatment of Hyperplasia and Cancer. ACS Med Chem Lett. 2019 Sep 30;10(10):1372-1373. [Content Brief]
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BRD4 Related Products (300)
Related Products (300)
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TAT-PiET-PROTAC
0 ImagesTAT-PiET-PROTAC is a proteolysis-targeting chimera (PROTAC)-modified TAT-PiET (HY-P10445), which is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4. TAT-PiET-PROTAC can reduce BRD4 and JMJD6 levels and inhibit cell proliferation. TAT-PiET-PROTAC also resists the endocrine resistance of ERα-positive breast cancer cells. TAT-PiET-PROTAC can be used for the research of cancer, such as breast cancer.
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ML 2-14
0 ImagesCat. No.: HY-132991Purity: 99.43%ML 2-14 is a PROTAC targeting BRD4 with a C4 alkyl linker. ML 2-14 consists of the E3 ligase ligand EN219 (HY-115715) (bule part), the target protein ligand JQ-1 (HY-13030) (red part), and the PROTAC linker (balck part). ML 2-14 can effectively degrade BRD4 in 231MFP breast cancer cells, and this effect can be reversed by the proteasome inhibitor Bortezomib (HY-10227) and the E1 activase inhibitor TAK-243 (HY-100487). ML 2-14 can be used for breast cancer-related research.
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Y06137
0 ImagesY06137 is a potent and selective BET inhibitor for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the BRD4(1) bromodomain with a Kd of 81 nM.
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PROTAC BRD4 Degrader linker conjugate-1
0 ImagesCat. No.: HY-138632CAS No.: 2417370-42-2PROTAC BRD4 Degrader linker conjugate is a linker-payload conjugate as well as a bifunctional degrader of BRD4 that binds to VHL, consisting of PROTAC and a linker. PROTAC BRD4 Degrader linker conjugate can be conjugated with STEAP1 and CLL1 antibodies to degrade BRD4 protein, with DC50 values of 0.86 nM and 7.6 nM, respectively. PROTAC BRD4 Degrader linker conjugate can be used in research related to prostate cancer and acute myeloid leukemia (BRD4 ligand: (HY-129939); VHL ligand: (HY-125845)).\n
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ET-JQ1-OH
0 ImagesCat. No.: HY-147046CAS No.: 2421153-77-5ET-JQ1-OH is an allele-specific BET inhibitor. ET-JQ1-OH can serve as a Ligand for Target Protein for PROTAC, and is used for the development and design of PROTAC Brd4 degraders, such as AB3145 (HY-180923).
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dHTC3
0 ImagesCat. No.: HY-181976dHTC3 is a selective BRD4 molecular glue degrader. dHTC3 selectively binds to BRD4 BD1 to form a BRD4-dHTC3 complex, which cooperatively recruits the SCFFBXO3 E3 ubiquitin ligase and mediates the degradation of BRD4 via the ubiquitin-proteasome pathway. dHTC3 induces proteasome- and CRL-dependent BRD4 degradation with no hook effect. dHTC3 can be used in related research on acute myeloid leukemia.
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TrimTAC1
0 ImagesTrimTAC1 is a TRIM21-based PROTAC degrader targeting BRD4, with a DC50 of 0.649 nM. TrimTAC1 selectively degrades multimeric proteins, including those localized in biomolecular condensates, while exerting no effect on monomeric proteins in the dilute phase. This degradation effect can be blocked by Bortezomib (HY-10227) or TAK-243 (HY-100487). TrimTAC1 can be used in research related to pancreatic cancer and autoimmune diseases.
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MS83
0 ImagesCat. No.: HY-139620CAS No.: 2762181-19-9MS83 is a selective degrader of BRD4/BRD3 belonging to the PROTAC class. MS83 hijacks the KEAP1-dependent CUL3 ligase complex by binding to KEAP1 and forming a ternary complex with BRD4/BRD3. MS83 induces polyubiquitination and degradation of BRD4/BRD3 in a concentration-, time- and ubiquitin-proteasome system-dependent manner. MS83 inhibits c-MYC protein levels and suppresses the proliferation of triple-negative breast cancer cells.
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BRD4 ligand 6
0 ImagesCat. No.: HY-161651CAS No.: 1101702-80-0BRD4 ligand 6 is a BRD4 ligand and can be used for synthesis of BRD4 PROTACs, such as PROTAC BRD4 Degrader-26 (HY-161650).
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CFT-2718
0 ImagesCat. No.: HY-132941Purity: 99.87%CFT-2718 is a selective CRBN-dependent BRD4 PROTAC degrader. CFT-2718 mediates rapid, selective BRD4 degradation, reduces total and phosphorylated Ser2 RPB1 levels, and reduces MYC protein levels. CFT-2718 can inhibit cancer cells proliferation and induce apoptosis. CFT-2718 reduces growth of lung cancer and pancreatic patient-derived xenograft models. CFT-2718 can be used for the research of cancer, such as small-cell lung cancer and pancreatic cancer.
