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]
-
BRD4 Related Products (300)
Related Products (300)
-
dBET23
0 ImagesCat. No.: HY-123911CAS No.: 1957234-83-1dBET23 is a highly potent and selective BRD4 PROTAC degrader, with a DC50/5h of approximately 50 nM against the BRD4BD1 protein. dBET23 induces the formation of a ternary complex consisting of CRBN, itself, and BRD4BD1, thereby mediating the degradation of BRD4BD1. dBET23 causes downregulation of BRD4 expression in cancer cells. dBET23 can be used for research on malignant tumors.
-
DP-15
0 ImagesDP-15 is a BRD4 and GSPT1 PROTAC degrader with DC50 values of 0.48 nM and 5.25 nM, respectively. DP-15 induces ubiquitination and degradation of BRD4 and GSPT1. DP-15 induces Apoptosis. DP-15 exerts anticancer activity against acute myeloid leukemia and non-Hodgkin's lymphoma cells. DP-15 can be used in studies related to acute myeloid leukemia and non-Hodgkin's lymphoma.
-
Zavabresib
0 ImagesSynonyms: OPN-2853; PLX2853; BET-IN-16Zavabresib (OPN-2853; PLX2853; BET-IN-16) is an orally active inhibitor of the BET family of proteins. Zavabresib blocks bromodomain-mediated interactions, reduces BRD4 enrichment at the regulatory regions of transcription factors in T cells, exerts tumor growth inhibitory effects, and enhances the efficacy of immunotherapy. Zavabresib is applicable to research on chronic lymphocytic leukemia, castration-resistant prostate cancer, diffuse large B-cell lymphoma, colon adenocarcinoma, and myelofibrosis.
-
PROTAC BRD4-binding moiety 1
0 ImagesPROTAC BRD4-binding moiety 1 is a ligand for BRD4. PROTAC BRD4-binding moiety 1 binds to cereblon ligand via a linker to form PROTAC to degrade BRD4 (HY-133136). PROTAC BRD4-binding moiety 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
-
PLK1/BRD4-IN-3
0 ImagesPLK1/BRD4-IN-3 (Compound 21) is a selective dual inhibitor for bromodomain 4 (BRD4) and polo-like kinase 1 (PLK1). PLK1/BRD4-IN-3 inhibits BRD4-BD1, PLK1 and BRDT-BD1, with IC50s of 0.059, 0.127 and 0.245 μM, respectively.
-
GNE-987 GSH linker-2
0 ImagesCat. No.: HY-138634Purity: 99.48%GNE-987 GSH linker-2 is a drug-linker conjugates for ADC. GNE-987 GSH linker-2 is a conjugation of PROTAC GNE-987 (HY-129937A) and ADC linker GSH linker-2 (HY-182740), and can be used to prepare antibody-drug conjugates (ADC) for BRD4 degradation. GNE-987 GSH linker-2 can be used for the research of cancer.
-
PROTAC BRD4 Degrader linker conjugate-3
0 ImagesPROTAC BRD4 Degrader linker conjugate-3 is a VHL-recruiting PROTAC that targets and degrades BRD4. It can be used in studies related to prostate cancer.
-
Desmethyl-QCA276
0 ImagesSynonyms: PROTAC BRD4-binding moiety 4Desmethyl-QCA276 (PROTAC BRD4-binding moiety 4), the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade BET. QCA276 is a BET inhibitor with an IC50 of 10 nM, and with a Ki of 2.3 nM. Desmethyl-QCA276 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
