BRD3
BRD3 (bromodomain-containing protein 3) is a member of the BET (bromodomain and extraterminal domain) family that functions as an epigenetic reader by recognizing acetylated lysine residues on histones and transcription factors, thereby regulating chromatin organization and transcriptional programs.[1][2] Mechanistically, BRD3 couples acetylation-dependent chromatin recognition to gene expression through its tandem bromodomains and recruitment of transcriptional regulatory complexes.[1][3] In hematopoietic systems, BRD3 directly binds acetylated GATA1 through its first bromodomain, promotes GATA1 chromatin occupancy, and supports erythroid gene expression and erythroid maturation, establishing a key role in lineage-specific transcriptional control.[2][3] Beyond hematopoiesis, BRD3 cooperates with the long noncoding RNA DIGIT to form phase-separated condensates at H3K18ac-enriched regulatory regions, where it facilitates transcriptional programs required for definitive endoderm differentiation.[4] These findings place BRD3 at the intersection of chromatin signaling, transcription factor regulation, and developmental cell-fate specification.[2][4] In disease contexts, BRD3 participates in oncogenic chromatin-dependent transcriptional networks, and chromosomal rearrangements involving BRD3-NUT have been implicated in NUT carcinoma.[5] Compared with related BET family members, BRD3 shares conserved bromodomains with BRD2 and BRD4 but lacks the extended C-terminal domain characteristic of BRD4, indicating distinct mechanisms of transcriptional regulation despite overlapping chromatin-binding functions.[1][6] For experimental applications, BET bromodomain inhibitors such as JQ1 and related compounds disrupt acetyl-lysine recognition by BET proteins, providing widely used tools to investigate BRD3-dependent transcriptional regulation and chromatin biology.[7]
References:
- [1]. Belkina AC, et al. BET domain co-regulators in obesity, inflammation and cancer. Nat Rev Cancer. 2012 Jun 22;12(7):465-77. [Content Brief]
- [2]. Lamonica JM, et al. Bromodomain protein Brd3 associates with acetylated GATA1 to promote its chromatin occupancy at erythroid target genes. Proc Natl Acad Sci U S A. 2011 May 31;108(22):E159-68. [Content Brief]
- [3]. Gamsjaeger R, et al. Structural basis and specificity of acetylated transcription factor GATA1 recognition by BET family bromodomain protein Brd3. Mol Cell Biol. 2011 Jul;31(13):2632-40. [Content Brief]
- [4]. Daneshvar K, et al. lncRNA DIGIT and BRD3 protein form phase-separated condensates to regulate endoderm differentiation. Nat Cell Biol. 2020 Oct;22(10):1211-1222. [Content Brief]
- [5]. French CA, et al. BRD-NUT oncoproteins: a family of closely related nuclear proteins that block epithelial differentiation and maintain the growth of carcinoma cells. Oncogene. 2008 Apr 3;27(15):2237-42. [Content Brief]
- [6]. Urra H, et al. A novel ER stress-independent function of the UPR in angiogenesis. Mol Cell. 2014 May 22;54(4):542-4. [Content Brief]
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BRD3 Related Products (62)
Related Products (62)
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BRD3/BRD4-L ligand-2
0 ImagesCat. No.: HY-175924CAS No.: 3075063-28-1
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BET-IN-13
0 ImagesCat. No.: HY-152213CAS No.: 2506823-08-9BET-IN-13 is a potent BET inhibitor with an IC50 value of 1.6 nM. BET-IN-13 reduces LPS-induced TNF-α, IL-1β, IL-6, and NOS2 mRNA expression levels. BET-IN-13 shows anti-inflammatory activity. BET-IN-13 has the potential for the research of acute liver injury.
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SJ44236
0 ImagesCat. No.: HY-170900SJ44236 is a BET PROTAC degrader with activity against BRD2, BRD3 and BRD4 (DC50 = 127 pM). SJ44236 induces ubiquitination and proteasomal degradation by forming a ternary complex with BET proteins and CRBN-DDB1. SJ44236 downregulates c-Myc, upregulates p53 and reduces cancer cell viability. SJ44236 can be used for the research of leukemia and medulloblastoma.
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BET BD2-IN-1
0 ImagesCat. No.: HY-155680CAS No.: 2677039-24-4
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BRD3 ligand-1
0 ImagesCat. No.: HY-180901CAS No.: 2257497-24-6BRD3 ligand-1 is a BRD3 ligand that can be used in studies related to PROTAC synthesis, such as serving as the target protein ligand for PROTAC BRD3 degrader-1 (HY-180889).
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PROTAC BET Degrader-17
0 ImagesCat. No.: HY-181869CAS No.: 2409674-38-8PROTAC BET Degrader-17 is a potent BET protein PROTAC degrader. By recruiting the VHL E3 ligase, PROTAC BET Degrader-17 specifically degrades BRD2, BRD3 (DC50=0.09 nM) and BRD4 (IC50=4.3 nM). PROTAC BET Degrader-17 exhibits strong anti-tumor activity in acute myeloid leukemia (AML) studies; it not only inhibits cancer cell proliferation, induces cell cycle arrest and apoptosis, but also effectively suppresses tumor growth in xenograft mouse models. PROTAC BET Degrader-17 can be used to explore targeted therapies for acute myeloid leukemia.
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SJ46420
0 ImagesCat. No.: HY-168635SJ46420 is a BRD3 PROTAC degrader with a DC50 of 224 nM in U2OS cells. SJ46420 selectively mediates BRD3 degradation, exerts only partial effects on BRD2 and BRD4, and its activity is dependent on KLHDC2. SJ46420 is a prodrug variant of SJ46421 (HY-168634). SJ46420 can be used in the research of prostate cancer.
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PROTAC BET Degrader-16
0 ImagesCat. No.: HY-181867CAS No.: 2410947-65-6PROTAC BET Degrader-16 (Compound A10) is a BET PROTAC degrader with a DC50 of 0.31 nM against BRD4, and it preferentially targets BRD4 over other BET family members. PROTAC BET Degrader-16 degrades BRD2, BRD3 and BRD4 via the ubiquitin-proteasome system, a process that requires target binding and recruitment of the CRBN E3 ligase. PROTAC BET Degrader-16 induces cell cycle arrest and promotes apoptosis. PROTAC BET Degrader-16 exerts anti-tumor activity against acute myeloid leukemia.
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WNY0824
0 ImagesCat. No.: HY-143471CAS No.: 2412707-81-2Synonyms: PLK1/BRD4-IN-1WNY0824 (PLK1/BRD4-IN-1) is an orally active dual inhibitor of PLK1 and BET protein families, with IC50 values of 22, 402.5, 150.7, 103.9, and 311.9 nmol/L for PLK1, BRD2, BRD3, BRD4, and BRDT, respectively. WNY0824 induces cell cycle arrest and apoptosis by inhibiting AR- and MYC-mediated transcriptional processes. In addition, WNY0824 also inhibits tumor growth in Enzalutamide (HY-70002) resistant CRPC xenograft tumor models.
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PROTAC BET Degrader-15
0 ImagesCat. No.: HY-181729PROTAC BET Degrader-15 is a BET PROTAC degrader with DC50 values of <0.10 nM, <0.01 nM, and <0.01 nM against BRD2, BRD3, and BRD4, respectively. PROTAC BET Degrader-15 induces significant G2/M phase cell cycle arrest and triggers apoptosis. PROTAC BET Degrader-15 causes marked downregulation of c-Myc, accompanied by upregulation of the cell cycle inhibitory protein p21, downregulation of CDK6, and an increase in the apoptosis marker cleaved PARP. PROTAC BET Degrader-15 is applicable to the research of hematologic malignancies and lung cancer.
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GXF-111
0 ImagesCat. No.: HY-153414GXF-111 is a BRD3 and BRD4-L PROTAC degrader. Its BD1 and BD2 Ki values against human BRD3 are 11.97 nM and 2.45 nM, respectively. The degradation activity of GXF-111 depends on its binding to BET proteins and Cereblon, as well as the involvement of a functional proteasome. The degradation selectivity of GXF-111 is mainly determined by differences in degradation kinetics and cell types. GXF-111 induces G1 phase cell cycle arrest, downregulates c-Myc expression, upregulates p21 expression, and exhibits antiproliferative activity against a variety of cancer cell lines. GXF-111 can serve as a research tool for cancer-related studies.
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PARP1/BRD4-IN-3
0 ImagesCat. No.: HY-169170PARP1/BRD4-IN-3 (compound HF4) is a potent BRD4 and PARP1 inhibitor with IC50 values of 1210, 2019 nM for BRD4, PARP1, respectively. PARP1/BRD4-IN-3 shows antiproliferative activities. PARP1/BRD4-IN-3 induces apoptosis and cell cycle arrest at G0/G1 phase. PARP1/BRD4-IN-3 causes DNA damage and reduces the protein expression of Rad51. PARP1/BRD4-IN-3 shows antitumor efficacy.
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BT-PROTAC
0 ImagesCat. No.: HY-155371CAS No.: 3032848-64-6BT-PROTAC is a bioorthogonally activatable BRD4/BRD3 PROTAC degrader prodrug. BT-PROTAC is inactive when present alone, but upon activation by tetrazine compounds, it promotes the degradation of BRD4 and BRD3 via the ubiquitin-proteasome system, inhibits c-Myc expression, activates caspase-3, and induces apoptosis in breast cancer cells. BT-PROTAC can be used for breast cancer research.
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BRD4 ligand 15
0 ImagesCat. No.: HY-182371CAS No.: 3076613-24-3
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PROTAC BRD4 Degrader-22
0 ImagesCat. No.: HY-155393CAS No.: 3032850-37-3
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CZL-077
0 ImagesCat. No.: HY-180804CAS No.: 3032444-06-4CZL-077 is a potent, selective, and orally active p300/CBP bromodomain (BRD) inhibitor (p300 IC50 = 0.034 μM, CBP IC50 = 0.052 μM) exhibiting high selectivity over the BRDs of BET proteins (BRD2/3/4). CZL-077 inhibits cell growth with IC50 values of 0.024 μM and 5.6 μM in OPM-2 and 22RV1 cells, respectively. CZL-077 shows antitumor efficacy in OPM-2 and 22RV1 xenograft mouse models. CZL-077 can be used for multiple myeloma and prostate cancer research.
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PROTAC BET Degrader-14
0 ImagesCat. No.: HY-179588PROTAC BET Degrader-14 is a highly efficient PROTAC targeting BET (bromodomain and extra-terminal domain). PROTAC BET Degrader-14 can degrade all BET (BRD2, BRD3, BRD4) family proteins. PROTAC BET Degrader-14 potently degrades BET proteins in U2OS osteosarcoma cell lines (BRD4 DC50 = 130 nM) and KYSE180 esophageal squamous cell carcinoma cell lines (DC50 = 40 nM). PROTAC BET Degrader-14’s dependence on the ubiquitin-proteasome system. PROTAC BET Degrader-14 decreases levels of BET-regulated gene products c-Myc, RUNX2, and KRT14. PROTAC BET Degrader-14 can be used for the study of osteosarcoma.
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AB3067
0 ImagesCat. No.: HY-170390AB3067 is a PROTAC degrader of BET that simultaneously recruits the E3 ligase activities of CRBN and VHL. The DC50 values of AB3067 against BRD2, BRD3, BRD4Short and BRD4Long are 15 nM, 1.6 nM, 2.1 nM and 2.3 nM, respectively. AB3067 induces additive protein ubiquitination and proteasomal degradation, and minimizes the cross-degradation of E3 ligases. AB3067 can be used in colon cancer-related studies.
