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 (55)
Related Products (55)
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ABBV-744
0 ImagesABBV-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.
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GSK778
0 ImagesSynonyms: iBET-BD1GSK778 (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.
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PROTAC BRD3 degrader-1
0 ImagesCat. No.: HY-180889CAS No.: 2257497-15-5PROTAC BRD3 degrader-1 (compound D072) is a potent and selective PROTAC BRD3 degrader. PROTAC BRD3 degrader-1 selectively degrades BRD3 in mice, leading to the downregulation of H3K18ac without affecting BRD2 or BRD4. PROTAC BRD3 degrader-1 reduces intraocular inflammation in the experimental autoimmune uveitis (EAU) mouse mode and inhibits proinflammatory microglia in both uveitis retina and LPS (HY-D1056) treated mouse microglia cell line BV2. PROTAC BRD3 degrader-1 can be used for uveitis research.
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BET-IN-30
0 ImagesCat. No.: HY-181735BET-IN-30 (Compound 11d) is a BTE family protein inhibitor, which can act as a BRD2/BRD3/BRD4 target protein ligand and be used for the synthesis of PROTACs, such as PROTAC BET Degrader-15 (HY-181729). BET-IN-30 exhibits potent anti-proliferative activity against acute myeloid leukemia (AML) cells such as MV4-11. BET-IN-30 can be used for the study of AML.
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PROTAC BRD4 Degrader-46
0 ImagesCat. No.: HY-182801CAS No.: 2766179-68-2PROTAC BRD4 Degrader-46 is a heterobifunctional BRD4 PROTAC degrader. PROTAC BRD4 Degrader-46 binds to both BRD4 and CRBN, thereby triggering ubiquitination and proteasomal degradation of BRD4. PROTAC BRD4 Degrader-46 downregulates the levels of downstream BRD2, BRD3 and MYC. PROTAC BRD4 Degrader-46 can be used in the research of cancers such as multiple myeloma.
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GSK046
0 ImagesSynonyms: iBET-BD2GSK046 (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.
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TMX1
0 ImagesTMX1 is a covalent, selective BRD4 molecular glue degrader. TMX1 binds to the JQ1-binding site of BRD4BD2, forms covalent bonds with Cys58 of DCAF16 and Cys87 of GAK in a BRD4BD2-dependent template-assisted manner, stabilizes the BRD4-TMX1-DCAF16 ternary complex, and promotes the ubiquitination of BRD4 via the CRL4DCAF16 ubiquitin ligase complex. TMX1 induces selective degradation of BRD4, mild degradation of BRD2 and BRD3, as well as DCAF16-dependent cytotoxicity.
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GSK973
0 ImagesGSK973, a chemical probe, is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5).
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LT052
0 ImagesLT052 is a highly selective BET BD1 inhibitor with an IC50 of 87.7 nM. LT052 exhibits nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2 (IC50=12.130 μM). LT052 has anti-inflammatory?activity and can be used for acute gout arthritis research.
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(S)-JQ-35
0 ImagesSynonyms: TEN-010(S)-JQ-35 (TEN-010) is an orally active, blood-brain barrier-permeable bromodomain inhibitor that selectively targets the bromodomain and extra-terminal domain (BET) protein family (BRD4, BRD3, BRD2 and BRDT). (S)-JQ-35 blocks the activation of Myc gene expression by BRD4, thereby inhibiting cancer cell proliferation and promoting cancer cell apoptosis. (S)-JQ-35 can be used in research related to NUT midline carcinoma and neuroblastoma.
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HJB97
0 ImagesHJB97 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).
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RVX-297
0 ImagesCat. No.: HY-114504CAS No.: 1044871-04-6RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models.
