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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CF53
0 ImagesCF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo.
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β-NF-JQ1
0 Imagesβ-NF-JQ1 is a BRD2/3/4 PROTAC degrader. β-NF-JQ1 recruits the AhR E3 ligase complex to BRD2, BRD3 and BRD4, induces AhR-BRD interaction, and mediates AhR-dependent degradation through the proximity effect between the target protein and AhR. β-NF-JQ1 acts as an antiproliferative and cytotoxic agent that induces anticancer activity associated with BRD protein knockdown. β-NF-JQ1 can be used for research on breast cancer and neuroblastoma.
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SNIPER(BRD)-1
0 ImagesSNIPER (BRD)-1 is a BRD2/3/4 SNIPER degrader. SNIPER (BRD)-1 induces ubiquitin-proteasome-dependent degradation of the epigenetic regulatory proteins BRD2/3/4 as well as the IAP family E3 ligase itself with its IC50 values for cIAP1, cIAP2 and XIAP of 6.8 nM, 17 nM and 49 nM, respectively. SNIPER (BRD)-1 can be used in the research of prostate cancer.
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BET bromodomain inhibitor 1
0 ImagesBET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity.
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BETd-246
0 ImagesBETd-246 is a BRD2/3/4 PROTAC degrader targeting the BET family. BETd-246 induces ubiquitination and proteasomal degradation of BRD2, BRD3 and BRD4 by recruiting the CUL4-RBX1-DDB1-CRBN E3 ubiquitin ligase complex; it also inhibits TRAT1 expression and depletes BET proteins. BETd-246 suppresses cancer cell proliferation and invasion, disrupts the cell cycle and induces apoptosis. BETd-246 is applicable to research related to triple-negative breast cancer and T-cell acute lymphoblastic leukemia.
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Nrf2 activator-1
0 ImagesNrf2 activator-1 is a potent activator of NF-E2 related factor 2 (Nrf2). Nrf2 activator-1 has the potential for the research of COPD and other respiratory diseases, including asthma, Acute Lung Injury (ALI), Acute Respiratory Distress Syndrome (ARDS) and pulmonary fibrosis (extracted from patent WO2018109647A1).
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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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PROTAC FLT3/JAK2/BRD4 Degrader-1
0 ImagesCat. No.: HY-175610CAS No.: 3067695-20-6PROTAC FLT3/JAK2/BRD4 Degrader-1 is a FLT3/JAK2/BRD4 PROTAC degrader with DC50 values of 5.23, 0.68, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces cereblon- and proteasome-dependent degradation of FLT3, JAK2, and BRD4 via the ubiquitin-proteasome system. PROTAC FLT3/JAK2/BRD4 Degrader-1 is used in studies related to FLT3 inhibitor-resistant leukemia and acute myeloid leukemia.
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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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SJ46421
0 ImagesCat. No.: HY-168634SJ46421 is a BRD3BD2 PROTAC degrader. SJ46421 induces a cooperative ternary complex of KLHDC2 and BRD3BD2 with an IC50 of 7.8 nM. SJ46421 binds to the substrate-binding pocket of KLHDC2, forms cooperative ternary complexes with BRD3BD2, BRD2BD2 and BRD4BD2, disrupts the autoinhibitory tetramer assembly of KLHDC2, drives selective ubiquitination of BRD3BD2, and inhibits the ubiquitination of endogenous KLHDC2 diglycine substrates. SJ46421 can be used in cancer research.
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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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RAJQ14
0 ImagesCat. No.: HY-181495CAS No.: 2375455-53-9RAJQ14 is a BRD4 PROTAC-like CAP-TAC (Proteasome Cap Targeting Chimeras) degrader. RAJQ14 binds to 19S proteasome cap subunits RPN1, RPN10, RPN13, and USP14 to recruit target proteins to the proteasome for ubiquitination-independent, proteasome-dependent degradation. RAJQ14 can be used for the research of cancer (Pink: BRD4 Ligand (HY-181496); Blue: Proteasome Ligand (HY-128978); Black: Linker).
