BRD2
BRD2 is a BET-family epigenetic reader with tandem bromodomains that bind lysine-acetylated histones and transcription factors, recruit transcription factors and coactivators, and support RNA polymerase II-dependent transcriptional elongation[1]. Mechanistically, BET proteins including BRD2, BRD3, BRD4, and BRDT connect acetylated chromatin to gene-expression programs that regulate transcription, chromatin remodeling, DNA replication, and DNA damage repair[1]. In pancreatic β-cells, BET inhibition with JQ1 increased insulin secretion and insulin content, while specific inhibition of Brd2 increased fatty acid oxidation, showing a discrete metabolic role for BRD2 compared with other BET isoforms[2]. Compared with BRD4, BRD2 appears less dominant in several disease models: BRD4, not BRD2 or BRD3, increased after repeated cocaine exposure, and BRD4 was preferentially linked to cocaine-induced Bdnf expression[3]. In prostate cancer, BET proteins BRD2, BRD3, and BRD4 are stabilized by SPOP mutations, contributing to BET-inhibitor resistance, but BRD4 often carries the main disease-specific transcriptional signal[4]. For experimental applications, pan-BET inhibitors such as JQ1, I-BET, OTX015, and RVX-208 help probe BRD2-containing acetyl-lysine reader complexes, although their limited isoform selectivity requires paired genetic approaches for BRD2-specific interpretation[5].
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]. Deeney JT, et al. BET Bromodomain Proteins Brd2, Brd3 and Brd4 Selectively Regulate Metabolic Pathways in the Pancreatic β-Cell. PLoS One. 2016 Mar 23;11(3):e0151329. [Content Brief]
- [3]. Sartor GC, et al. Epigenetic Readers of Lysine Acetylation Regulate Cocaine-Induced Plasticity. J Neurosci. 2015 Nov 11;35(45):15062-72. [Content Brief]
- [4]. Dai X, et al. Prostate cancer-associated SPOP mutations confer resistance to BET inhibitors through stabilization of BRD4. Nat Med. 2017 Sep;23(9):1063-1071. [Content Brief]
- [5]. Lucas X, et al. Targeting the BET family for the treatment of leukemia. Epigenomics. 2014 Apr;6(2):153-5. [Content Brief]
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BRD2 Related Products (66)
Related Products (66)
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Antibodies (1)
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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).
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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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BRD4 Inhibitor-40
0 ImagesCat. No.: HY-173062CAS No.: 2994635-04-8BRD4 Inhibitor-40 (Compound 23) is the inhibitor for BRD that inhibits BRD4-BD1, BRD4-BD2, BRD2-BD1 and BRD2-BD2 with IC50s of 16.1, 142.18, 29.35 and 302.35 nM, respectively. BRD4 Inhibitor-40 modulates the expression of c-Myc and p21, arrests cell cycle at G1 phase, inhibits Pkd1-null (PN) renal cystic epithelial cells, and blocks the renal cysts formation in Madin-Darby canine kidney and embryonic kidney vesicle models. BRD4 Inhibitor-40 exhibits renal cysts inhibitory activity in mouse models.
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BET BD2-IN-1
0 ImagesCat. No.: HY-155680CAS No.: 2677039-24-4
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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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PROTAC BRD2 BD1 Degrader-1
0 ImagesCat. No.: HY-175678PROTAC BRD2 BD1 Degrader-1 is a potent and selective BRD2 BD1 PROTAC degrader, with a DC50 of 65 nM, an EC50 of 423 nM, and a Kd of 69 nM against BRD2 BD1. PROTAC BRD2 BD1 Degrader-1 induces the formation of a ternary complex between the BET bromodomain and the VHL E3 ubiquitin ligase complex, triggering VCB-dependent degradation of the target bromodomain. PROTAC BRD2 BD1 Degrader-1 can be used in cancer research.
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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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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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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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BRD4 D1-IN-3
0 ImagesCat. No.: HY-180831BRD4 D1-IN-3 (compound 39) is a potent, selective, and cell-active BRD4-D1 inhibitor (IC50 = 39 nM, Ki = 2.4 nM) with >1700-fold selectivity over BRD2-D1. BRD4 D1-IN-3 reduces the expression of pro-inflammatory chemokines CXCL1 and CCL2 in an LPS (HY-D1056)-mediated cellular model of liver inflammation. BRD4 D1-IN-3 can be used for liver inflammation research.
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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.
