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]
-
BRD2 Related Products (67)
Related Products (67)
-
Antibodies (1)
-
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.
-
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.
-
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.
-
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.
-
BRD4 Inhibitor-20
0 ImagesBRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer.
-
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.
-
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.
-
GSK785
0 ImagesCat. No.: HY-181003CAS No.: 3125088-67-4
-
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.
-
PROTAC BRD2/BRD4 degrader-1
0 ImagesCat. No.: HY-130612CAS No.: 2570470-42-5PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. PROTAC BRD2/BRD4 degrader-1 effectively inhibits solid tumors with low cytotoxic effect.
-
KB-0118
0 ImagesCat. No.: HY-176535CAS No.: 2648377-08-4Synonyms: BBC0115KB-0118 (BBC0115) is an orally active BET bromodomain inhibitor. KB-0118 selective binds to BRD2 and BRD4 over BRD3, with Kd values of 36.7 μM for BRD2 BD1 and 47.4 μM for BRD4 BD1. KB-0118 inhibits pro-inflammatory cytokines, including TNF, IL-1β, and IL-23a and selectively suppresses Th17 cell differentiation. KB-0118 modulates Th17-driven inflammation occurs through epigenetic suppression of BRD4, confirmed by downregulation of STAT3 and BRD4 target genes. KB-0118 has immunomodulatory effects in inflammatory bowel disease (IBD) model.
-
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.
-
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.
