2. Signaling Pathways
  3. Epigenetics
  4. Epigenetic Reader Domain
  5. BD2 Isoform

BD2

BD2 is one of the tandem bromodomains within bromodomain and extraterminal (BET) proteins, a family of epigenetic readers that recognize acetyl-lysine marks on chromatin and facilitate transcriptional regulation through chromatin binding.[1][2] Mechanistically, BET bromodomains enable chromatin association that supports transcriptional programs, and BRD4 further contributes to transcriptional elongation through recruitment of positive transcription elongation factor complexes.[2][3] Because BET proteins influence gene expression, they are implicated in cancer and other disease-associated transcriptional states.[1][3] Disease relevance is particularly evident in BRD4-driven malignancies, including NUT midline carcinoma, where disruption of bromodomain-mediated chromatin interactions suppresses proliferation and promotes differentiation in experimental models.[3] Compared with the related BD1 bromodomain, BD2 has emerged as a distinct pharmacological target, and selective targeting of BD1 and BD2 has demonstrated that the two bromodomains make non-identical contributions to BET protein function.[2][4] This isoform distinction has stimulated the development of BD2-selective chemical probes and inhibitors designed to preferentially engage the second bromodomain while preserving greater selectivity than dual BD1/BD2 inhibition.[4][5] For experimental applications, BD2-selective inhibitors provide tools to investigate BET-dependent transcriptional regulation, chromatin remodeling, oncogenic gene-expression programs, and disease-associated signaling pathways.[4][5]

BD2 Related Products (8):

Cat. No. Product Name Effect Purity
  • HY-114416
    GS-626510
    		Inhibitor 99.46%
    GS-626510 is a potent, and orally active BET family bromodomains inhibitor, with Kd values of 0.59-3.2 nM for BRD2/3/4, with IC50 values of 83 nM and 78 nM foe BD1 and BD2, respectively.
  • HY-178041
    BRD4-BD1/2-IN-3
    		Inhibitor 99.52%
    BRD4-BD1/2-IN-3 (Compound B6) is a selective BRD4 BD2 inhibitor with an IC50 of 0.41  nM for BRD4 BD2 over BRD4 BD1. BRD4-BD1/2-IN-3 significantly inhibits the LPS (HY-D1056)-induced expression of IL-6. BRD4-BD1/2-IN-3 shows anti-inflammatory activities by modulating the TNF and NF-κB signaling pathway. BRD4-BD1/2-IN-3 can be used for inflammatory diseases research.
  • HY-132230
    GSK040
    		Inhibitor
    GSK040 is a potent and highly selective BET BD2 inhibitor, with a pIC50 of 8.3. GSK040 shows more than 5000-fold selectivity for BET BD2 over BET BD1 (pIC50=4.6). GSK040 can be used for the research of oncology and immunology diseases.
  • HY-160634
    BRD4 Inhibitor-31
    		Inhibitor
    BRD4 Inhibitor-31 (Example 136) is a BRD4 inhibitor (Kis: 0.234 μM and 0.295 μM for BRD4 BD1 and BRD4 BD2 respectively). BRD4 Inhibitor-31 can be used for research of inflammatory diseases, cancer, and AIDS.
  • HY-162622
    BET-IN-26
    		Inhibitor
    BET-IN-26 (compound 13a) is a potent, selective and orally active BD1 inhibitor with IC50 values of 0.0055, 9.0 µM for BD1, BD2, respectively. BET-IN-26 decreases LPS (HY-D1056) induced serum levels of IL-6 and MCP-1.
  • HY-183922
    SRX3212
    		Inhibitor
    SRX3212 is a potent PI3Kα/BRD4 inhibitor with human IC50 values of 22 nM, 3.7 nM, and 32 nM for PI3Kα, BRD4BD1, and BRD4BD2, respectively. SRX3212 inhibits PI3K kinase activity and blocks acetyllysine binding function of BRD4BD1 and BRD4BD2. SRX3212 can be used for the research of mantle cell lymphoma, colon carcinoma, neuroblastoma, prostate cancer[1].
  • HY-173237
    CDK4/6/BRD4-IN-1
    		Inhibitor
    CDK4/6/BRD4-IN-1 (B15) is an inhibitor of CDK4, CDK6 and BRD4, with IC50 values of 220 nM, 146 nM, 106 nM and 85 nM for BRD4-BD2, BRD4-BD1, CDK6 and CDK4, respectively. CDK4/6/BRD4-IN-1 (B15) can be used in the study of NSCLC (Non-Small Cell Lung Cancer). CDK4/6/BRD4-IN-1 (B15) induces cell cycle arrest and apoptosis.
  • HY-155078
    BRD4 Inhibitor-27
    		Inhibitor
    BRD4 Inhibitor-27 (compound 6) is a BRD4 inhibitor with IC50 of 9.6 and 11.3 μM for BRD4 BD1 and BRD4 BD2, respectively. BRD4 Inhibitor-27 has the potential to study cancer.