Epigenetic Reader Domain

Epigenetic reader domain inhibitors, mostly bromodomain inhibitors, block recognition of acetylated histone lysines. Structural work on a histone acetyltransferase bromodomain first showed that this module binds acetylated lysine. Proteins of the bromodomain and extra-terminal (BET) family, such as bromodomain-containing protein 4 (BRD4), link histone acetylation to gene transcription. The thienodiazepine (+)-JQ1 was described in 2010 as a selective BET inhibitor that displaces BRD4 from chromatin. PFI-1, GSK1324726A and CPI-203 provide further BET inhibitor chemotypes for comparative studies. Other entries reach beyond BET binding, such as SGC-CBP30 for a non-BET bromodomain and the BRD4-degrading compound ARV-825.

7 Items

  • UNC1215
    Cat. No.
    A12948

    UNC1215

    UNC1215 is a potent, selective antagonist of L3MBTL3 with cellular activity.

    2 mg
    $30.00
    5 mg
    $50.00
    All 7 sizes
  • UNC 669
    Cat. No.
    A13717

    UNC 669

    UNC669 is a small-molecule antagonist of methyl-lysine (KMe) reader protein with selectivity for L3MBTL1 and L3MBTL3 (IC50 of 4.2μM and 3.1μM respectively)

    5 mg
    $20.00
    10 mg
    $30.00
    All 8 sizes
  • MZ1
    Cat. No.
    A17014

    MZ1

    MZ1 is a potent inducer of reversible, long-lasting and selective removal of BRD4 over BRD2 and BRD3.

    1 mg
    $40.00
    2 mg
    $75.00
    All 7 sizes
  • AR420626
    Cat. No.
    A23991

    AR420626

    AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3, also known as GPR41), with an IC₅₀ of 117 nM. It demonstrates anti-inflammatory, antitumor, and antidiabetic activities. AR420626 improves neurogenic diarrhea by modulating neural pathways mediated by nicotinic acetylcholine receptors (nAChRs). In cancer models, it suppresses the growth of HepG2 xenografts and inhibits hepatoma cell proliferation through apoptosis induction. Additionally, AR420626 mitigates allergic asthma and eczema and enhances glucose uptake by activating FFAR3-mediated Ca²⁺ signaling, offering potential therapeutic benefits in metabolic disorders such as diabetes.

    5 mg
    $77.00
    10 mg
    $132.00
    All 4 sizes
  • UNC3866 TFA
    Cat. No.
    A26666

    UNC3866 TFA

    UNC3866 TFA is a selective antagonist of the CBX7-H3 interaction, exhibiting a potency with an IC50 value of 66±1.2 nM as determined by AlphaScreen assays. This compound shows over 100-fold selectivity for CBX7 compared to other members of the methyl-lysine reader panel. UNC3866 TFA is valuable for research applications focused on elucidating the role of CBX7 in epigenetic regulation and potential therapeutic strategies targeting this pathway.

    2 mg
    $25.00
    5 mg
    $40.00
    All 5 sizes
  • C-82
    Cat. No.
    A37081

    C-82

    C-82 is a selective antagonist of CBP/β-catenin interaction, designed to inhibit the binding of β-catenin to CBP while promoting its association with p300. This compound effectively modulates the Wnt signaling pathway, making it a valuable tool for research in cancer biology and developmental processes. C-82 serves as an important reagent for studies investigating the role of β-catenin in transcriptional regulation and related disease mechanisms.

    1 mg
    $300.00
    5 mg
    $620.00
    All 4 sizes
  • BRD4 Inhibitor-37
    Cat. No.
    A40623

    BRD4 Inhibitor-37

    BRD4 Inhibitor-37 is a selective antagonist of the Epigenetic Reader Domain BRD4, demonstrating significant anticancer activity. With an IC50 ranging from 0.05-0.1 μM in binding assays and a GI50 of 0.1-0.3 μM in cellular models, this compound effectively impedes the c-Myc signaling pathway, a critical downstream target of BRD4. Its selectivity across multiple bromodomain proteins positions BRD4 Inhibitor-37 as an important tool for investigating BET protein functions in cancer research and therapeutic development.

    1 mg
    $20.00
    5 mg
    $25.00
    All 7 sizes

7 Items

Added to your cart

View Cart Checkout

    Loading...