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.

5 Items

  • 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
  • 653-47 hydrochloride
    Cat. No.
    A24421

    653-47 hydrochloride

    653-47 hydrochloride is a potentiator that significantly enhances the CREB (cAMP-response element-binding protein) inhibitory activity of 666-15. It also functions as a very weak CREB inhibitor on its own, with an IC₅₀ of 26.3 μM.

    5 mg
    $198.00
    10 mg
    $341.00
    All 4 sizes
  • UNC4976
    Cat. No.
    A26805

    UNC4976

    UNC4976 is a positive allosteric modulator of the CBX7 chromodomain, targeting nucleic acid binding. It functions by antagonizing the H3K27me3-specific recruitment of CBX7 to target genes while enhancing non-specific binding to DNA and RNA. This compound is valuable for research focused on chromatin regulation and the epigenetic mechanisms involved in gene expression.

    Out of stock

    All 3 sizes

5 Items

Added to your cart

View Cart Checkout

    Loading...