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.

8 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
  • 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
  • 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
  • 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
  • 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

8 Items

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