GLPBio

Epigenetic Reader Domain

Read More about this category

Epigenetic regulators of gene expression and chromatin state include so-called writers, erasers, and readers of chromatin modifications.Well-characterized examples of reader domains include bromodomains typically binding acetyllysine and chromatin organization modifier (chromo), malignant brain tumor (MBT), plant homeodomain (PHD), and Tudor domains generally associating with methyllysine. Research on epigenetic readers has been tremendously influenced by the discovery of selective inhibitors targeting the bromodomain and extraterminal motif (BET) family of acetyl-lysine readers. The human genome encodes 46 proteins containing 61 bromodomains clustered into eight families. Distinct experimental approaches are used to identify the first BET inhibitors, GSK 525762A and (+)-JQ-1.

The Polycomb group (PcG) protein, enhancer of zeste homologue 2 (EZH2), has an essential role in promoting histone H3 lysine 27 trimethylation (H3K27me3) and epigenetic gene silencing. This function of EZH2 is important for cell proliferation and inhibition of cell differentiation, and is implicated in cancer progression. Cyclin-dependent kinases regulate epigenetic gene silencing through phosphorylation of EZH2. In many types of cancers including lymphomas and leukemia, EZH2 is postulated to exert its oncogenic effects via aberrant histone and DNA methylation, causing silencing of tumor suppressor genes.

p300/CBP is not only a transcriptional adaptor but also a histone acetyltransferase.

Products Related to Epigenetic Reader Domain(298)

  • GC14699 structure
    GC14699CPI-203
    CAS: 1446144-04-2
    Purity: >99.00%

    BET bromodomain inhibitor

  • GC14787 structure
    GC14787Curcumin
    CAS: 458-37-7
    Purity: >98.00%

    A yellow pigment with diverse biological activities

  • GC15175 structure
    GC15175BAZ2-ICR
    CAS: 1665195-94-7
    Purity: >98.50%

    Selective BAZ2 bromodomain inhibitor

  • GC15375 structure
    GC15375PFI-1 (PF-6405761)
    CAS: 1403764-72-6
    Purity: >99.50%

    A BET bromodomain inhibitor

  • GC15747 structure
    GC15747I-BET151 (GSK1210151A)
    CAS: 1300031-49-5
    Purity: >99.50%

    I-BET151 (GSK1210151A) (GSK1210151A) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively.

  • GC15789 structure
    GC15789GSK2801
    CAS: 1619994-68-1
    Purity: >99.50%

    inhibitor of BAZ2A and BAZ2B bromodomains

  • GC16299 structure
    GC16299BET bromodomain inhibitor
    CAS: 1380087-89-7
    Purity: >99.50%

    Potent and selective inhibitor for BRD4

  • GC16531 structure
    GC16531Bromodomain Inhibitor, (+)-JQ1
    CAS: 1268524-70-4
    Purity: >99.50%

    A selective inhibitor of BET bromodomains

  • GC16599 structure
    GC16599CPI-169
    CAS: 1450655-76-1
    Purity: >98.00%

    EZH2 inhibitor

  • GC16726 structure
    GC16726BI-7273
    CAS: 1883429-21-7
    Purity: >99.50%

    BRD9 bromodomain inhibitor

  • GC16763 structure
    GC16763NI-57
    CAS: 1883548-89-7
    Purity: >99.50%

    bromodomains of BRPF proteins inhibitor

  • GC16817 structure
    GC16817BI-9564
    CAS: 1883429-22-8
    Purity: >99.50%

    BRD9/7 specific inhibitor

  • GC17073 structure
    GC17073I-BET-762
    CAS: 1260907-17-2
    Purity: >99.00%

    I-BET-762 (I-BET762; GSK525762) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.

  • GC17284 structure
    GC17284Anacardic acid
    CAS: 16611-84-0
    Purity: >98.00%

    Anacardic acid, from cashew nut shell liquid, is a Histone acetyltransferase (HAT) inhibitor with IC 50 values of 8.5μM and 5μM for p300 and p300/CBP-associated factor (PCAF), respectively.

  • GC17482 structure
    GC17482OF-1
    CAS: 919973-83-4
    Purity: >98.00%

    BRPF1B and BRPF2 bromodomain inhibitor

  • GC17973 structure
    GC17973OTX-015
    CAS: 202590-98-5
    Purity: >99.50%

    OTX-015 inhibits the binding of BRD2, BRD3, and BRD4 to acetylated histone 4 in a concentration-dependent manner, with IC 50 values from 92-112nM.

  • GC18508 structure
    GC18508BAY-299
    CAS: 2080306-23-4
    Purity: >99.00%

    BAY-299 is a potent and selective inhibitor of the bromodomain and PHD finger-containing (BRPF) family protein BRD1 (IC50 = 6 nM), also known as BRPF2, and the second bromodomain of transcription initiation factor TFIID subunits 1 (TAF1; IC50 = 13 nM).

  • GC18729 structure
    GC18729MZ1
    CAS: 1797406-69-9
    Purity: >99.00%

    MZ1 is a hybrid compound that drives the selective proteasomal degradation of bromodomain-containing protein 4 (BRD4).

  • GC18731 structure
    GC18731LP99
    CAS: 1808951-93-0
    Purity: >99.50%

    LP99 is a potent inhibitor of the bromodomain containing proteins BRD7 and BRD9 that binds with Kd values of 99 and 909 nM, respectively, as determined by isothermal titration calorimetry.

  • GC18750 structure
    GC18750NEO2734
    CAS: 2081072-29-7
    Purity: >99.50%

    An orally active dual p300/CBP and BET bromodomain selective inhibitor

  • GC19038 structure
    GC19038ARV-825
    CAS: 1818885-28-7
    Purity: >99.00%

    ARV-825 is a BRD4 Inhibitor based on PROTAC technology.

  • GC19098 structure
    GC19098CeMMEC1
    CAS: 440662-09-9
    Purity: >99.50%

    CeMMEC1 is an inhibitor of BRD4, and also has high affinity for TAF1, with an IC50 of 0.9 uM for TAF1, and a Kd of 1.8 uM for TAF1 (2).

  • GC19119 structure
    GC19119dBET1
    CAS: 1799711-21-9
    Purity: >98.00%

    dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM.

  • GC19200 structure
    GC19200INCB-057643
    CAS: 1820889-23-3
    Purity: >98.00%

    INCB-057643 is a novel, orally bioavailable BET inhibitor.