GlpBio

Epigenetic Reader Domain

Epigenetic Reader Domain(表观识别蛋白结构域)

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.

Epigenetic Reader Domain 相关产品(242)

  • GC19328 structure
    GC19328SF2523
    CAS: 1174428-47-7

    A dual inhibitor of PI3K and BRD4

  • GC19409 structure
    GC19409ABBV-744
    CAS: 2138861-99-9
    纯度: >99.50%

    A BD2 bromodomain inhibitor

  • GC19455 structure
    GC19455ZL0420
    CAS: 2230496-80-5
    纯度: >98.00%

    A BRD4 inhibitor

  • GC30644 structure
    GC30644INCB054329 Racemate
    CAS: 1628607-62-4

    INCB054329Racemate是BET蛋白的抑制剂。

  • GC30714 structure
    GC30714GSK4028
    CAS: 2079886-19-2
    纯度: >98.50%

    GSK4028是GSK4027的对映体阴性对照，GSK4027是一种PCAF/GCN5溴结构域的化学探针，而GSK4028对应的pIC50值为4.9。

  • GC31245 structure
    GC31245EML 425
    CAS: 1675821-32-5
    纯度: >98.00%

    An inhibitor of p300 and CBP

  • GC31654 structure
    GC31654KG-501 (Naphthol AS-E phosphate)
    CAS: 18228-17-6
    纯度: >98.00%

    KG-501 (Naphthol AS-E phosphate) 是一种能够抑制cAMP反应元件结合蛋白（CREB）与CREB结合蛋白（CBP）相互作用的小分子化合物，其IC₅₀值为6.89μM。

  • GC31731 structure
    GC31731GSK 4027
    CAS: 2079896-25-4
    纯度: >98.50%

    A PCAF/GCN5 bromodomain inhibitor

  • GC31831 structure
    GC31831BET-IN-1
    CAS: 1422554-34-4
    纯度: >99.00%

    BET-IN-1 是所有八个 BET 溴结构域的泛抑制剂，并且比其他具有代表性的含溴结构域的蛋白质具有选择性。

  • GC31881 structure
    GC31881MS417 (GTPL7512)
    CAS: 916489-36-6
    纯度: >99.50%

    MS417 (GTPL7512) 是一种选择性 BET 特异性 BRD4 抑制剂，与 BRD4-BD1 和 BRD4-BD2 结合，IC50 分别为 30、46 nM 和 Kds 分别为 36.1、25.4 nM，对 CBP BRD 的选择性较弱 (IC50, 32.7 μ ;M)。

  • GC32081 structure
    GC32081GNE-781
    CAS: 1936422-33-1
    纯度: >98.00%

    GNE-781 (compound 19) is an orally active, highly potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein (CBP) with IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50 of 6.2 nM and 5100 nM, respectively. GNE-781 exhibits antitumor activity.

  • GC32677 structure
    GC32677A-485
    CAS: 1889279-16-6
    纯度: >99.50% / >98.00%

    A-485是有效的选择性p300/CBP（组蛋白乙酰转移酶旁系同源物/CREB结合蛋白）的催化抑制剂，对p300 HAT的IC 50 值为60nM。A-485可抑制p300-BHC（溴域HAT-C/H3）和CBP-BHC结构域的活性，IC 50 分别为9.8nM和2.6nM。

  • GC32685 structure
    GC32685ARV-771
    CAS: 1949837-12-0
    纯度: >99.50%

    ARV-771是一种泛BET-PROTAC，能有效降解BRD2/3/4蛋白，DC 50 值低于5nM。

  • GC32689 structure
    GC32689666-15
    CAS: 1433286-70-4
    纯度: >99.50%

    666-15是一种选择性环磷酸腺苷反应元件结合蛋白（CREB）抑制剂，IC 50 值为0.081±0.04μM。

  • GC32719 structure
    GC32719dBET6
    CAS: 1950634-92-0
    纯度: >99.50%

    dBET6是一种新型的、具有口服活性的BRD4降解剂，可抑制c-Myc等致癌基因的转录和表达。

  • GC32747 structure
    GC32747GNE-272
    CAS: 1936428-93-1
    纯度: >99.50%

    GNE-272是一种有效和选择性的环磷酸腺苷反应元件结合蛋白（CBP）抑制剂，是E1A结合蛋白p300（EP300）的抑制剂，IC 50 值分别为0.02和0.03μM，也是CBP/EP300溴结构域体内探针。

  • GC32791 structure
    GC32791BETd-260 (ZBC 260)
    CAS: 2093388-62-4
    纯度: >98.00%

    BETd-260 (ZBC 260)是一种基于蛋白水解靶向嵌合体（PROTAC）技术设计的异双功能小分子化合物，通过连接Cereblon配体和BET配体来发挥作用。

  • GC32798 structure
    GC32798MI-538
    CAS: 1857417-10-7
    纯度: >99.00%

    MI-538是menin和MLL融合蛋白相互作用的抑制剂；IC50值为21nM。

  • GC32812 structure
    GC32812BMS-986158
    CAS: 1800340-40-2
    纯度: >98.50%

    A BET bromodomain inhibitor

  • GC32863 structure
    GC32863Target Protein-binding moiety 4
    CAS: 1300019-38-8
    纯度: >98.50%

    Target Protein-binding moiety 4 (Molibresib carboxy acid) 是一种基于 I-BET762 的弹头配体，用于 PROTAC 靶向 BET 的共轭反应。 Target Protein-binding moiety 4 (Molibresib carboxy acid) 是一种 BRD4 抑制剂，pIC50 为 5.1。

  • GC32880 structure
    GC32880TPOP146
    CAS: 2018300-62-2
    纯度: >99.50%

    TPOP146是选择性的CBP/P300苯并西泮溴结构域抑制剂；对CBP和BRD4的Kd值分别为134nM和5.02μM。

  • GC32960 structure
    GC32960GNE-049
    CAS: 1936421-41-8
    纯度: >98.50%

    GNE-049是一种高效的选择性CBP抑制剂，在TR-FRET实验中IC50为1.1nM。GNE-049还抑制BRET和BRD4(1)，IC50分别为12nM和4200nM。

  • GC32980 structure
    GC32980PROTAC BET degrader-2
    CAS: 2093388-33-9
    纯度: >98.50%

    PROTACBETdegrader-2是一种强效的溴域及末端外(BET)蛋白的降解剂，在RS4;11细胞中测得其对细胞生长的IC50值为9.6nM，并能实现肿瘤消退。

  • GC33015 structure
    GC33015FL-411 (BRD4-IN-1)
    CAS: 2118944-88-8
    纯度: >98.00%

    FL-411 (BRD4-IN-1) is a potent and selective inhibitor of Bromodomain-containing protein 4 (BRD4) with IC50 of 0.43 μM for BRD4(1). FL-411 induces ATG5-dependent autophagy-associated cell death (ACD) by blocking BRD4-AMPK interaction.