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)

  • GC33017 structure
    GC33017BRD4 degrader AT1
    CAS: 2098836-45-2
    纯度: >98.50%

    BRD4degraderAT1是基于PROTAC技术的一种高度选择性的Brd4降解剂，在细胞中对Brd4BD2的Kd值为44nM。

  • GC33026 structure
    GC33026INCB054329
    CAS: 1628607-64-6
    纯度: >98.00%

    INCB054329 (INCB-054329, INCB-54329) is a structurally distinct bromodomain and extraterminal domain (BET) inhibitor with IC50 values of 44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM and 63 nM for BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2, respectively.

  • GC33028 structure
    GC33028CF53
    CAS: 1808160-52-2
    纯度: >98.00%

    CF53是一种高效、选择性、可口服的BET抑制剂，对BRD4BD1的Ki值为<1nM，Kd值为2.2nM，IC50值为2nM；CF53对BRD2，BRD3，BRD4和BRDTBET蛋白的BD1和BD2两个结构域都有高亲和性，对其选择性远高于非含溴结构域BET蛋白。CF53在体外和体内都具有显著的抗肿瘤活性[1]</su

  • GC33042 structure
    GC33042IACS-9571 (ASIS-P040)
    CAS: 1800477-30-8

    IACS-9571 (ASIS-P040) 是一种有效的选择性 TRIM24 和 BRPF1 抑制剂，对 TRIM24 的 IC50 为 8 nM，对 TRIM24 和 BRPF1 的 Kd 分别为 31 nM 和 14 nM。

  • GC33102 structure
    GC33102MZP-54
    CAS: 2010159-47-2
    纯度: >98.00%

    MZP-54是基于PROTAC技术的一种选择性的BRD3/4降解剂，对Brd4BD2的Kd值为4nM。

  • GC33104 structure
    GC33104BAY1238097
    CAS: 1564268-08-1
    纯度: >98.50%

    BAY1238097是一种有效的、BET与组蛋白结合的选择性抑制剂，通过下调c-Myc水平及下游转录组，在AML(急性髓性白血病)和MM(多发性骨髓瘤)模型中表现出较强的抗增殖活性(TR-FRET中测得的IC50值<100nM)。

  • GC33109 structure
    GC33109PROTAC BET Degrader-1
    CAS: 2093386-22-0
    纯度: >98.50%

    PROTACBETDegrader-1是基于PROTAC技术的BET降解剂，能够在低浓度下降低BRD2，BRD3和BRD4的蛋白水平。

  • GC33183 structure
    GC33183L-45 (L-Moses)
    CAS: 2079885-05-3
    纯度: >99.00%

    L-45 (L-Moses) (L-45) 是第一个有效的、选择性的和细胞活性的 p300/CBP 相关因子 (PCAF) 溴结构域 (Brd) 抑制剂，Kd 为 126 nM。

  • GC33198 structure
    GC33198(S)-JQ-35 (TEN-010)
    CAS: 1349719-98-7
    纯度: >98.50%

    (S)-JQ-35 (TEN-010) (TEN-010) 是溴结构域和末端外 (BET) 家族含溴结构域蛋白的抑制剂，具有潜在的抗肿瘤活性。

  • GC33204 structure
    GC33204GS-626510
    CAS: 1637770-13-8
    纯度: >99.50%

    GS-626510是一个有效的、且具有口服活性的BET家族的抑制剂，其对BRD2/3/4的Kd值为0.59-3.2nM，对BD1和BD2的IC50值分别为83nM和78nM。

  • GC33211 structure
    GC33211HJB97
    CAS: 2093391-24-1
    纯度: >98.00%

    HJB97是一种高亲和力BET抑制剂，Ki值分别为0.9±0.2nM(BRD2BD1)，0.27±0.09nM(BRD2BD2)，0.18±0.01nM(BRD3BD1)，0.21±0.03nM(BRD3BD2)，0.5±0.2nM(BRD4BD1)，1.0±0.1nM(BRD4BD2)。HJB97可用于开发设计PROTACBET的降解剂。具有抗肿瘤活性。

  • GC33212 structure
    GC33212GNE-207
    CAS: 2158266-58-9
    纯度: >96.00%

    GNE-207是一种有效、选择性、可口服的CBP溴结构域抑制剂，IC50值为1nM，对其选择性是的BRD4(1)的2500多倍，IC50值为3.1μM。在MV-4-11细胞中，GNE-207对MYC表达具有高效活性，EC50值为18nM。

  • GC33217 structure
    GC33217QCA570
    CAS: 2207569-08-0
    纯度: >99.50%

    QCA570是基于PROTAC技术的BET的强效降解剂，其对BRD4BD1蛋白的IC50值为10nM。

  • GC33264 structure
    GC33264Y06137
    CAS: 2226534-49-0
    纯度: >99.50%

    Y06137是一种有效的选择性BET抑制剂，可与BRD4(1)溴结构域结合，Kd值为81nM。具有抗肿瘤活性。

  • GC33280 structure
    GC33280A1874
    CAS: 2064292-12-0
    纯度: >98.00%

    A1874 is a much improved nutlin-based, BRD4-degrading PROTAC and is able to degrade its target protein by 98% with nanomolar potency.

  • GC33285 structure
    GC33285Y06036
    CAS: 1832671-96-1
    纯度: >99.00%

    Y06036 (Compound 6i) is a potent and selective inhibitor of BET with antitumor activity. Y06036 binds to the BRD4(1) bromodomain with Kd of 82 nM.

  • GC33324 structure
    GC33324GSK9311
    CAS: 1923851-49-3
    纯度: >99.00%

    GSK9311是有效的BRPF溴结构域抑制剂，对BRPF1和BRPF2的pIC50值分别为6.0和4.3。

  • GC33363 structure
    GC33363MZP-55
    CAS: 2010159-48-3
    纯度: >99.00%

    MZP-55是基于PROTAC技术的一种选择性的BRD3/4降解剂，对Brd4BD2的Kd值为8nM。

  • GC33372 structure
    GC33372PROTAC BRD9 Degrader-1
    CAS: 2097971-01-0
    纯度: >98.00%

    PROTACBRD9Degrader-1是一种先导PROTACBRD9化学降解剂，可用作研究BAF复合物的选择性探针。

  • GC33403 structure
    GC33403E-7386
    CAS: 1799824-08-0
    纯度: >98.00%

    E-7386是一种口服有效的CBP/β-连环蛋白(CBP/beta-catenin)调节剂。

  • GC34078 structure
    GC34078I-CBP112
    CAS: 1640282-31-0
    纯度: >98.00%

    A p300 and CBP inhibitor

  • GC34319 structure
    GC34319TD-428
    CAS: 2334525-50-5

    TD-428是一种高度特异的BRD4降解剂，DC50为0.32nM。

  • GC34325 structure
    GC34325PROTAC BET degrader-3
    纯度: >98.50%

    PROTACBETDegrader-3是基于PROTAC技术的BET降解剂。

  • GC34377 structure
    GC34377L-45 dihydrochloride (L-Moses dihydrochloride)

    L-45dihydrochloride是第一个有效的选择性p300/CBP相关因子(PCAF)溴结构域(Brd)抑制剂，Kd为126±15nM。