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Home >> Signaling Pathways >> Chromatin/Epigenetics >> 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.

Products for  Epigenetic Reader Domain

  1. Cat.No. 产品名称 Information
  2. GC34377 L-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。
  3. GC34325 PROTAC BET degrader-3 PROTACBETDegrader-3是基于PROTAC技术的BET降解剂。
  4. GC34319 TD-428 TD-428是一种高度特异的BRD4降解剂，DC50为0.32nM。
  5. GC34078 I-CBP112 A p300 and CBP inhibitor
  6. GC33403 E-7386 E-7386是一种口服有效的CBP/β-连环蛋白(CBP/beta-catenin)调节剂。
  7. GC33372 PROTAC BRD9 Degrader-1 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。
  8. GC33363 MZP-55 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。
  9. GC33324 GSK9311 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。
  10. GC33285 Y06036 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.
  11. GC33280 A1874 A1874 is a much improved nutlin-based, BRD4-degrading PROTAC and is able to degrade its target protein by 98% with nanomolar potency.
  12. GC33264 Y06137 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。
  13. GC33217 QCA570 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。
  14. GC33212 GNE-207 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。
  15. GC33211 HJB97 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。
  16. GC33204 GS-626510 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。
  17. GC33198 (S)-JQ-35 (TEN-010)

    TEN-010

     (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。
  18. GC33183 L-45 (L-Moses)

    L-45

     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。
  19. GC33109 PROTAC BET Degrader-1 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。
  20. GC33104 BAY1238097 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)。
  21. GC33102 MZP-54 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。
  22. GC33042 IACS-9571 (ASIS-P040)

    ASIS-P040

     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。
  23. GC33028 CF53 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]
  24. GC33026 INCB054329 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.
  25. GC33017 BRD4 degrader AT1 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。
  26. GC33015 FL-411 (BRD4-IN-1)

    2-(4-羟基-3,5-二甲基苯基)-7-甲基-5,6,7,8-四氢吡啶并[4',3':4,5]噻吩并[2,3-D]嘧啶-4(1H)-酮,BRD4-IN-1

     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.
  27. GC32980 PROTAC BET degrader-2 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。
  28. GC32960 GNE-049 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。
  29. GC32880 TPOP146 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。
  30. GC32863 Target Protein-binding moiety 4

    Molibresib carboxylic acid; GSK525762A carboxylic acid; PROTAC BRD4-binding moiety 2

     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。
  31. GC32812 BMS-986158 A BET bromodomain inhibitor
  32. GC32798 MI-538 MI-538是menin和MLL融合蛋白相互作用的抑制剂；IC50值为21nM。
  33. GC32791 BETd-260 (ZBC 260)

    ZBC 260

     BETd-260 (ZBC 260) (ZBC 260) 是一种 PROTAC，通过 Cereblon 和 BET 的配体连接，对 RS4;11 白血病细胞系中的 BRD4 蛋白具有低至 30 pM 的作用。 BETd-260 (ZBC 260) 在肝细胞癌 (HCC) 细胞中有效抑制细胞活力并强烈诱导细胞凋亡。
  34. GC32747 GNE-272 GNE-272是有效和选择性的CBP/EP300溴结构域体内探针，对CBP，EP300和BRD4的IC50值分别为0.02，0.03和13μM。
  35. GC32719 dBET6 A PROTAC that drives BRD4 degradation
  36. GC32689 666-15

    Compound 3i

     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，IC50值为0.081±0.04μM。
  37. GC32685 ARV-771 A PROTAC that drives BET family protein degradation
  38. GC32677 A-485 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IC50值为60nM。A-485可抑制p300-BHC（溴域HAT-C/H3）和CBP-BHC结构域的活性，IC50分别为9.8nM和2.6nM。
  39. GC32081 GNE-781 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.
  40. GC31881 MS417 (GTPL7512)

    GTPL7512

    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 &#956 ;M)。
  41. GC31831 BET-IN-1 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。
  42. GC31731 GSK 4027 A PCAF/GCN5 bromodomain inhibitor
  43. GC31654 KG-501 (Naphthol AS-E phosphate)

    色酚AS-E磷酸盐,Naphthol AS-E phosphate

     An inhibitor of the protein-protein interaction between CREB and KIX domains
  44. GC31245 EML 425 An inhibitor of p300 and CBP
  45. GC30714 GSK4028 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。
  46. GC30644 INCB054329 Racemate INCB054329Racemate是BET蛋白的抑制剂。
  47. GC19455 ZL0420 A BRD4 inhibitor
  48. GC19409 ABBV-744 A BD2 bromodomain inhibitor
  49. GC19328 SF2523 A dual inhibitor of PI3K and BRD4
  50. GC19298 PLX51107 A BET family protein inhibitor
  51. GC19248 Mivebresib

    米维布塞; ABBV-075

     A BRD2, BRD4, and BRDT inhibitor

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