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Epigenetic Reader Domain

Inhibitory Selectivity

Catalog No.Inhibitor Name Epigenetic Reader Domain
A12729(*)-JQ1
***
A11783I-BET151
*
A12545PFI-1
**
A11440I-BET-762
***
A13956RVX-208
*
A13227SGC-CBP30
****
A13163Bromosporine
****
A13890OTX015
****
A12948UNC1215
**
A13717UNC669
*
A14133GSK1324726A
***
A13749MS436
**
A13068CPI-203
***
A13957PFI-3

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

产品 51 到 81 共 81个

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  1. BETd-246
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    BETd-246

    Catalog No. A18913
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    BRD inhibitor
    BETd-246 is a second-generation BET bromodomain (BRD) inhibitor, exhibiting superior selectivity, potency and antitumor activity. 了解更多
  2. Bromodomain IN-1
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    Bromodomain IN-1

    Catalog No. A18845
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    Bromodomain inhibitor
    Bromodomain IN-1 is a Bromodomain inhibitor extracted from patent WO2016069578A1, compound 4 . 了解更多
  3. BRD4 Inhibitor-10
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    BRD4 Inhibitor-10

    Catalog No. A18679
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    BRD4-BD1 inhibitor
    BRD4 Inhibitor-10 is a potent BRD4-BD1 inhibitor extracted from patent WO2015022332A1, Compound II-25, has an IC50 of 8 nM. 了解更多
  4. GSK9311
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    GSK9311

    Catalog No. A12453
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    inhibitor of the BRPF bromodomain
    GSK9311 is a potent inhibitor of the BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively. 了解更多
  5. BET-IN-1
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    BET-IN-1

    Catalog No. A12141
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    bromodomain inhibitor
    BET-IN-1 is a bromodomain inhibitor extracted from patent WO/2013024104A1, compound example 2, has a plC50 in the range 6.0 - 7.0. IC50 value: 6.0 - 7.0 (plC50) Target: bromodomain 了解更多
  6. GS-626510
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    GS-626510

    Catalog No. A13305
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    BET family bromodomains inhibitor
    GS-626510 is a potent, and orally bioavailable BET family bromodomains inhibitor, with Kd values of 0.59-3.2 nM for BRD2/3/4, with IC50 values of 83 nM and 78 nM foe BD1 and BD2, respectively. 了解更多
  7. (Rac)-BAY1238097
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    (Rac)-BAY1238097

    Catalog No. A21598
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    BET inhibitor
    (Rac)-BAY1238097 is a BET inhibitor, with an IC50 of 1.02 μM for BRD4. Used in cancer research. 了解更多
  8. INCB054329 Racemate
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    INCB054329 Racemate

    Catalog No. A21609
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    BET protein inhibitor
    INCB054329 Racemate is a BET protein inhibitor. 了解更多
  9. CPI-0610 carboxylic acid
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    CPI-0610 carboxylic acid

    Catalog No. A21714
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    BET inhibitor
    CPI-0610 carboxylic acid is a potent bromodomain and extra-terminal (BET) protein inhibitor. CPI-0610 carboxylic acid has the potential in the therapy of multiple myeloma. 了解更多
  10. AZD5153 6-Hydroxy-2-naphthoic acid
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    AZD5153 6-Hydroxy-2-naphthoic acid

    Catalog No. A21852
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    BET/BRD4 bromodomain inhibitor
    AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM. 了解更多
  11. Molibresib besylate
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    Molibresib besylate

    Catalog No. A21855
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    BET bromodomain inhibitor
    Molibresib besylate (GSK 525762C; I-BET 762 besylate) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM. 了解更多
  12. GSK 1210151A (I-BET151)
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    GSK 1210151A (I-BET151)

    Catalog No. A11783
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    BET Bromodomain 抑制剂
    GSK 1210151A (I-BET151)是溴结构域和额外末端（BET）家族蛋白BRD2，BRD3和BRD4的新型选择性抑制剂。 了解更多
  13. PFI-1
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    PFI-1

    Catalog No. A12545
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    BET 抑制剂
    PFI-1是BET溴结构域抑制剂，对BRD2和BRD4表现出抑制活性。 了解更多
  14. GSK 525762A (I-BET-762)
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    GSK 525762A (I-BET-762)

    Catalog No. A11440
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    BET 抑制剂
    GSK 525762A (I-BET-762)是BET(溴域和末端外)家族的小分子抑制剂。 了解更多
  15. CPI-203
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    CPI-203

    Catalog No. A13068
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    BET bromodomain 抑制剂
    CPI203是溴结构域和额外末端（BET）家族蛋白BRD4的新型有效，选择性和细胞渗透性抑制剂，IC50为?37 nM（BRD4α筛选试验）。 了解更多
  16. Bromosporine
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    Bromosporine

    Catalog No. A13163
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    bromodomain 抑制剂
    Bromosporine是一种针对溴结构域的广谱抑制剂，对于BRD2，BRD4，BRD9和CECR2的IC50分别为0.41μM，0.29μM，0.122μM和0.017μM。 了解更多
  17. UNC 669
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    UNC 669

    Catalog No. A13717
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    L3MBTL 抑制剂
    UNC669是L3MBTL1和L3MBTL3的抑制剂,对L3MBTL1和L3MBTL3具有选择性（IC50分别为4.2μM和3.1μM）。 了解更多
  18. (+)-JQ1
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    (+)-JQ1

    Catalog No. A12729
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    BET 抑制剂
    (+)-JQ1是有效的，高亲和力的选择性BET溴结构域抑制剂。 了解更多
  19. SGC-CBP30
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    SGC-CBP30

    Catalog No. A13227
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    CBP/p300 bromodomain 抑制剂
    SGC-CBP30是一种有效且选择性的CREBBP（CBP）和EP300抑制剂，无细胞试验中IC50分别为21 nM和38 nM。它们是一般的转录共激活因子。 了解更多
  20. OTX015
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    OTX015

    Catalog No. A13890
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    BET 抑制剂
    OTX015是口服可生物利用的BRD2，BRD3和BRD4的小分子抑制剂（EC50s = 10-19 nM）。 了解更多
  21. UNC1215
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    UNC1215

    Catalog No. A12948
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    L3MBTL3 抑制剂
    UNC1215是具有细胞活性的L3MBTL3的强效选择性拮抗剂。 了解更多
  22. I-CBP112
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    I-CBP112

    Catalog No. A13165
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    CBP/p300 bromodomain 抑制剂
    I-CBP112是一种高效且选择性的p300/CBP溴结构域抑制剂（对于CBP，IC50为?0.14-0.17 uM，对于p300为?0.625 uM）。 了解更多
  23. MS436
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    MS436

    Catalog No. A13749
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    BRD4 抑制剂
    MS436是用于BRD4溴结构域的重氮基小分子抑制剂，Ki值为30-50 nM。 了解更多
  24. I-BRD9
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    I-BRD9

    Catalog No. A15872
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    Selective BRD9 抑制剂
    I-BRD9是一种有效的选择性BRD9抑制剂，pIC50为7.3，而对BRD4的pIC50为5.3。 了解更多
  25. BI-7273
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    BI-7273

    Catalog No. A16068
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    BRD9 BD 抑制剂
    BI-7273是一种选择性的，细胞可渗透的BRD9 BD抑制剂。 了解更多
  26. BI-9564
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    BI-9564

    Catalog No. A16196
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    BRD7/9 抑制剂
    BI-9564是BRD9和BRD7溴结构域的有效和选择性抑制剂（Kds分别为14.1和239 nM；IC50分别为75 nM和3.4 uM）。 了解更多
  27. VZ185
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    VZ185

    Catalog No. A18685
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    dual BRD7/9 PROTAC degrader
    VZ185 is a potent, fast, and selective dual BRD7/9 PROTAC degrader with DC50s of 4.5 and 1.8 nM, respectively. 了解更多
  28. ZXH-3-26
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    ZXH-3-26

    Catalog No. A18399
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    PROTAC BRD4 degrader
    ZXH-3-26 is a selective PROTAC BRD4 degrader with a DC50/5h (DC50/5h referring to half-maximal degradation after 5 hours of treatment) of ~ 5 nM. 了解更多
  29. (E)-ZL0420
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    (E)-ZL0420

    Catalog No. A20136
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    BRD4 inhibitor
    ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2. 了解更多
  30. ZL0454
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    ZL0454

    Catalog No. A20123
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    BRD4 inhibitor
    ZL0454 is a potent and selective Bromodomain-containing protein 4 (BRD4) inhibitor with an IC50 of 49 and 32 nM for BD1 and BD2. 了解更多
  31. BMS-986158
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    BMS-986158

    Catalog No. A19442
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    Bromodomain inhibitor
    BMS-986158 is an inhibitor of the bromodomain and extra-terminal (BET) proteins. 了解更多

产品 51 到 81 共 81个

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作用机制
  1. Inhibitor (抑制剂) (70)
  2. Modulator (调节剂) (1)
  3. Degrader (降解剂) (7)
靶点
  1. BAZ2A (2)
  2. BAZ2B (2)
  3. BET (5)
  4. BRD2 (7)
  5. BRD3 (4)
  6. BRD4 (9)
  7. BRD7 (1)
  8. BRD9 (4)
  9. BRPF1 (4)
  10. BRPF2 (1)
  11. CECR2 (1)
  12. KAT5 (Tip60) (1)
  13. L3MBTL (2)
  14. L3MBTL1 (1)
  15. p300/CBP (7)
  16. PCAF (1)
  17. SMARCA4 (1)
  18. TAF1 (1)
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