Epigenetic Reader Domain

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.

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  1. 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. Learn More
  2. BMS-986158

    Catalog No. A19442
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    Bromodomain inhibitor
    BMS-986158 is an inhibitor of the bromodomain and extra-terminal (BET) proteins. Learn More
  3. MS417

    Catalog No. A19433
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    BRD4 inhibitor
    MS417 is a BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC50, 32.7 μM). Learn More
  4. MZP-54

    Catalog No. A19426
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    BRD3/4 degrader
    MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 4 nM for Brd4BD2. Learn More
  5. MZP-55

    Catalog No. A19415
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    BRD3/4 degrader
    MZP-55 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 8 nM for Brd4BD2. Learn More
  6. dBET57

    Catalog No. A19133
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    BRD4BD1degrader
    dBET57 is a potent and selective degrader of BRD4BD1 based on the PROTAC technology. Learn More
  7. CD235

    Catalog No. A19115
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    BET bromodomain inhibitor
    CD235 is a structurally similar analogue of CD161. CD161 is a potent and orally bioavailable BET bromodomain inhibitor. Learn More
  8. 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. Learn More
  9. 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 . Learn More
  10. 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. Learn More
  11. 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. Learn More
  12. 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 Learn More
  13. 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. Learn More
  14. (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. Learn More
  15. INCB054329 Racemate

    Catalog No. A21609
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    BET protein inhibitor
    INCB054329 Racemate is a BET protein inhibitor. Learn More
  16. 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. Learn More
  17. 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. Learn More
  18. 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. Learn More
  19. (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. Learn More
  20. GSK 1210151A (I-BET151)

    Catalog No. A11783
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    BET Bromodomain Inhibitor
    GSK1210151A is a novel selective inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2, BRD3, and BRD4. Learn More
  21. PFI-1

    Catalog No. A12545
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    BET inhibitor
    PFI-1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4. Learn More
  22. GSK 525762A (I-BET-762)

    Catalog No. A11440
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    BET inhibitor
    GSK-525762A is a small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family Learn More
  23. CPI-203

    Catalog No. A13068
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    BET bromodomain Inhibitor
    CPI203 is a novel potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family protein BRD4 with an IC50 of ~37 nM (BRD4 α-screen assay). Learn More
  24. Bromosporine

    Catalog No. A13163
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    bromodomain inhibitor
    Bromosporine is a broad spectrum inhibitor for bromodomains with IC50 of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM for BRD2, BRD4, BRD9 and CECR2, respectively. Learn More
  25. UNC 669

    Catalog No. A13717
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    L3MBTL inhibitor
    UNC669 is a small-molecule antagonist of methyl-lysine (KMe) reader protein with selectivity for L3MBTL1 and L3MBTL3 (IC50 of 4.2μM and 3.1μM respectively) Learn More
  26. (+)-JQ1

    Catalog No. A12729
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    BET Inhibitor
    (+)-JQ1 is a potent, high affinity, selective BET bromodomain inhibitor. Learn More
  27. SGC-CBP30

    Catalog No. A13227
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    CBP/p300 bromodomain inhibitor
    SGC-CBP30 is a potent and selective inhibitor of CREBBP (CBP) and EP300; which are general transcriptional co-activators. Learn More
  28. OTX015

    Catalog No. A13890
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    BET inhibitor
    OTX015 is an orally bioavailable, small molecule inhibitor of BRD2, BRD3, and BRD4 (EC50s = 10-19 nM). Learn More
  29. UNC1215

    Catalog No. A12948
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    L3MBTL3 inhibitor
    UNC1215 is a potent, selective antagonist of L3MBTL3 with cellular activity. Learn More
  30. 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. Learn More
  31. 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. Learn More
  32. BI-9564

    Catalog No. A16196
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    BRD7/9 inhibitor
    BI-9564 is a potent and selective inhibitor of BRD9 and BRD7 bromodomains (Kds = 14.1 and 239 nM; IC50s = 75 nM and 3.4 uM, respectively). Learn More
  33. BI-7273

    Catalog No. A16068
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    BRD9 BD Inhibitor
    BI-7273 is a selective, and cell-permeable BRD9 BD inhibitor. Learn More
  34. I-BRD9

    Catalog No. A15872
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    Selective BRD9 inhibitor
    I-BRD9 is a potent and selective BRD9 inhibitor with pIC50 of 7.3, while it displayed a pIC50 of 5.3 against BRD4. Learn More
  35. MS436

    Catalog No. A13749
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    BRD4 inhibitor
    MS436 is a diazobenzene-based small-molecule inhibitor for the BRD4 bromodomains with a Ki value of 30-50 nM. Learn More
  36. I-CBP112

    Catalog No. A13165
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    CBP/p300 bromodomain inhibitor
    I-CBP112 is a highly potent and selective p300/CBP bromodomain inhibitor (IC50 ~0.14-0.17 uM for CBP and ~0.625 uM for p300). Learn More
  37. CF53

    Catalog No. A17175
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    BET inhibitor
    CF53 is a bromodomain and extra-terminal (BET) bromodomain Inhibitor with IC50 value of 11.7 nM. Learn More
  38. TP-472

    Catalog No. A17180
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    BRD9/7 inhibitor
    TP-472 is a potent BRD9/7 inhibitor with Kd of 33 and 340 nM, respectively. Learn More
  39. E-7386

    Catalog No. A17089
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    CBP/beta-catenin modulator
    E-7386 is an orally active CBP/beta-catenin modulator. Learn More
  40. dBET1

    Catalog No. A16858
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    BRD4 protein degrader
    dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM. Learn More
  41. ARV-825

    Catalog No. A16859
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    BRD4 Inhibitor
    ARV-825 is a hetero-bifunctional molecule that is composed of a BRD4 binding moiety joined to an E3 ligase cereblon binding moiety using proteolysis targeting chimera (PROTAC) technology. Learn More
  42. HJB-97

    Catalog No. A16872
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    BET bromodomian inhibitor
    HJB-97 is a potent BET bromodomian inhibitor. It acts by targeting BRD2/3/4 BD1 and BD2. Learn More
  43. BAY1238097

    Catalog No. A16881
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    BET inhibitor
    BAY1238097 is a potent and selective BET inhibitor. BAY1238097 binds to the acetylated lysine recognition motifs on the BRD of BET proteins, thereby preventing the interaction between BET proteins and histones. Learn More
  44. ABBV-744

    Catalog No. A16831
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    BET bromodomain inhibitor
    ABBV-744 is a BDII-selective BET bromodomain inhibitor that is being investigated to treat AML and metastic castration-resistant prostate cancer. Learn More
  45. A-485

    Catalog No. A16830
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    p300/CBP inhibitor
    A-485 is a potent and selective HAT inhibitor of p300/CBP in vitro with an IC50 of 10 nM in a p300 TR-FRET assay and 3 nM in a CBP TR-FRET assay with selectivity > 1000-fold over closely related HATs. Learn More
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    MZ1

    Catalog No. A17014
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    BRD4 protein degrader
    MZ1 is a potent inducer of reversible, long-lasting and selective removal of BRD4 over BRD2 and BRD3. Learn More
  46. PLX51107

    Catalog No. A18345
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    selective BET inhibitor
    PLX51107 is a potent and selective BET inhibitor, with Kds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively; PLX51107 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range). Learn More
    • New

    Mivebresib (ABBV-075)

    Catalog No. A17226
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    BET inhibitor
    Mivebresib, also known as ABBV-075, is a potent BET inhibitor (bromodomain (BRD)-containing proteind) with potential antineoplastic activity. Learn More
  47. BRD7-IN-1 free base

    Catalog No. A21530
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    BRD7-IN-1 free base, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC50s of 4.5 and 1.8 nM, respectively). Learn More
  48. TPOP146

    Catalog No. A12655
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    CBP/P300 benzoxazepine bromodomain inhibitor
    TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4. Learn More

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