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. 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
  2. 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
  3. BI-9564

    Catalog No. A16196
    Quick View
    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
  4. 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
  5. 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
  6. (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
  7. 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
  8. 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
  9. 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
  10. 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
  11. 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
  12. 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
  13. 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
  14. 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
  15. 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
  16. 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
  17. 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
  18. 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
  19. 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
  20. (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
  21. INCB054329 Racemate

    Catalog No. A21609
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    BET protein inhibitor
    INCB054329 Racemate is a BET protein inhibitor. Learn More
  22. 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
  23. 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
  24. 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
  25. 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
  26. 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
  27. 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
  28. UNC1215

    Catalog No. A12948
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    L3MBTL3 inhibitor
    UNC1215 is a potent, selective antagonist of L3MBTL3 with cellular activity. Learn More
  29. 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
  30. 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
  31. (+)-JQ1

    Catalog No. A12729
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    BET Inhibitor
    (+)-JQ1 is a potent, high affinity, selective BET bromodomain inhibitor. Learn More
  32. 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
  33. 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
  34. 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
  35. 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
  36. 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
  37. (-)-JQ1

    Catalog No. A14160
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    BET bromodomain inhibitor
    The bromodomain and extra terminal domain (BET) family of proteins, including BRD2, BRD3, and BRD4, play a key role in many cellular processes, including inflammatory gene expression, mitosis, and viral/host interaction by controlling the assembly of histone acetylation-dependent chromatin complexes. Learn More
  38. UNC 926 hydrochloride

    Catalog No. A15367
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    MBT Domain (L3MBTL1) Inhibitor
    UNC 926 is a methyl lysine reader domain inhibitor. Learn More
  39. P300/CBP-IN-3

    Catalog No. A18544
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    p300/CBP histone acetyltransferase inhibitor
    P300/CBP-IN-3, a p300/CBP histone acetyltransferase inhibitor. Learn More
  40. BRD-IN-3

    Catalog No. A18454
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    BRD inhibitor
    BRD-IN-3 ((R,R)-36n) is a highly potent PCAF bromodomain (BRD) inhibitor, with an IC50 of 7 nM. BRD-IN-3 also exhibits activity against GCN5 and FALZ. Learn More
  41. Apabetalone (RVX-208)

    Catalog No. A13956
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    BET bromodomain inhibitor
    RVX-208 is a potent BET bromodomain inhibitor with IC50 of 0.510 uM for BD2, about 170-fold selectivity over BD1. Learn More
  42. GNE-049

    Catalog No. A20206
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    CBP inhibitor
    GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively. Learn More
  43. PFI-3

    Catalog No. A13957
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    SMARCA bromodomains probe
    PFI-3 is a selective chemical probe for SMARCA bromodomains. Learn More
  44. Anacardic Acid

    Catalog No. A14226
    KAT5 (Tip60), p300/PCAF inhibitor
    Anacardic Acid is a potent inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases. Learn More
  45. GSK 525768A

    Catalog No. A14134
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    GSK 525768A is the enantiomer compound of GSK 525762A, which is a potent small molecule inhibitor that disrupt the function of the BET family of bromodomains (Brd2, Brd3, and Brd4); GSK 525768A has NO activity towards BET. Learn More
  46. GSK1324726A (I-BET726)

    Catalog No. A14133
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    BET inhibitor
    GSK1324726A (I-BET726) is a novel, potent, and selective small molecule inhibitor of BET proteins with high affinity to BRD2 (IC50= 41 nM), BRD3 (IC50= 31 nM), and BRD4 (IC50= 22 nM). Learn More
  47. ZEN-3219

    Catalog No. A19367
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    BET inhibitor
    ZEN-3219 is a BET inhibitor with IC50s of 0.48, 0.16 and 0.47 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3219 can be used to form PROTACs to induce degradation of BRD4. Learn More
  48. GSK2801

    Catalog No. A14015
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    BAZ2A and BAZ2B inhibitor
    GSK2801 is a very potent inhibitor of the BAZ2 family of bromodomain containing proteins Learn More
  49. GNE-207

    Catalog No. A18844
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    CBP bromodomain inhibitor
    GNE-207 is a novel, potent, and orally bioavailable inhibitor of the bromodomain of CBP. GNE-207 has excellent CBP potency (CBP IC50?=?1?nM, MYC EC50?=?18?nM), and it exhibits a good pharmacokinetic profile. Learn More
  50. SF1126

    Catalog No. A12704
    Pan PI3K inhibitor
    SF1126 is a water soluble, small-molecule prodrug containing the pan-PI3K/mTOR inhibitor LY294002/SF1101 conjugated to the RGD-containing tetra-peptide SF1174 with potential antineoplastic and antiangiogenic activities. Learn More

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