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Epigenetic Reader Domain

Items 1-50 of 554

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Catalog No.
Product Name
Application
Product Information
Citations
  1. A16859
    ARV-825

    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.
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  2. A13068
    CPI-203

    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).
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  3. A19059
    BRM/BRG1 ATP Inhibitor-1

    BRM/BRG1 ATP Inhibitor

    BRM/BRG1 ATP Inhibitor-1 is an allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are below 0.005 ?M.
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  4. A13227
    SGC-CBP30

    CBP/p300 bromodomain inhibitor

    SGC-CBP30 is a potent and selective inhibitor of CREBBP (CBP) and EP300; which are general transcriptional co-activators.
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  5. A12545
    PFI-1

    BET inhibitor

    PFI-1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4.
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  6. A11783
    GSK 1210151A (I-BET151)

    BET Bromodomain Inhibitor

    GSK1210151A is a novel selective inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2, BRD3, and BRD4.
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  7. A15856
    Foscenvivint (PRI-724)

    CBP/beta-catenin antagonist

    PRI-724 is the second-generation, potent and specific inhibitor of CBP/β-Catenin complex, and a modulator of the β-Catenin dependent canonical Wnt signaling pathway in cancer stem cells.

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  8. A20579
    JQ1 (carboxylic acid)

    BRD4 inhibitor

    JQ-1 carboxylic acid is a highly potent, selective and cell-permeable BRD4 inhibitor with IC50s of 77 nM and 33 nM for BRD4(1) and BRD4(2), respectively.
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  9. A12815
    C646

    p300/CBP inhibitor

    C646 is a selective p300/CREB-binding protein (CBP) inhibitor (Ki = 400 nM).
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  10. A12729
    (+)-JQ1

    BET Inhibitor

    (+)-JQ1 is a potent, high affinity, selective BET bromodomain inhibitor.
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  11. A14133
    GSK1324726A (I-BET726)

    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).
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  12. A12453
    GSK9311

    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.
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  13. A12474
    GNE-272

    CBP/EP300 Inhibitor

    GNE-272 is a potent and selective in vivo probe for the bromodomains of CBP/EP300 with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively.
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  14. A12531
    GSK 4027
    GSK 4027 is a chemical probe for the PCAF/GCN5 bromodomain with an pIC50 of 7.4??0.11 for PCAF in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.
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  15. A12655
    TPOP146

    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.
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  16. A12704
    SF1126

    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.
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  17. A12764
    PNZ5

    BET inhibitor

    PNZ5 is a potent and isoxazole-based pan-BET inhibitor with high selectivity and potency similar to the well-established (+)-JQ1, with a KD of 5.43 nM for BRD4(1).
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  18. A12948
    UNC1215

    L3MBTL3 inhibitor

    UNC1215 is a potent, selective antagonist of L3MBTL3 with cellular activity.
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  19. A13163
    Bromosporine

    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.
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  20. A13165
    I-CBP112

    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).
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  21. A13305
    GS-626510

    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.
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  22. A11440
    Molibresib (GSK 525762A, I-BET-762)

    BET inhibitor

    GSK-525762A is a small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family
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  23. A12141
    I-BET282

    Bromodomain inhibitor

    I-BET282 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

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  24. A13383
    IACS-9571

    TRIM24/BRPF1 inhibitor

    IACS-9571 is a potent and selective inhibitor of TRIM24 and BRPF1, with IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively.
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  25. A13451
    PF-4

    BRPF1 bromodomain inhibitor

    PFI-4 is a potent and selective and cell permeable BRPF1 bromodomain inhibitor (IC50 = 80 nM). Exhibits >100-fold selectivity for BRPF1 over a panel of other bromodomains including BRPF2 (BRD1), BRPF3 and BRD4.
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  26. A13717
    UNC 669

    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)
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  27. A13749
    MS436

    BRD4 inhibitor

    MS436 is a diazobenzene-based small-molecule inhibitor for the BRD4 bromodomains with a Ki value of 30-50 nM.
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  28. A13890
    Birabresib (OTX015)

    BET inhibitor

    OTX015 is an orally bioavailable, small molecule inhibitor of BRD2, BRD3, and BRD4 (EC50s = 10-19 nM).
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  29. A13956
    Apabetalone (RVX-208)

    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.
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  30. A13957
    PFI-3

    SMARCA bromodomains probe

    PFI-3 is a selective chemical probe for SMARCA bromodomains.
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  31. A14015
    GSK2801

    BAZ2A and BAZ2B inhibitor

    GSK2801 is a very potent inhibitor of the BAZ2 family of bromodomain containing proteins
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  32. A14134
    GSK 525768A
    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.
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  33. A14160
    (-)-JQ1

    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.
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  34. A14226
    Anacardic Acid

    KAT5 (Tip60), p300/PCAF inhibitor

    Anacardic Acid is a potent inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases.
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  35. A17014
    MZ1

    BRD4 protein degrader

    MZ1 is a potent inducer of reversible, long-lasting and selective removal of BRD4 over BRD2 and BRD3.
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  36. A17089
    E-7386

    CBP/beta-catenin modulator

    E-7386 is an orally active CBP/beta-catenin modulator.
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  37. A17175
    CF53

    BET inhibitor

    CF53 is a bromodomain and extra-terminal (BET) bromodomain Inhibitor with IC50 value of 11.7 nM.
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  38. A17180
    TP-472

    BRD9/7 inhibitor

    TP-472 is a potent BRD9/7 inhibitor with Kd of 33 and 340 nM, respectively.
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  39. A17226
    Mivebresib (ABBV-075)

    BET inhibitor

    Mivebresib, also known as ABBV-075, is a potent BET inhibitor (bromodomain (BRD)-containing proteind) with potential antineoplastic activity.
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  40. A18344
    666-15

    selective CREB inhibitor

    666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM.
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  41. A18345
    PLX51107

    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).
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  42. A18399
    ZXH-3-26

    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.
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  43. A18454
    BRD-IN-3

    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.
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  44. A15872
    I-BRD9

    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.
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  45. A15876
    PF-CBP1

    CREBBP inhibitor

    PF-CBP1 is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.
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  46. A15947
    BAZ2-ICR

    BAZ2 bromodomain inhibitor

    BAZ2-ICR is an excellent chemical probe for functional studies of the BAZ2 bromodomains in vitro and in vivo.
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  47. A16000
    OF-1

    BRPF1B/BRPF2 bromodomain inhibitor

    OF-1 is a chemical probe for BRPF bromodomains. OF-1 has been shown to bind to BRPF1B with a KD of 100 nM (ITC), to BRPF2 with a KD of 500 nM (ITC) and to BRPF3 with a KD of 2.4 uM (ITC).
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  48. A16068
    BI-7273

    BRD9 BD Inhibitor

    BI-7273 is a selective, and cell-permeable BRD9 BD inhibitor.
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  49. A16076
    Pelabresib (CPI 0610)

    BET bromodomain inhibitor

    CPI 0610 is a small molecule inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, with potential antineoplastic activity.
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  50. A16092
    GSK 5959

    BRPF1 bromodomain inhibitor

    GSK 5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with IC50 ~ 80 nM. Exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains.
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