Epigenetic Reader Domain

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  1. BET inhibitor

    GSK-525762A is a small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family
  2. BET Bromodomain Inhibitor

    GSK1210151A is a novel selective inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2, BRD3, and BRD4.
  3. 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
  4. 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.
  5. 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.
  6. 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.
  7. BET inhibitor

    PFI-1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4.
  8. 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.
  9. 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.
  10. BET Inhibitor

    (+)-JQ1 is a potent, high affinity, selective BET bromodomain inhibitor.
  11. 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).
  12. p300/CBP inhibitor

    C646 is a selective p300/CREB-binding protein (CBP) inhibitor (Ki = 400 nM).
  13. L3MBTL3 inhibitor

    UNC1215 is a potent, selective antagonist of L3MBTL3 with cellular activity.
  14. 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).
  15. 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.
  16. 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).
  17. CBP/p300 bromodomain inhibitor

    SGC-CBP30 is a potent and selective inhibitor of CREBBP (CBP) and EP300; which are general transcriptional co-activators.
  18. 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.
  19. 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.
  20. 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.
  21. 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)
  22. BRD4 inhibitor

    MS436 is a diazobenzene-based small-molecule inhibitor for the BRD4 bromodomains with a Ki value of 30-50 nM.
  23. BET inhibitor

    OTX015 is an orally bioavailable, small molecule inhibitor of BRD2, BRD3, and BRD4 (EC50s = 10-19 nM).
  24. 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.
  25. SMARCA bromodomains probe

    PFI-3 is a selective chemical probe for SMARCA bromodomains.
  26. BAZ2A and BAZ2B inhibitor

    GSK2801 is a very potent inhibitor of the BAZ2 family of bromodomain containing proteins
  27. 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).
  28. 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.
  29. 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.
  30. KAT5 (Tip60), p300/PCAF inhibitor

    Anacardic Acid is a potent inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases.
  31. MBT Domain (L3MBTL1) Inhibitor

    UNC 926 is a methyl lysine reader domain inhibitor.
  32. 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.
  33. 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.
  34. BAZ2 bromodomain inhibitor

    BAZ2-ICR is an excellent chemical probe for functional studies of the BAZ2 bromodomains in vitro and in vivo.
  35. 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).
  36. BRD9 BD Inhibitor

    BI-7273 is a selective, and cell-permeable BRD9 BD inhibitor.
  37. BET bromodomain inhibitor

    CPI 0610 is a small molecule inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, with potential antineoplastic activity.
  38. 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.
  39. CBP/p300 inhibitor

    EML 425 is a reversible and non-competitive CBP/p300 inhibitor that is cell permeable (IC50 values are 1.1 and 2.9 uM, respectively).
  40. 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).
  41. BRPF1 bromodomain inhibitor

    GSK6853 is a potent and selective inhibitor of the BRPF1 bromodomain. shows excellent BRPF1 potency (pKd 9.5) and greater than 1600-fold selectivity over all other bromodomains tested.
  42. TAF1 inhibitor

    CeMMEC13 is an isoquinolinone that selectively inhibits the second bromodomain of TAF1 (IC50 = 2.1 μM).
  43. BRD4 inhibitor

    OXF BD 02, selective inhibitor of the first bromodomain of BRD4 (BRD4(1)) (IC50 = 382 nM). Exhibits 2-3-fold selectivity for BRD4(1) over the CBP bromodomain and has little affinity for a range of other bromodomains.
  44. BET Inhibitor

    GW841819X is an analogue of (+)-JQ1 and a novel inhibitor of BET bromodomains. GW841819X was a single enantiomer but of undefined chirality at the 4-position of the benzodiazepine ring 3.
  45. BET inhibitor

    BET-BAY 002 is a potent BET inhibitor; shows efficacy in a multiple myeloma model.
  46. CBP/EP300 bromodomain inhibitor

    CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor.
  47. BRD4 inhibitor

    ZL0420 is a potent and selective BRD4 inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2 respectively and good selectivity over that of the related BRD2 homolog.
  48. 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.
  49. 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.
  50. BRD4 protein degrader

    dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM.

Items 1-50 of 129

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