2. Signaling Pathways
  3. Epigenetics
  4. Epigenetic Reader Domain

Epigenetic Reader Domain

Epigenetic Reader Domain

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Epigenetic regulators of gene expression and chromatin state include so-called writers, erasers, and readers of chromatin modifications.Well-characterized examples of reader domains include bromodomains typically binding acetyllysine and chromatin organization modifier (chromo), malignant brain tumor (MBT), plant homeodomain (PHD), and Tudor domains generally associating with methyllysine. Research on epigenetic readers has been tremendously influenced by the discovery of selective inhibitors targeting the bromodomain and extraterminal motif (BET) family of acetyl-lysine readers. The human genome encodes 46 proteins containing 61 bromodomains clustered into eight families. Distinct experimental approaches are used to identify the first BET inhibitors, GSK 525762A and (+)-JQ-1.

The Polycomb group (PcG) protein, enhancer of zeste homologue 2 (EZH2), has an essential role in promoting histone H3 lysine 27 trimethylation (H3K27me3) and epigenetic gene silencing. This function of EZH2 is important for cell proliferation and inhibition of cell differentiation, and is implicated in cancer progression. Cyclin-dependent kinases regulate epigenetic gene silencing through phosphorylation of EZH2. In many types of cancers including lymphomas and leukemia, EZH2 is postulated to exert its oncogenic effects via aberrant histone and DNA methylation, causing silencing of tumor suppressor genes.

p300/CBP is not only a transcriptional adaptor but also a histone acetyltransferase.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-111875
    SNIPER(BRD)-1
    		Inhibitor 99.68%
    SNIPER(BRD)-1 is a SNIPER degrader of BRD4, cIAP1 and XIAP. SNIPER(BRD)-1 has IC50 values of 6.8 nM, 17 nM and 49 nM for cIAP1, cIAP2 and XIAP, respectively. SNIPER(BRD)-1 can be used for cancer research.
    SNIPER(BRD)-1
  • HY-136920
    CBP/p300-IN-8
    		Inhibitor 98.03%
    CBP/p300-IN-8 is a potent inhibitor of the CBP/P300 family of bromodomains. CBP/p300-IN-8 inhibits CBP (IC50=0.01-0.1 µΜ) and BRD4 (IC50=1-1000 µΜ) activity.
    CBP/p300-IN-8
  • HY-132197
    CBP/p300-IN-12
    		Inhibitor 99.72%
    CBP/p300-IN-12 is a potent and selective covalent histone acetyltransferases p300 (IC50 of 166 nM) and CBP inhibitor. CBP/p300-IN-12 decreases the levels of H3K27Ac of PC-3 cells (EC50 of 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450.
    CBP/p300-IN-12
  • HY-145260
    BRD4/CK2-IN-1
    		Inhibitor 98.21%
    BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)
    BRD4/CK2-IN-1
  • HY-131061
    BET bromodomain inhibitor 1
    		Inhibitor 99.67%
    BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity.
    BET bromodomain inhibitor 1
  • HY-123911
    dBET23
    		Inhibitor
    dBET23 is a highly effective and selective PROTAC BRD4 degrader with a DC50/5h of ~ 50 nM for BRD4BD1 protein.
    dBET23
  • HY-117491
    BRD4 Inhibitor-10
    		Inhibitor 99.52%
    BRD4 Inhibitor-10 (Compound II-25) is a potent BRD4-BD1 inhibitor with an IC50 of 8 nM. BRD4 Inhibitor-10 can be used to study diseases caused by abnormal or excessive cell proliferation, such as cancer.
    BRD4 Inhibitor-10
  • HY-139148
    UMB298
    		Inhibitor 99.28%
    UMB298 is a potent and selective CBP/P300 bromodomain inhibitor.
    UMB298
  • HY-123621
    GNE-375
    		Inhibitor 99.93%
    GNE-375 is a potent and highly selective BRD9 inhibitor with an IC50 of 5 nM. GNE-375 shows >100-fold selective for BRD9 over BRD4, TAF1, and CECR2. GNE-375 decreases BRD9 binding to chromatin.
    GNE-375
  • HY-104067
    Naphthol AS-MX phosphate
    		Inhibitor 99.50%
    Naphthol AS-MX phosphate (NASTRp) is a small molecule inhibitor of the CREB (cyclic adenosine phosphate reaction element binding protein)-CBP (CREB binding protein) transcription factor complex. Naphthol AS-MX phosphate shows antitumor activity against lung cancer cells, inhibiting tumor cell proliferation (IC50=3.701 μmol/L), colony formation, and anchored independent growth in soft AGAR. Naphthol AS-MX phosphate can be used in the study of KRAS mutated lung cancer, especially for KRAS mutated lung cancer with poor chemotherapy resistance and prognosis.
    Naphthol AS-MX phosphate
  • HY-104068
    Naphthol AS-E
    		Inhibitor 98.0%
    Naphthol AS-E is a potent and cell-permeable inhibitor of KIX-KID interaction. Naphthol AS-E directly binds to the KIX domain of CBP (Kd:8.6 μM), blocks the interaction between the KIX domain and the KID domain of CREB with IC50 of 2.26 μM. Naphthol AS-E can be used for cancer research.
    Naphthol AS-E
  • HY-146208
    BRD4 Inhibitor-20
    		Inhibitor 99.24%
    BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer.
    BRD4 Inhibitor-20
  • HY-151593
    dBRD4-BD1
    		Inhibitor 98.02%
    dBRD4-BD1 is a selective and durable BRD4 degrader with an DC50 value of 280 nM (Dmax=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1.
    dBRD4-BD1
  • HY-112316B
    (Rac)-BAY1238097
    		Inhibitor 99.67%
    (Rac)-BAY1238097 is a BET inhibitor, with an IC50 of 1.02 μM for BRD4. Used in cancer research.
    (Rac)-BAY1238097
  • HY-133136
    PROTAC BRD4 Degrader-2
    		Inhibitor 98.30%
    PROTAC BRD4 Degrader-2 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC50 of 14.2 nM against BRD4 BD1.
    PROTAC BRD4 Degrader-2
  • HY-109050
    Alobresib
    		Inhibitor 98.04%
    Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc. Alobresib can be used in the metastatic castration-resistant prostate cancer (mCRPC) research.
    Alobresib
  • HY-114228
    PROTAC BET degrader-2
    		Inhibitor 98.21%
    PROTAC BET degrader-2 is a PROTAC connected by ligands for Cereblon and BET with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.
    PROTAC BET degrader-2
  • HY-145264
    OARV-771
    		Inhibitor 98.77%
    OARV-771 is a VHL-based BET degrader (PROTAC) with improved cell permeability. OARV-771 shows DC50s of 6, 1, and 4 nM for Brd4, Brd2 and Brd3, respectively.
    OARV-771
  • HY-112377
    MZP-55
    		Inhibitor 99.94%
    MZP-55 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 BD2, with a Kd of 8 nM.
    MZP-55
  • HY-133738
    M-808
    		Inhibitor 98.72%
    M-808 is a highly potent and efficacious covalent Menin-MLL interaction inhibitor, with a binding IC50 value of 2.6 nM.
    M-808
Cat. No. Product Name / Synonyms Application Reactivity