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-139861
    CBP/p300-IN-14
    		Inhibitor
    CBP/p300-IN-14 is a potent inhibitor of CBP/EP300 (lysine acetyltransferase) with an IC50 of 3.3 nM (extracted from patent WO2021213521A1, compound 27).
    CBP/p300-IN-14
  • HY-169994
    BC13
    		Inhibitor
    BC13 is a CDK6/BRD4 inhibitor with the IC50 values of 234 nM and 36 nM for CDK6 and BRD4, respectively. BC13 shows antiproliferative activity and induces cell apoptosis and DNA damage. BC13 increases in ROS levels.
    BC13
  • HY-142954
    UNC6212 (Kme2)
    		Inhibitor
    UNC6212 (Kme2), a dimethyllysine (Kme2)-containing ligand, has a KD for CBX5 of 5.7 μM.
    UNC6212 (Kme2)
  • HY-163811
    BRD9 Degrader-4
    		Inhibitor
    BRD9 Degrader-4 (BRD9c), a bifunctional molecular glue, is a potent BRD9 degrader with a DC50 of ≤25 nM. BRD9 Degrader-4 has anti-cancer effects.
    BRD9 Degrader-4
  • HY-183825
    Eleven-Nineteen-Leukemia Protein IN-4
    		Inhibitor
    Eleven-Nineteen-Leukemia Protein IN-4 is a ENL YEATS domain inhibitor with an IC50 of 62.0 nM and a Kd of 100.4 nM. Eleven-Nineteen-Leukemia Protein IN-4 downregulates MYC expression and inhibits cancer cell growth; it exerts a synergistic effect with the bromodomain inhibitor JQ-1 (HY-13030). Eleven-Nineteen-Leukemia Protein IN-4 can be used in the research of acute myeloid leukemia.
    Eleven-Nineteen-Leukemia Protein IN-4
  • HY-145431
    (S)-GSK1379725A
    		Inhibitor
    (S)-GSK1379725A (compound AU1) is a selective bromodomain and PHD finger containing transcription factor (BPTF) bromodomain inhibitor with a Kd of 2.8 μM. (S)-GSK1379725A shows to be selective for BPTF over BRD4 bromodomain. (S)-GSK1379725A shows antimalarial activity.
    (S)-GSK1379725A
  • HY-161494
    XYD190
    		Inhibitor
    XYD190 (Compound 14g) is an orally active degrader for CBP/p300. XYD190 inhibits CBP/p300 bromodomain with IC50 of 483.7 nM. XYD190 exhibits antitumor activity against acute myeloid leukemia. (Structure: Pink, CBP/p300 ligand 4 (HY-161495); Blue, E3 ligase ligand (HY-14658); Black: linker (HY-161496)).
    XYD190
  • HY-176391
    Ad-JQ1
    		Inhibitor
    Ad-JQ1 (Compound 16) is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for BRD4 (HY-78695) and a PROTAC linker (HY-176390), which recruits E3 ligases. Ad-JQ1 can be used for synthesis of PROTAC β-NF-JQ1 (HY-130256).
    Ad-JQ1
  • HY-183992
    CZL-149
    		Inhibitor
    CZL-149 is an orally active dual BET and p300/CBP bromodomains inhibitor with IC50s of 13 nM and 10.5 nM for BED4 BD1 and p300, respectively. CZL-149 reduces c-Myc and H3K27Ac levels. CZL-149 has good drug-like properties and metabolic characteristics, as well as good safety. CZL-149 can be used for the study of multiple myeloma.
    CZL-149
  • HY-160261S
    EP300/CBP-IN-2
    		Inhibitor
    EP300/CBP-IN-2 is a potent EP300/CBP inhibitor that has good activity in vivo. EP300/CBP-IN-2 can be used for the research of cancer.
    EP300/CBP-IN-2
  • HY-147571
    BET-IN-9
    		Inhibitor
    BET-IN-9 is a BET inhibitor extracted from patent WO2022012456A1, compound example 1.
    BET-IN-9
  • HY-143299
    BRD4-BD1-IN-1
    		Inhibitor
    BRD4-BD1-IN-1 (Compound 9a) is a BRD4-BD1 inhibitor with an IC50 of 38.20 μM.
    BRD4-BD1-IN-1
  • HY-138623
    GSK789
    		Inhibitor
    GSK789 is a selective inhibitor of BET BD1. GSK789 inhibits the growth of leukemia cell lines. GSK789 inhibits LPS-stimulated production of MCP-1, TNFα and IL-6 in human whole blood. GSK789 exhibits antiproliferative, anti-inflammatory and immunomodulatory activities. GSK789 can be used in research related to cancers such as leukemia, as well as inflammatory and immune diseases.
    GSK789
  • HY-160286
    BI-7190
    		Inhibitor
    BI-7190 is a selective BPTF inhibitor (Kd = 3.5 nM). BI-7190 can be used in the research of cancer.
    BI-7190
  • HY-179606
    RWT9996
    		Inhibitor
    RWT9996 is a balanced GPR17 antagonist. RWT9996 has an inhibitory effect on G protein activation and β-arrestin-2 recruitment induced by MDL-29951. RWT9996 inhibits the phosphorylation of ERK/CREB and the accumulation of inositol phosphate (b IP1) induced by MDL-29951. RWT9996 can be used for the study of neurological diseases.
    RWT9996
  • HY-160634
    BRD4 Inhibitor-31
    		Inhibitor
    BRD4 Inhibitor-31 (Example 136) is a BRD4 inhibitor (Kis: 0.234 μM and 0.295 μM for BRD4 BD1 and BRD4 BD2 respectively). BRD4 Inhibitor-31 can be used for research of inflammatory diseases, cancer, and AIDS.
    BRD4 Inhibitor-31
  • HY-155229
    CBP/p300-IN-21
    		Inhibitor
    CBP/p300-IN-21 (Compound 5d) is a selective CBP/p300 inhibitor (IC50: 0.07 and 1.755 μM for p300 and CBP). CBP/p300-IN-21 decreases H3K18Ac level. CBP/p300-IN-21 inhibits growth of 4T1 tumor growth in mice.
    CBP/p300-IN-21
  • HY-178697
    DC-BPi-07
    		Inhibitor
    DC-BPi-07 is a selective BPTF inhibitor with an IC50 value of 16.0 nM against BPTF-H4. DC-BPi-07 can be used in the research of leukemia.
    DC-BPi-07
  • HY-180490
    eIF3e-IN-1
    		Inhibitor
    eIF3e-IN-1 (Compound 209) is an elF3e inhibitor with an EC50 of 18.3 μM. eIF3e-IN-1 significantly reduces the accumulation of HIF1α protein induced by hypoxia and inhibits the acute translation hypoxia response. eIF3e-IN-1 significantly inhibits the expression of ATF4 protein. eIF3e-IN-1 can be used in cancer research, such as in breast cancer studies.
    eIF3e-IN-1
  • HY-121511
    EML631
    		Inhibitor
    EML631 is a SPIN1 inhibitor with a Kd of 3-7 μM. EML631 interacts with the second Tudor domain of SPIN1 and blocks its ability to read the H3K4me3 histone mark. EML631 inhibits the coactivator activity of SPIN1 in the Wnt signaling pathway and reduces the activity of Wnt response reporter genes. EML631 can be used in cancer-related research.
    EML631
Cat. No. Product Name / Synonyms Application Reactivity