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-174397
    EED-IN-3
    		Inhibitor
    EED-IN-3 is an orally active EED inhibitor. EED-IN-3 effectively inhibits PRC2 by binding to EED (IC50 = 0.62 μM for EED) and downregulates H3K27me3. EED-IN-3 can efficiently and selectively inhibit PC3 cells with the IC50 of 3.69 μΜ and could significantly suppress colony formation and migration. EED-IN-3 can be used for research on prostate cancer.
    EED-IN-3
  • HY-173564
    DW34
    		Inhibitor
    DW34 is an orally active pan-BRD4-D1 biased inhibitor with additional BRD4-D2 inhibitive activity. DW34 displays comparable inhibitive efficacy to I-BET151 (HY-13235) (EC50 = 0.16 μM) with low nanomolar EC50 values of 0.14 μM. DW34 significantly reduces liver inflammation induced by LPS (HY-D1056) and APAP (HY-66005) via reducing chemokine expression and cellular necrosis.
    DW34
  • HY-178172
    AF9/ENL-DOT1L PPI-IN-1
    		Inhibitor
    AF9/ENL-DOT1L/AF4 PPI-IN-1 is a potent AF9/ENL and histone methyltransferase DOT1L/AF4 protein-protein interactions (PPI) inhibitor. AF9/ENL-DOT1L/AF4 PPI-IN-1 can inhibit the AF9-DOT1L (IC50 = 1.5 μM), AF9-AF4 (IC50 = 1 μM), ENL-AF4 (IC50 = 1.2 μM) interactions. AF9/ENL-DOT1L/AF4 PPI-IN-1 can suppress the expression of Mixed lineage leukemia (MLL) target genes Myc and Meis1 and selectively block the proliferation of MLL-r and several other leukemia cells. AF9/ENL-DOT1L/AF4 PPI-IN-1 exhibits significant antitumor activities in a mouse model of MLL-r leukemia without overt toxicities. AF9/ENL-DOT1L/AF4 PPI-IN-1 can be used for the study of MLL-r leukemia.
    AF9/ENL-DOT1L PPI-IN-1
  • HY-176467
    TAF1 ligand 1
    		Ligand
    TAF1 ligand 1 is a TAF1 ligand. TAF1 ligand 1 can be used as a Ligands for Target Protein for PROTAC synthesis, such as ZS3-046 (HY-176457).
    TAF1 ligand 1
  • HY-116277
    Z118332870
    		Inhibitor
    Z118332870 is a potent dual inhibitor of EGFR and BRD4, exhibiting significant potential as a therapeutic agent for overcoming resistance in cancer treatment.
    Z118332870
  • HY-174975
    JY-21
    		Degrader
    JY-21 is a BRD4 PROTAC degrader with a DC50 of 3.797 μM. JY-21 has a potent anticancer activity against MDA-MB-231 cells. Pink: BRD4 ligand (HY-78695); Blue: E3 ligase ligand (HY-174994); Black: linker (HY-151862)
    JY-21
  • HY-142675
    BRD4-BD1/2-IN-2
    		Inhibitor
    BRD4-BD1/2-IN-2 is a potent BRD4 BD2 inhibitor with IC50s of <0.5 nM and <300 nM for BRD4 BD2 and BRD4 BD1, respectively (WO2021233371A1, compound 2).
    BRD4-BD1/2-IN-2
  • HY-169937
    (R)-SR-C-107
    (R)-SR-C-107 is an orally available inhibitor of ENL (YEAST domain-containing protein) designed to target acute myeloid leukemia (AML). (R)-SR-C-107 targets ENL with IC50 and KD of 40 nM and 144 nM, respectively. (R)-SR-C-107 demonstrates in vivo efficacy in a xenograft mouse model of AML, with a tumor regression rate of 45% at a dose of 200 mg/kg (PO; QD).
    (R)-SR-C-107
  • HY-119490
    UMB-136
    		Inhibitor
    UMB-136 is a bromodomain inhibitor. UMB-136 is a promising latency-reversing agent (LRA) for HIV-1 eradication. UMB-136 reactivates HIV-1 in multiple cell models. UMB-136 enhances HIV-1 transcription and increases viral production through the release of P-TEFb.
    UMB-136
  • HY-150797
    QA-68
    		Inhibitor
    QA-68 (QA-68-ZU81) is an effective PROTAC-class BRD9 degrader. QA-68 can inhibit cell cycle progression and cell colony formation. QA-68 has antiproliferative activity against acute myeloid leukemia (AML) cell lines. QA-68 can be formed by a target protein ligand (red part) EA-89 (HY-170314), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-I (HY-131318), and a PROTAC linker (black part) Ethyne-C2-Pip-CO-Pip-Boc (HY-170315). E3 ubiquitin ligase and linker can form Lenalidomide-ethyne-C2-Pip-CO-Pip (HY-170319).
    QA-68
  • HY-174451
    KMT9-IN-2
    		Inhibitor
    KMT9-IN-2 (Compound 7b) is an active form of a KMT9 inhibitor (Kd of 10 nM). KMT9-IN-2 can be used in the research of colon cancer.
    KMT9-IN-2
  • HY-147572
    BET-IN-10
    		Inhibitor
    BET-IN-10 is a BET inhibitor with anticancer effects. BET-IN-10 inhibits the cell growth of MV4-11 cells with an IC50 of 26.5 nM (WO2022012456A1; example 6).
    BET-IN-10
  • HY-149519
    BRD4 Inhibitor-28
    		Inhibitor
    BRD4 Inhibitor-28 (Compound 18) is an orally active BRD4 Inhibitor. BRD4 Inhibitor-28 inhibits BRD40-BD1, BRD40-BD2 with IC50s of 15, 55 nM. BRD4 Inhibitor-28 also inhibits BRD2-BD1, BRD3-BD1, BRDT-BD1 with IC50s of 19, 25, 68 nM. BRD4 Inhibitor-28 has anti-melanoma activity.
    BRD4 Inhibitor-28
  • HY-169094
    PFI-6-COOH
    PFI-6-COOH (Compound 18) is an eleven-nineteen leukemia (ENL) ligand, and can be used for synthesis of MS41 (HY-169093), an ENL PROTAC degrader.
    PFI-6-COOH
  • HY-163282
    NB512
    		Inhibitor
    NB512 (compound 39a) is a dual inhibitor for BET and HDAC, which exhibits a efficient binding affinity with BRD4 bromodomains and HDAC1/2, with EC50s of 100-400 nM. NB512 exhibits an anti-proliferative activity towards cancer cells PaTu8988T and NMC.
    NB512
  • HY-162245
    PROTAC SMARCA2 degrader-3
    		Inhibitor
    PROTAC SMARCA2 degrader-3 is a PROTAC degrader of the SWI/SNF ATPase subunits, SMARCA2. PROTAC SMARCA2 degrader-3 has anticancer effects (WO2023244764A1; Compound 153).
    PROTAC SMARCA2 degrader-3
  • HY-149098
    SJ1461
    		Inhibitor
    SJ1461 is a potent and orally active BET inhibitor. SJ1461 inhibits BRD2 (BD1), and BRD2 (BD2), BRD4 (BD1), and BRD4 (BD2) with IC50 values of 1.6 nM, 0.1 nM, 6.5 nM, and 0.2 nM, respectively.
    SJ1461
  • HY-163810
    BRD9 Degrader-3
    		Degrader
    BRD9 Degrader-3 (compound B20) is a BRD9 molecular glue, with a DC50 of <1.25 nM.
    BRD9 Degrader-3
  • HY-134598
    653-47
    		Inhibitor
    653-47, a potentiator, significantly potentiates the cAMP-response element binding protein (CREB) inhibitory activity of 666-15. 653-47 is also a very weak CREB inhibitor with IC50 of 26.3 μM.
    653-47
  • HY-114902
    Y02224
    		Inhibitor
    Y02224 is a potent BRD4 inhibitor and exhibits reasonable antiproliferative effect on leukemia cells.Y02224 has the potential for? CRPC research.
    Y02224
Cat. No. Product Name / Synonyms Application Reactivity