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-P10445
    TAT-PiET
    		Inhibitor
    TAT-PiET is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4. TAT-PiET can reduce BRD4 and JMJD6 levels and inhibit cell proliferation. TAT-PiET also resists the endocrine resistance of ERα-positive breast cancer cells. TAT-PiET can be used for the research of cancer, such as breast cancer.
    TAT-PiET
  • HY-143235
    BRD4 Inhibitor-15
    		Inhibitor
    BRD4 Inhibitor-15 (compound 13) is a potent BRD4 inhibitor, with an IC50 of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research.
    BRD4 Inhibitor-15
  • HY-149863
    DDO-8926
    		Inhibitor
    DDO-8926 is a potent and selective BET inhibitor that can significantly reduce mechanical hypersensitivity by inhibiting the expression of pro-inflammatory cytokines and reducing excitability for neuropathic pain research.
    DDO-8926
  • HY-163019
    EN884
    		Degrader
    EN884 is a BRD4 degrader via a SKP1- and proteasome-dependent manner. EN884 can be used in synthetic proteolysis targeting chimeras (PROTACs).
    EN884
  • HY-162743
    PROTAC SMARCA2/4-degrader-29
    		Degrader
    PROTAC SMARCA2/4-degrader-29 (Compound I-279) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-29 degrades SMARCA2 in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: ligand for target protein (HY-163926); Black: linker (HY-159682); Blue: ligand for E3 ligase (HY-W382038)).
    PROTAC SMARCA2/4-degrader-29
  • HY-117365
    MI-1481
    		Inhibitor
    MI-1481 is a highly potent inhibitor of the Menin-MLL1 interaction with IC50 of 3.6 nM. MI-1481 markedly reduces cell growth of murine bone marrow cells transformed and inhibits leukemia progression.
    MI-1481
  • HY-175354
    PROTAC BET Degrader-13
    		Degrader
    PROTAC BET Degrader-13 (Compound 34) is a TRIM21-based PROTAC (TRIMTAC) degrader targeting BET. PROTAC BET Degrader-13 significantly degrades PML-eGFP-BRD4 fusion protein with a near-complete loss of EGFP+ nuclear puncta with an EC50 of 1.4 μM. Pink: BET ligand (HY-13030); Blue: E3 ligase ligand (HY-W1125585); Black: linker
    PROTAC BET Degrader-13
  • HY-149421
    BRD7-IN-3
    		Inhibitor
    BRD7-IN-3 (compound 1-78) is a dual inhibitor of bromodomain-containing proteins BRD7/BRD9 with IC50s of 1.6 μM and 2.7 μM respectively.
    BRD7-IN-3
  • HY-175242
    PROTAC BRD4 ligand-4
    		Ligand
    PROTAC BRD4 ligand-4 is a BRD4 ligand, which can be used to synthesize PROTAC BRD4 Degrader-37 (HY-175225).
    PROTAC BRD4 ligand-4
  • HY-151533
    PBRM1-BD2-IN-6
    		Inhibitor
    PBRM1-BD2-IN-6 is a potent PBRM1 bromodomain inhibitor with an IC50 value of 0.22 μM. PBRM1-BD2-IN-6 shows antiproliferation activity. PBRM1-BD2-IN-6 has the potential for the research of PBRM1-dependent cancer.
    PBRM1-BD2-IN-6
  • HY-151528
    PBRM1-BD2-IN-1
    		Inhibitor
    PBRM1-BD2-IN-1 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-1 has binding affinity and inhibitory activity for PBRM1-BD2 with Kd and IC50 values of 0.7 μM and 0.2 μM, respectively. PBRM1-BD2-IN-1 can be used for the research of cancer.
    PBRM1-BD2-IN-1
  • HY-163809
    BRD9 Degrader-2
    		Degrader
    BRD9 Degrader-2 (Compound B11) is a BRD9 degrader (DC50 ≤1.25 nM; Dmax≥75%). BRD9 Degrader-2 can be used for research of cancers.
    BRD9 Degrader-2
  • HY-178481
    BRM/BRG1 ATP-IN-5
    		Inhibitor
    BRM/BRG1 ATP-IN-5 (Compound 6) is a BRG1/BRM inhibitor. BRM/BRG1 ATP-IN-5 acts on the BAF complex, which is involved in chromatin regulation and gene expression via ATP-dependent chromatin remodeling. BRM/BRG1 ATP-IN-5 demonstrates anti-tumor potential, particularly in cancers associated with BAF complex disorders.
    BRM/BRG1 ATP-IN-5
  • HY-44824
    SMARCA2 ligand-13
    		Inhibitor
    SMARCA2 ligand-13 is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). SMARCA2 ligand-13 can be used for synthesis PROTACs.
    SMARCA2 ligand-13
  • HY-168236
    PROTAC SMARCA2 degrader-28
    		Degrader
    PROTAC SMARCA2 degrader-28 (Compound 158) is a PROTAC degrader for SMARCA2, that degrades SMARCA2 with a DC50 of 3 nM in HiBiT A549 cells. (Pink: Ligand for target protein (HY-168237); Black: Linker (HY-168238); Blue: Ligand for E3 ligase (HY-W087383))
    PROTAC SMARCA2 degrader-28
  • HY-170841
    HDAC3/BRD4-IN-1
    		Inhibitor
    HDAC3/BRD4-IN-1 (compound 26n) is an inhibitor of HDAC3/BRD4 with an IC50 of 8 nM for HDAC3 (IC50s are 220 nM and 120 nM for HDAC1 and HDAC2, respectively). HDAC3/BRD4-IN-1 has anti-tumor and anti-proliferative effects by upregulating Ac-H3 and downregulating c-Myc. The half-life of HDAC3/BRD4-IN-1 in human liver microsomes is 29.36 min.
    HDAC3/BRD4-IN-1
  • HY-156130
    Menin-MLL inhibitor 29
    		Inhibitor
    Menin-MLL inhibitor 29 (Compound C1) is a Menin-MLL PPI inhibitor. Menin-MLL inhibitor 29 binds to Menin with a KD value of 138 nM, and inhibits the binding of Menin to MBM1 (Menin-binding motif 1) with an IC50 value of 46 nM. Menin-MLL inhibitor 29 inhibits HepG2 and Hep3B hepatoma cell proliferation (IC50s: 0.31 μM and 0.71 μM). Menin-MLL inhibitor 29 inhibits tumor growth.
    Menin-MLL inhibitor 29
  • HY-161888
    DCSM06
    		Inhibitor
    DCSM06 is an inhibitor for the bromodomain of SWI/SNF chromatin remodeling complexe SMARCA2 with an IC50 of 9.7 μM
    DCSM06
  • HY-177139
    CDD-1349
    		Inhibitor
    CDD-1349 (Compound 15) is a BRDT-BD2/BRD4-BD2 selective inhibitor. CDD-1349is an analog with sixfold selectivity for BRDT-BD2 versus BRD4-BD2. CDD-1349 has an IC50 of 22 nM against BRDT. CDD-1349 can be studied in research on nonhormonal contraceptive agent.
    CDD-1349
  • HY-176732
    MJ-26
    		Inhibitor
    MJ-26 is an inhibitor targeting Menin. MJ-26 has high binding affinity (Ki: 0.56 μM) and significant antiproliferative activity. MJ-26 works by inhibiting Menin-MLL interaction and inducing Menin protein degradation. MJ-26 has significant antitumor effects on acute myeloid leukemia (AML). MJ-26 can be used in AML research.
    MJ-26
Cat. No. Product Name / Synonyms Application Reactivity