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-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
  • HY-111502
    Y06036
    		Inhibitor 98.57%
    Y06036 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with Kd value of 82 nM. Antitumor activity.
    Y06036
  • HY-111916
    ODM-207
    		Inhibitor 99.58%
    ODM-207 (BET-IN-4) is a potent BET bromodomain protein (BRD4) inhibitor, with an IC50 of ≤ 1 μM.
    ODM-207
  • HY-114205A
    TP-238 hydrochloride
    		Inhibitor ≥99.0%
    TP-238 hydrochloride is a potent and selective dual CECR2/BPTF probe with IC50 values of 30 nM and 350 nM, respectively. TP-238 hydrochloride also inhibits BRD9 with a pIC50 of 5.9 and is less active against other 338 kinases.
    TP-238 hydrochloride
  • HY-150268
    Zavabresib
    		Inhibitor 99.60%
    Zavabresib (BET-IN-16) (Compound I) is a BET inhibitor. BET-IN-16 shows anticancer activity. Zavabresib inhibits prostate cancer cell growth, with IC50 values of 0.043 and 0.034 μM against LNCaP and 22Rv1 cells, respectively.
    Zavabresib
  • HY-134598A
    653-47 hydrochloride
    		Inhibitor 99.42%
    653-47 hydrochloride, a potentiator, significantly potentiates the cAMP-response element binding protein (CREB) inhibitory activity of 666-15. 653-47 hydrochloride is also a very weak CREB inhibitor with IC50 of 26.3 μM.
    653-47 hydrochloride
  • HY-110215
    XD14
    		Inhibitor
    XD14 is a potent BET inhibitor with antitumor effect. It binds to BRD2, BRD3, and BRD4 with Kds of 170, 380, and 160 nM, respectively.
    XD14
  • HY-146999
    YM458
    		Inhibitor 99.16%
    YM458 is a potent EZH2 and BRD4 dual inhibitor with IC50s of 490 nM and 34 nM, respectively. YM458 inhibits cell proliferation and colony formation and induces cell cycle arrest and apoptosis in solid cancer cells. YM458 can be used for researching anticancer.
    YM458
  • HY-160287
    NVS MLLT-1
    		Inhibitor 99.79%
    NVS MLLT-1 (compound 3), a chemical probe, is a potent and selective MLLT1 inhibitor with Kd values of 0.18 μM, 0.24 μM, and 0.22 μM for wild-type, T1 mutants, and T3 mutants, respectively.
    NVS MLLT-1
  • HY-19760
    I-BET282
    		Inhibitor 98.90%
    I-BET282 is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282 shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD).
    I-BET282
  • HY-117865
    GNE-886
    		Inhibitor 99.81%
    GNE-886 (Compound 21) is a potent and selective inhibitor of Cat eye syndrome chromosome region candidate 2 bromodomain (CECR2) (BRD) with an IC50 value of 0.016 µM and an EC50 value of 370 nM. GNE-886 also inhibits BRD9 with an IC50 value of 1.6 µM.
    GNE-886
  • HY-163729
    I-BET787
    		Inhibitor 99.88%
    I-BET787 is a orally active BET bromine domain inhibitor with pIC50s of 7.1 and 5.9 for BRD4 BD1 and BRD4 BD2, respectively. I-BET787 has anti-inflammatory activity in mice.
    I-BET787
  • HY-W010649
    Isoxazole
    		Inhibitor 99.98%
    Isoxazole is a member of the five-membered heterocycle drug scaffold. Isoxazole has been used as a BET bromodomain inhibitor and can improve β-cell function in a diabetic mouse model. Isoxazole and its derivatives exhibit broad biological activities (such as antimicrobial, antibacterial, antifungal, antiviral, anticancer, anti-inflammatory, immunomodulatory, analgesic, anti-tuberculosis, and anti-diabetic effects). For example, the bicyclic Isoxazole can act as an HSP90 inhibitor, and the tricyclic Isoxazole is promising as a selective multidrug resistance protein (MRP1) inhibitor​.
    Isoxazole
  • HY-110315
    Ischemin sodium
    		Inhibitor 99.32%
    Ischemin sodium is a CBP bromodomain inhibitor that inhibits p53 interaction with CBP and transcriptional activity in cells. Ischemin sodium salt inhibits p53-induced p21 activation with an IC50 value of 5 µM. Ischemin sodium salt also prevents apoptosis in ischemic cardiomyocytes. Ischemin sodium salt can be used in the study of cardiovascular diseases (such as myocardial ischemia).
    Ischemin sodium
  • HY-160558
    PLK1/BRD4-IN-3
    		Inhibitor 98.55%
    PLK1/BRD4-IN-3 (Compound 21) is a selective dual inhibitor for bromodomain 4 (BRD4) and polo-like kinase 1 (PLK1). PLK1/BRD4-IN-3 inhibits BRD4-BD1, PLK1 and BRDT-BD1, with IC50s of 0.059, 0.127 and 0.245 μM, respectively.
    PLK1/BRD4-IN-3
  • HY-128347
    M‑89
    		Inhibitor 99.14%
    M-89 is a highly potent and specific menin inhibitor, with a Kd of 1.4 nM for binding to menin. M-89 inhibits the menin-mixed lineage leukemia (Menin-MLL) protein-protein interaction and has potential to study MLL leukemia. M-89 inhibits the cell growth in leukemia cell lines carrying MLL fusion.
    M‑89
  • HY-138634
    GNE-987 GSH linker-2
    		Inhibitor 99.48%
    GNE-987 GSH linker-2 is a drug-linker conjugates for ADC. GNE-987 GSH linker-2 is a conjugation of PROTAC GNE-987 (HY-129937A) and ADC linker GSH linker-2 (HY-182740), and can be used to prepare antibody-drug conjugates (ADC) for BRD4 degradation. GNE-987 GSH linker-2 can be used for the research of cancer.
    GNE-987 GSH linker-2
  • HY-138635
    PROTAC BRD4 Degrader-12
    		Inhibitor 98.54%
    PROTAC BRD4 Degrader-12 (compound 9c) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-12 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.39 nM and 0.24 nM, respectively.
    PROTAC BRD4 Degrader-12
  • HY-151595
    Menin-MLL inhibitor-22
    		Inhibitor 99.85%
    Menin-MLL inhibitor-22 (compound C20) is an orally active inhibitor of the interaction between menin and mixed lineage leukemia (MLL) (IC50=7 nM). Menin-MLL inhibitor-22 binds menin protein and inhibits cancer cell growth (MV4 cells, IC50=0.3 μM). Menin is a putative tumor suppressor associated with multiple endocrine neoplasia type 1 (MEN-1 syndrome).
    Menin-MLL inhibitor-22
  • HY-114229
    PROTAC BET degrader-3
    		Inhibitor 99.11%
    PROTAC BET Degrader-3 is a PROTAC connected by ligands for von Hippel-Lindau and BET.
    PROTAC BET degrader-3
Cat. No. Product Name / Synonyms Application Reactivity