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.

Epigenetic Reader Domain Isoform Specific Products:

Epigenetic Reader Domain Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-100015R
    Mivebresib (Standard)
    		Inhibitor
    Mivebresib (Standard) is the analytical standard of Mivebresib. This product is intended for research and analytical applications. Mivebresib (ABBV-075) is a potent and orally active bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a Ki of 1.5 nM.
    Mivebresib (Standard)
  • HY-100482R
    CPI-637 (Standard)
    		Inhibitor
    CPI-637 (Standard) is the analytical standard of CPI-637 (HY-100482). This product is intended for research and analytical applications. CPI-637 is a selective and potent CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM, 0.051 μM and 11.0 μM for CBP, EP300 and BRD4 BD-1, respectively, and an EC50 of 0.3 μM for CBP.
    CPI-637 (Standard)
  • HY-102000BR
    IACS-9571 hydrochloride (Standard)
    		Inhibitor
    IACS-9571 hydrochloride (Standard) is the analytical standard of IACS-9571 hydrochloride (HY-102000B). This product is intended for research and analytical applications. IACS-9571 (ASIS-P040) hydrochloride is a potent and selective inhibitor of TRIM24 and BRPF1, with an IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively.
    IACS-9571 hydrochloride (Standard)
  • HY-186043
    Menin-MLL-IN-35
    		Inhibitor
    Menin-MLL-IN-35 (compound 286) is an inhibitor of menin/MLL protein/protein interaction with an IC50 value of 0.096 μM in MEIS1 mRNA expression. Menin-MLL-IN-35 can be used in the research of cancer, myelodysplastic syndrome (MDS), myeloproliferative neoplasms (MPN), and diabetes.
    Menin-MLL-IN-35
  • HY-136570A
    GSK778 hydrochloride
    		Inhibitor
    GSK778 (iBET-BD1) hydrochloride is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively.
    GSK778 hydrochloride
  • HY-19541A
    I-CBP112 hydrochloride
    		Inhibitor
    I-CBP112 hydrochloride is a selective inhibitor of CBP/P300 that directly binds their bromodomains (Kds = 142 and 625 nM, respectively). I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. I-CBP112 increases the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin.
    I-CBP112 hydrochloride
  • HY-160636
    BRD4 Inhibitor-32
    		Inhibitor
    BRD4 Inhibitor-32 (example 15) is a BRD4 inhibitor that can be used in acute kidney disease and chronic kidney disease research.
    BRD4 Inhibitor-32
  • HY-104068R
    Naphthol AS-E (Standard)
    		Inhibitor
    Naphthol AS-E (Standard) is the analytical standard of Naphthol AS-E (HY-104068). This product is intended for research and analytical applications. 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 (Standard)
  • HY-107425R
    MZ 1 (Standard)
    		Inhibitor
    MZ 1 (Standard) is the analytical standard of MZ 1 (HY-107425). This product is intended for research and analytical applications. MZ 1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. MZ 1 potently and rapidly induces reversible, long-lasting, and selective removal of BRD4 over BRD2 and BRD3. Kds of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively.
    MZ 1 (Standard)
  • HY-101120R
    666-15 (Standard)
    		Inhibitor
    666-15 (Standard) is the analytical standard of 666-15 (HY-101120). This product is intended for research and analytical applications. 666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM. 666-15 suppresses tumor growth in a breast cancer xenograft model.
    666-15 (Standard)
  • HY-186044
    Menin-MLL-IN-36
    		Inhibitor
    Menin-MLL-IN-36 (compound 398) is an inhibitor of menin/MLL protein/protein interaction with an IC50 value of 0.043 μM in MEIS1 mRNA expression. Menin-MLL-IN-36 can be used in the research of cancer, myelodysplastic syndrome (MDS), myeloproliferative neoplasms (MPN), and diabetes.
    Menin-MLL-IN-36
  • HY-160446
    BET-IN-24
    		Inhibitor
    Bet-in-24 (example 2) is a bromodomain and extra-terminal (BET) inhibitor. BET-IN-24 can be used in the study of virology, heart failure, inflammation, central nervous system (CNS) diseases and many cancers
    BET-IN-24
  • HY-100351R
    BI-7273 (Standard)
    		Inhibitor
    BI-7273 (Standard) is the analytical standard of BI-7273 (HY-100351). This product is intended for research and analytical applications. BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM.
    BI-7273 (Standard)
  • HY-100729R
    GSK9311 (Standard)
    		Inhibitor
    GSK9311 (Standard) is the analytical standard of GSK9311 (HY-100729). This product is intended for research and analytical applications. GSK9311, a less active analogue of GSK6853, can be used as a negative control. GSK9311 inhibits BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively.
    GSK9311 (Standard)
  • HY-108696R
    GNE-781 (Standard)
    		Inhibitor
    GNE-781 (Standard) is the analytical standard of GNE-781 (HY-108696). This product is intended for research and analytical applications. GNE-781 is an orally active, highly potent and selective CBP inhibitor with an IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50s of 6.2 nM and 5100 nM, respectively. GNE-781 displays antitumor activity in an MOLM-16 AML xenograft model.
    GNE-781 (Standard)
  • HY-N0005S1
    Curcumin-d3
    		Inhibitor
    Curcumin-d3 (Diferuloylmethane-d3 ) is deuterium labeled Curcumin (HY-N0005). Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
    Curcumin-d<sub>3</sub>
  • HY-108435R
    GNE-049 (Standard)
    		Inhibitor
    GNE-049 (Standard) is the analytical standard of GNE-049 (HY-108435). This product is intended for research and analytical applications. GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively.
    GNE-049 (Standard)
  • HY-123758
    XDM-CBP
    		Inhibitor
    XDM-CBP is a CBP/p300 inhibitor. XDM-CBP can be used in the study of malignant melanoma, breast cancer and leukemia.
    XDM-CBP
  • HY-101838R
    dBET1 (Standard)
    		Inhibitor
    dBET1 (Standard) is the analytical standard of dBET1 (HY-101838). This product is intended for research and analytical applications. dBET1 is a PROTAC connected by ligands for Cereblon and BRD4 with an EC50 of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to NSC 527179 (HY-14658) with a linker.
    dBET1 (Standard)
  • HY-103633R
    PROTAC BET Degrader-1 (Standard)
    		Inhibitor
    PROTAC BET Degrader-1 (Standard) is the analytical standard of PROTAC BET Degrader-1 (HY-103633). This product is intended for research and analytical applications. PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
    PROTAC BET Degrader-1 (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Epigenetic Reader Domain Isoform Comparison

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