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-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-123626
    BiBET
    BiBET is a chemical probe of BET/BRD4 and is able to bind to two bromodomains simultaneously in a bivalent and cis-binding mode.
    BiBET
  • HY-16652R
    Apabetalone (Standard)
    		Inhibitor
    Apabetalone (Standard) is the analytical standard of Apabetalone. This product is intended for research and analytical applications. Apabetalone (RVX-208) is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. The IC50s are 87 μM and 0.51 μM for BD1 and BD2, respectively.
    Apabetalone (Standard)
  • HY-176070
    HRG038
    		Inhibitor
    HRG038 is a selective covalent BRD4 degrader. HRG038 binds covalently to the E3 ubiquitin ligase CUL4 DCAF16, recruiting it to BRD4, leading to the ubiquitination and subsequent proteasomal degradation of BRD4. HRG038 is promising for research of cancers.
    HRG038
  • HY-139804
    CTK7A
    CTK7A is a curcumin derivative with anticancer activity by inhibiting the HAT activity of p300 and reducing the autoacetylation of p300, thereby affecting its interaction with HIF-1α. The inhibition of CTK7A leads to decreased HIF-1α accumulation and activity, which can be used for cancer treatment research.
    CTK7A
  • HY-15743R
    Birabresib (Standard)
    		Inhibitor
    Birabresib (Standard) is the analytical standard of Birabresib. This product is intended for research and analytical applications. Birabresib (OTX-015) is a potent bromodomain (BRD2/3/4) inhibitor with IC50s ranging from 92 to 112 nM.
    Birabresib (Standard)
  • HY-122703
    BETi-211
    		Inhibitor
    BETi-211 is an orally active BET inhibitor (Ki: <1 nM). BETi-211 inhibits growth of triple-negative breast cancers (TNBC) cell lines with IC50 < 1 μM. BETi-211 degrades BET proteins and suppress tumor growth in xenograft breast tumors.
    BETi-211
  • HY-137075
    (±)-JQ1
    		Inhibitor
    (±)-JQ1 is the racemate of (+)-JQ-1 (HY-13030).
    (±)-JQ1
  • HY-160660
    BRD4 Inhibitor-33
    		Inhibitor
    BRD4 Inhibitor-33 (example 13) is a BRD4 inhibitor that can be used in acute kidney disease and chronic kidney disease research.
    BRD4 Inhibitor-33
  • HY-W539427
    BRM/BRG1 ligand 1
    		Inhibitor
    BRM/BRG1 ligand 1 is a BRM/BRG1 ligand, and can be used for synthesis of PROTAC BRM/BRG1 degrader-1 (HY-168242).
    BRM/BRG1 ligand 1
  • 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-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-132130
    BRD4 Inhibitor-13
    		Inhibitor
    BRD4 Inhibitor-13 (Compound 2) is a BRD4 ligand, and can be used for research of cancer, inflammation.
    BRD4 Inhibitor-13
  • 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-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-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-116588
    FT001
    		Inhibitor
    FT001 is an orally active and selective BET inhibitor. FT001 has potent anti-proliferative effects against MV-4-11. FT001 can be used for research of cancer.
    FT001
  • HY-172446
    SMARCA2/4-ligand-5
    SMARCA2/4-ligand-5 is a SMARCA2/4 ligand for PROTAC SMARCA2/4 degrader-37 (Example 4). PROTAC SMARCA2/4 degrader-37 (Example 4) is a PROTAC-based SMARCA2/4 degrader, with an IC50 of ≤0.1 μM.
    SMARCA2/4-ligand-5
Cat. No. Product Name / Synonyms Application Reactivity