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-153226
    BET-IN-14
    		Inhibitor 99.07%
    BET-IN-14 is an orally active pan BET inhibitor (IC50: 5.35 nM). BET-IN-14 has anti-cancer activity.
    BET-IN-14
  • HY-18372
    UNC1021
    		Inhibitor 99.85%
    UNC1021 is a selective L3MBTL3 inhibitor with an IC50 of 0.048 μM.
    UNC1021
  • HY-170380
    XY221
    		Inhibitor
    XY221 (Compound 16o) selectively inhibits BRD4 BD2, with an IC50 of 5.8 nM. XY221 demonstrates high pan-BD2 selectivity (667-fold over BRD4 BD1) and BRD4 BD2 domain selectivity (9−32-fold over BRD2/3/T BD2). XY221 induce Apoptosis in MV4-11 cells and shows anticancer activity .
    XY221
  • HY-173333
    PROTAC SMARCA2/4 degrader-38
    		Degrader
    PROTAC SMARCA2/4 degrader-38 is a degrader SMARCA2/4 PROTAC (DC50: 3.0 nM and 4.0 nM respectively). PROTAC SMARCA2/4 degrader-38 promotes the ubiquitination and degradation of SMARCA2/4. PROTAC SMARCA2/4 degrader-38 blocks the G0/G1 cell cycle and induces apoptosis. PROTAC SMARCA2/4 degrader-38 can be used in acute myeloid leukemia (AML) research. (Pink: SMARCA2/4 ligand; Blue: VHL ligand (HY-112078); Black: linker; Target Protein Ligand-Linker Conjugates (HY-173343)).
    PROTAC SMARCA2/4 degrader-38
  • HY-126299
    NVS-BPTF-1
    		Inhibitor
    NVS-BPTF-1, a chemical probe, is a selective inhibitor for bromodomain and PHD finger containing transcription factor (BPTF), with KD of 71 nM.
    NVS-BPTF-1
  • HY-147046
    ET-JQ1-OH
    		Inhibitor
    ET-JQ1-OH is an allele-specific BET inhibitor.
    ET-JQ1-OH
  • HY-143332
    TRIM24/BRPF1-IN-2
    		Inhibitor 98.74%
    TRIM24/BRPF1-IN-2 (compound 20l) is a potent TRIM24/BRPF1 dual inhibitor, with IC50 values of 0.98 and 1.16 μM, respectively. TRIM24/BRPF1-IN-2 shows TRIM24/BRPF1 bromodomain binding affinity. TRIM24/BRPF1-IN-2 can be used for prostate cancer research.
    TRIM24/BRPF1-IN-2
  • HY-161346
    EBET-1055
    		Degrader
    EBET-1055 is a bromodomain and extra-terminal (BET) PROTAC degrader. EBET-1055 effectively inhibits the growth of pancreatic ductal adenocarcinoma (PDAC). EBET-1055 also simultaneously modulates cancer-associated fibroblast (CAF) activity, upregulating all reporter gene activities in organoid co-cultures. Pink: BET ligand (HY-161387); Blue: CRBN ligase ligand (HY-14658); Black: linker
    EBET-1055
  • HY-107425B
    cis-MZ 1 hydrate
    		Inhibitor 99.0%
    cis-MZ 1 hydrate is a negative control for BRD4-targeted PROTAC MZ 1 (HY-107425). cis-MZ 1 or MZ 1 is a combination of the von Hippel-Lindau ligand (red part in the structural formula) and the BRD4 ligand (blue part in the structural formula). The Kd of MZ 1 for BRD4 BD1/2 was 382 nM and 120 nM, respectively.
    cis-MZ 1 hydrate
  • HY-107443A
    (R)-I-BET762 carboxylic acid
    		Control 99.50%
    (R)-I-BET762 carboxylic acid, the R-enantiomer of I-BET762 carboxylic acid (HY-107443). I-BET762 carboxylic acid is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid is a BRD4 inhibitor with a pIC50 value of 5.1.
    (R)-I-BET762 carboxylic acid
  • HY-161651
    BRD4 ligand 6
    BRD4 ligand 6 is a BRD4 ligand and can be used for synthesis of BRD4 PROTACs, such as PROTAC BRD4 Degrader-26 (HY-161650).
    BRD4 ligand 6
  • HY-107425A
    cis-MZ 1
    		Degrader 99.8%
    cis-MZ 1 is a negative control of MZ 1 (HY-107425). cis-MZ 1 is a PROTAC targeting to BRD4.
    cis-MZ 1
  • HY-147868
    DC-CPin711
    		Inhibitor 99.09%
    DC-CPin711 is a potent and selective inhibitor of CREB-binding protein (CBP) bromodomain with an IC50 of 0.0626 μM. DC-CPin711 arrests cell cycle at G1 phase and induces apoptosis.
    DC-CPin711
  • HY-151594A
    iBRD4-BD1 diTFA
    		Inhibitor 99.52%
    iBRD4-BD1 diTFA is selective BRD4 bromodomain inhibitor. iBRD4-BD1 diTFA has inhibition activity for BRD4 bromodomain with an IC50 value of 12 nM. iBRD4-BD1 diTFA can be used for the research of inflammation and oncology.
    iBRD4-BD1 diTFA
  • HY-111977
    ZEN-3219
    		Inhibitor 99.75%
    ZEN-3219 is a BET inhibitor with IC50s of 0.48, 0.16 and 0.47 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3219 can be used to form PROTACs to induce degradation of BRD4.
    ZEN-3219
  • HY-116227
    (2S,3R)-LP99
    		Inhibitor 99.4%
    (2S,3R)-LP99 is a potent and selective BRD7 and BRD9 inhibitor with an KD of 99 nM for BRD9. (2S,3R)-LP99 inhibits the association of BRD7 and BRD9 to acetylated histones in vitro and in cells. (2S,3R)-LP99 demonstrates that BRD7/9 plays a role in regulating pro-inflammatory cytokine secretion.
    (2S,3R)-LP99
  • HY-114162R
    VTP50469 (Standard)
    		Inhibitor
    VTP50469 (Standard) is the analytical standard of VTP50469. This product is intended for research and analytical applications. VTP50469 is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 has potently anti-leukemia activity.
    VTP50469 (Standard)
  • HY-131633A
    (+)-JQ-1-aldehyde
    		Inhibitor 98.07%
    (+)-JQ-1-aldehyde is the aldehyde form of (+)-JQ1. (+)-JQ-1-aldehyde can be uesd as a precursor to synthesize PROTACs, which targets BET bromodomains.
    (+)-JQ-1-aldehyde
  • HY-128703
    Bromodomain inhibitor-8
    		Inhibitor 98.02%
    Bromodomain inhibitor-8 (Intermediate 21) is a BET bromodomain inhibitor for treating autoimmune and inflammatory diseases.
    Bromodomain inhibitor-8
  • HY-135236
    OXFBD04
    		Inhibitor 98.99%
    OXFBD04 is a potent and selective BRD4 inhibitor with an IC50 of 166 nM. OXFBD04 is a potent BET bromodomain ligand with additional modest affinity for the CREBBP bromodomain. OXFBD04 has anti-cancer activity.
    OXFBD04
Cat. No. Product Name / Synonyms Application Reactivity