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-124596
    CD161
    		99.90%
    CD161 is a potent, selective and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50s of 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 has good anticancer activity.
    CD161
  • HY-162088
    DW71177
    		Inhibitor
    DW71177 is a novel [1,2,4]triazolo[4,3-a] quinoxaline-based potent and BD1-Selective BET inhibitor, and can be used for study of acute myeloid leukemia.
    DW71177
  • HY-142520
    I-BET567
    		Inhibitor 99.49%
    I-BET567 is a potent and orally active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation.
    I-BET567
  • HY-101121
    NI-42
    		Inhibitor 99.53%
    NI-42 (compound 13-d), a structurally orthogonal chemical probe for the BRPFs, is a biased, potent inhibitor of the BRD of the BRPFs (IC50s of BRPF1/2/3=7.9/48/260 nM; Kds of BRPF1/2/3=40/210/940 nM) with excellent selectivity over nonclass IV BRD proteins.
    NI-42
  • HY-139707
    PROTAC CBP/P300 Degrader-3
    		Degrader 98.55%
    PROTAC CBP/P300 Degrader-3 (P-007) is a PROTAC-based CBP and p300 degrader (extracted from patent WO2020173440).
    PROTAC CBP/P300 Degrader-3
  • HY-110263
    EML 425
    		Inhibitor 98.04%
    EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor with IC50s of 2.9 and 1.1 μM, respectively.
    EML 425
  • HY-151529
    PBRM1-BD2-IN-2
    		Inhibitor ≥99.0%
    PBRM1-BD2-IN-2 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-2 has binding affinity and inhibitory activity for PBRM1-BD2 with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. PBRM1-BD2-IN-2 can be used for the research of cancer.
    PBRM1-BD2-IN-2
  • HY-13032A
    GSK 525768A
    		Control 99.68%
    GSK 525768A is the inactive enantiomer of GSK525762A. GSK 525768A has no activity towards BET.
    GSK 525768A
  • HY-149100
    PLK1-IN-6
    		Inhibitor
    PLK1-IN-6 is a potent and selective PLK1 inhibitor, with an IC50 of 0.45 nM. PLK1-IN-6 shows significant anti-proliferative activities against cancer cells.
    PLK1-IN-6
  • HY-N3213
    Naringenin triacetate
    		99.65%
    Naringenin triacetate is a flavonoid isolated from plant, exhibits a good binding affinity with multiple crystal structures of first bromodomain BRD4 (BRD4 BD1).
    Naringenin triacetate
  • 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-174866
    BT-O2C
    		Inhibitor
    BT-O2C is a highly selective p300 PROTAC degrader. BT-O2C can significantly degrade the level of p300 in HAP1 cells. BT-O2C has significant cytotoxicity in CIC:DUX4 sarcoma (CDS) cell lines (IC50 ranges from 152 to 221 nM) and significantly reduces the expression of CDS target genes (ETV1, ETV4, ETV5). BT-O2C can be used for research on cancer. (Pink: p300 Ligand (HY-174868); Blue: CRBN Ligand (HY-W023573); Black: Linker; CRBN Ligand+Linker (HY-174869)).
    BT-O2C
  • 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-107425A
    cis-MZ 1
    		Control 99.8%
    cis-MZ 1 is a cis isomer of meso-zeaxanthin, a xanthophyll carotenoid component of total zeaxanthin measured in serum and egg yolks.cis-MZ 1 is a triphenyltin benzoate that adopts either a tetrahedral monomeric structure (I) or a trans-SnR3O2 polymeric structure (III), with structure determined by a balance of steric and electronic factors.
    cis-MZ 1
  • HY-156273
    HDAC/JAK/BRD4-IN-1
    		Inhibitor
    HDAC/JAK/BRD4-IN-1(compound 25ap) is a potent HDAC/JAK/BRD4 triple inhibitor. HDAC/JAK/BRD4-IN-1 inhibit cell growth and induces apoptosis in MDA-MB-231 cells, and shows anticancer activity in vivo.
    HDAC/JAK/BRD4-IN-1
  • HY-100696
    PNZ5
    		Inhibitor 99.61%
    PNZ5 is a potent and isoxazole-based pan-BET inhibitor with high selectivity and potency similar to the well-established (+)-JQ1, with a KD of 5.43 nM for BRD4(1).
    PNZ5
  • HY-P10446
    TAT-PiET-PROTAC
    		Inhibitor 98.04%
    TAT-PiET-PROTAC is a proteolysis-targeting chimera (PROTAC)-modified TAT-PiET (HY-P10445), which is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4. TAT-PiET-PROTAC can reduce BRD4 and JMJD6 levels and inhibit cell proliferation. TAT-PiET-PROTAC also resists the endocrine resistance of ERα-positive breast cancer cells. TAT-PiET-PROTAC can be used for the research of cancer, such as breast cancer.
    TAT-PiET-PROTAC
  • HY-147174
    PROTAC_ERRα
    		Inhibitor 99.71%
    PROTAC_ERRα is a potent and selective ERRα PROTAC degrader (DC50: 100 nM in MCF-7 cells). PROTAC_ERRα induces proteasomal degradation and has capable of specifically degrading ERRα protein by >80%. Blue: VHL ligand (HY-125845), Pink: ERRα ligand (HY-U00425), black: linker.
    PROTAC_ERRα
  • HY-150211
    DC-BPi-03
    		Inhibitor 99.77%
    DC-BPi-03 is a potent BPTF-BRD inhibitor with an IC50 of 698.3 nM and a Kd of 2.81 μM.
    DC-BPi-03
  • HY-114164G
    Murine Thrombin
    		Activator
    Murine Thrombin is a murine serine protease that plays a central role in blood coagulation. Murine Thrombin stimulates macrophages to polarize into a unique phenotype characterized by anti-inflammatory and pro-repair properties. Murine Thrombin activates PAR1, induces the production of MCP-1, MMP3 and VEGF in mouse intervertebral discs, and causes degradation of the cartilage matrix and destruction of intervertebral disc structure. Murine Thrombin activity increases significantly in paraoxon-induced status epilepticus.
    Murine Thrombin
Cat. No. Product Name / Synonyms Application Reactivity