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-103036
    BET bromodomain-IN-5
    		Inhibitor 99.49%
    BET bromodomain-IN-5 is an orally active BET inhibitor with an IC50 of 14 nM against BRD4 (1). BET bromodomain-IN-5 can inhibit the proliferation of tumor cells and induce cell cycle arrest and apoptosis. BET bromodomain-IN-5 can be used in the research of tumors.
    BET bromodomain-IN-5
  • 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-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-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-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-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-103297
    OXFBD02
    		Inhibitor 98.04%
    OXF BD 02 is a selective inhibitor of BRD4(1) (the first bromodomain of BRD4) with IC50 value of 382 nM.
    OXFBD02
  • HY-12421
    BET-BAY 002
    		Inhibitor 99.80%
    BET-BAY 002 is a potent BET inhibitor; shows efficacy in a multiple myeloma model.
    BET-BAY 002
  • HY-160499
    BRD4 Inhibitor-30
    		Inhibitor 99.89%
    BRD4 inhibitor-30 (Compound 1) is a BRD4 inhibitor with a IC50 value of 415 nM.
    BRD4 Inhibitor-30
  • HY-112504A
    INCB054329 Racemate
    		Inhibitor
    INCB054329 Racemate is a BET protein inhibitor.
    INCB054329 Racemate
  • HY-101125A
    L-Moses dihydrochloride
    		Inhibitor 99.38%
    L-Moses (L-45) dihydrochloride is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126 nM.
    L-Moses dihydrochloride
  • HY-102000
    IACS-9571
    		Inhibitor
    IACS-9571 is a potent and selective inhibitor of TRIM24 and BRPF1, with IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively.
    IACS-9571
Cat. No. Product Name / Synonyms Application Reactivity