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-138563A
    (2R,3R)-GSK973
    		Control
    (2R,3R)-GSK973 is an isomer of GSK973. GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family.
    (2R,3R)-GSK973
  • HY-160557
    PLK1/BRD4-IN-2
    		Inhibitor
    PLK1/BRD4-IN-2 (compound 15) is a BI-2536 (HY-50698) analog and dual inhibitor that targets both Polo-like kinase 1 (PLK1) and BRD4bromodomain (BRD4-BD1 IC50=28 nM, PLK1 IC50=40 nM).
    PLK1/BRD4-IN-2
  • HY-157591
    MMH1-NR
    		Control 99.36%
    MMH1-NR, containing a non-reactive (ethyl) group is a negative control of MMH1. MMH1 is a CUL4-associated factor (DCAF16)-based bromodomain protein 4 (BRD4) degrader.
    MMH1-NR
  • HY-112316A
    (R)-BAY1238097
    		99.07%
    (R)-BAY1238097 is the R-isomer with lower activity of BAY1238097. BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome.
    (R)-BAY1238097
  • HY-112504A
    INCB054329 Racemate
    		Inhibitor
    INCB054329 Racemate is a BET protein inhibitor.
    INCB054329 Racemate
  • 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
  • HY-132991
    ML 2-14
    		Degrader 99.43%
    ML 2-14 is a PROTAC targeting BRD4 with a C4 alkyl linker. ML 2-14 consists of the E3 ligase ligand EN219 (HY-115715) (bule part), the target protein ligand JQ-1 (HY-13030) (red part), and the PROTAC linker (balck part). ML 2-14 can effectively degrade BRD4 in 231MFP breast cancer cells, and this effect can be reversed by the proteasome inhibitor Bortezomib (HY-10227) and the E1 activase inhibitor TAK-243 (HY-100487).
    ML 2-14
  • HY-138634
    GNE-987 GSH linker-2
    		Inhibitor 99.45%
    GNE-987 GSH linker-2 (compound 9a) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GNE-987 GSH linker-2 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.23 nM and 0.38 nM, respectively.
    GNE-987 GSH linker-2
  • HY-145226
    XY-06-007
    		Inhibitor 98.9%
    XY-06-007 is a selective and potent bump-and-hole (B&H)-PROTAC BRD4BD1L94V degrader. XY-06-007 shows a DC50, 6 h of 10 nM against BRD4BD1L94V with no degradation of off-targets. XY-06-007 demonstrates suitable pharmacokinetics for in vivo studies.
    XY-06-007
  • HY-148381
    A947
    A947 is a potent and selective SMARCA2 proteolysis-targeting chimera molecule (PROTAC). A947 also is a potent and moderately selective SMARCA2 degrader. A947 has binding affinity to the SMARCA2 bromodomain with a Kd value of 93 nM. A947 can be used for the research of cancer.
    A947
  • HY-111503
    Y06137
    		Inhibitor 99.90%
    Y06137 is a potent and selective BET inhibitor for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the BRD4(1) bromodomain with a Kd of 81 nM.
    Y06137
  • HY-133738
    M-808
    		Inhibitor
    M-808 is a highly potent and efficacious covalent Menin-MLL interaction inhibitor, with a binding IC50 value of 2.6 nM.
    M-808
  • HY-125837
    MS31
    		Inhibitor
    MS31 is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 potently inhibits binding of trimethyllysine-containing peptides to SPIN1. MS31 is not toxic to nontumorigenic cells.
    MS31
  • 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-138632
    PROTAC BRD4 Degrader-9
    		Inhibitor 98.23%
    PROTAC BRD4 Degrader-9 (compound 8a) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-9 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.86 nM and 7.6 nM, respectively.
    PROTAC BRD4 Degrader-9
  • HY-115867A
    (S)-GSK852
    		99.07%
    (S)-GSK852 is a diastereomer of GSK852 (HY-115867). GSK852 is a BET inhibitor targeting BD2 (pIC50=7.9).
    (S)-GSK852
  • HY-139076
    Menin-MLL inhibitor 19
    		Inhibitor 98.07%
    Menin-MLL inhibitor 19, a potent exo-aza spiro inhibitor of menin-mll interaction, example A17, extracted from patent WO2019120209A1. Menin-MLL inhibitor 19 can be used for the reseaech of various diseases, such as cancer, myelodysplastic syndrome (MDS) and diabetes.
    Menin-MLL inhibitor 19
  • HY-18373
    UNC1079
    		98.0%
    UNC1079 is a piperidine analog of UNC1021, structurally similar but with lower efficacy as an inhibitor.
    UNC1079
  • HY-173351
    G-6599
    		Degrader
    G-6599 is a SMARCA2/A4 target-anchored monovalent degrader with DC50 values of 0.018 nM and 0.056 nM, respectively. G-6599 has degradation activity and anti-proliferative effects in AR-dependent prostate cancer cell lines.
    G-6599
  • HY-168546
    CFT-1297
    		Degrader
    CFT-1297 is a BET PROTAC degrader that can degrade BRD4.
    CFT-1297
Cat. No. Product Name / Synonyms Application Reactivity