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-145946
    BRM/BRG1 ATP Inhibitor-2
    		Inhibitor 99.67%
    BRM/BRG1 ATP Inhibitor-2 is a BRG1/BRM ATPase inhibitor for the research of BAF-related disorders.
    BRM/BRG1 ATP Inhibitor-2
  • HY-130622
    LT052
    		Inhibitor 98.02%
    LT052 is a highly selective BET BD1 inhibitor with an IC50 of 87.7 nM. LT052 exhibits nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2 (IC50=12.130 μM). LT052 has anti-inflammatory?activity and can be used for acute gout arthritis research.
    LT052
  • HY-112150
    ZL0454
    		Inhibitor
    ZL0454 is a potent and selective Bromodomain-containing protein 4 (BRD4) inhibitor with an IC50 of 49 and 32 nM for BD1 and BD2.
    ZL0454
  • HY-156820
    HLDA-221
    		99.24%
    HLDA-221 is a non-covalent regulated induced proximity targeting chimeras (RIPTAC). The binding of HLDA-221 to BRD4-BD1 is significantly increased after pre-incubation with FKBP. HLDA-221 can be used in cancer research.
    HLDA-221
  • HY-148116
    DN02
    		Inhibitor 98.68%
    DN02 is a potent, selective BRD8 bromodomain probe. DN02 has exhibits high affinity for the BRD8 (1) (Ki=32 nM), which is 30-fold more affinity than BRD8 (2) (Ki>1000 nM).
    DN02
  • HY-N0005S
    Curcumin-d6
    		Inhibitor 99.78%
    Curcumin-d6 (Diferuloylmethane-d6 ) 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>6</sub>
  • HY-117286
    (S)-JQ-35
    		Inhibitor 99.46%
    (S)-JQ-35 (TEN-010) is an orally active, blood-brain barrier-permeable bromodomain inhibitor that selectively targets the bromodomain and extra-terminal domain (BET) protein family (BRD4, BRD3, BRD2 and BRDT). (S)-JQ-35 blocks the activation of Myc gene expression by BRD4, thereby inhibiting cancer cell proliferation and promoting cancer cell apoptosis. (S)-JQ-35 can be used in research related to NUT midline carcinoma and neuroblastoma.
    (S)-JQ-35
  • HY-125236
    ZEN-3694
    		Inhibitor 99.74%
    ZEN-3694 (Compound 146) is a BET inhibitor. ZEN-3694 inhibits hlL-6 mRNA transcription (IC50 ≤0.3 uM), and c-myc activity in human AML MV4-11 cell (IC50 ≤0.3 uM). ZEN-3694 inhibits tetra-acetylated histone H4 binding to BRD4 bromodomain 1 (IC50 ≤0.3 uM).
    ZEN-3694
  • HY-13032B
    Molibresib besylate
    		Inhibitor
    Molibresib besylate (GSK 525762C; I-BET 762 besylate) is an orally active pan-BET inhibitor that targets and binds to BRD2, BRD3, BRD4 and BRDT. By competitively occupying acetylated lysine binding sites, Molibresib besylate disrupts the interaction between BET proteins and chromatin, thereby effectively inhibiting MYC expression and target gene transcription. Molibresib besylate exhibits broad antiproliferative activity, which not only inhibits cancer cell growth and induces growth arrest, but also downregulates mitosis-related genes and upregulates the level of p-ERK1/2. When combined with MEK inhibitors, Molibresib besylate shows a significant synergistic effect, reduces tumor burden in mouse models of leukemia, modulates the immune microenvironment and prolongs survival. Molibresib besylate is widely applicable to research related to acute myeloid leukemia, multiple myeloma, triple-negative breast cancer, small-cell lung cancer and various advanced refractory solid tumors.
    Molibresib besylate
  • HY-163638
    BRD4 degrader-1
    		Degrader 99.85%
    BRD4 degrader-1 (Compound mL 1-50) is a relatively selective, monovalent and covalent BRD4 Molecular glue degrader. BRD4 degrader-1 induces degradation of both long and short isoforms of BRD4 by targeting DCAF16 (an E3 ligase). BRD4 degrader-1 can be used in breast cancer research.
    BRD4 degrader-1
  • HY-148739
    dBRD 9-A
    		Degrader 99.50%
    dBRD 9-A is a selective BRD9 PROTAC degrader. dBRD 9-A induces near complete BRD9 degradation dependent on E3 ubiquitin ligase CRBN and BRD9 bromodomain engagement, and drives loss of BRD9 chromatin binding genome-wide. dBRD 9-A downregulates oncogenic SS18-SSX-driven transcriptional programs, super enhancer-associated gene expression, and SS18-SSX1 super enhancer binding, and depletes GBAF complex members GLTSCR1/1L from SS18-SSX complexes. dBRD 9-A induces cell cycle arrest and increases apoptosis in synovial sarcoma cells. dBRD 9-A can be used for the research of synovial sarcoma.
    dBRD 9-A
  • HY-156568B
    SMD-3040 formate
    		Degrader 99.78%
    SMD-3040 formate is a potent and selective SMARCA2 PROTAC degrader (DC50: 12 nM; Dmax: 91%). SMD-3040 formate can inhibit tumor cell proliferation and exhibits antitumor activity. SMD-3040 formate can be used in the study of tumors such as melanoma. (SMARCA2/4-ligand (HY-171765); HY-112078 VHL ligand (HY-112078))
    SMD-3040 formate
  • HY-158031
    PLK1/BRD4-IN-5
    		Inhibitor 98.80%
    PLK1/BRD4-IN-5 (Compound SC10) is an orally active PLK1 and BRD4 inhibitor with IC50 values of 0.3  nM and 60.8  nM, respectively. PLK1/BRD4-IN-5 can induce MV4-11 cell block in S phase and apoptosis) in a dose-dependent manner. PLK1/BRD4-IN-5 can be used in cancer research.
    PLK1/BRD4-IN-5
  • HY-119769
    XX-650-23
    		Inhibitor 99.90%
    XX-650-23 is a potent CREB inhibitor. XX-650-23inhibits CREB function through disruption of CBP-CREB interaction. XX-650-23 can be used for AML research.
    XX-650-23
  • HY-101125
    L-Moses
    		Inhibitor 99.97%
    L-Moses (L-45), a chemical probe, is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126 nM.
    L-Moses
  • HY-111905
    BRD7-IN-1
    		Inhibitor 99.77%
    BRD7-IN-1, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC50s of 4.5 and 1.8 nM, respectively).
    BRD7-IN-1
  • HY-103633
    PROTAC BET Degrader-1
    		Inhibitor 99.41%
    PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
    PROTAC BET Degrader-1
  • HY-129939
    BET-IN-31
    		Inhibitor 99.85%
    BET-IN-31 is a potent BET inhibitor and a ligand for target BRD4 protein for PROTACT GNE-987 (HY-129937A).
    BET-IN-31
  • HY-112429
    HJB97
    		Inhibitor 98.05%
    HJB97 is a high-affinity BET inhibitor with Ki values of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), and 1.0 nM (BRD4 BD2). HJB97 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC BET degraders with antitumor activity. HJB97 can be used for the synthesis of BETd-260 (HY-101519).
    HJB97
  • HY-125837A
    MS31 trihydrochloride
    		Inhibitor 98.0%
    MS31 trihydrochloride is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 trihydrochloride potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 trihydrochloride selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 trihydrochloride potently inhibits binding of trimethyllysine-containing peptides to SPIN1, and is not toxic to nontumorigenic cells.
    MS31 trihydrochloride
Cat. No. Product Name / Synonyms Application Reactivity