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-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-117286
    (S)-JQ-35
    		Inhibitor 99.46%
    (S)-JQ-35 (TEN-010) is a selective bromodomain and extra-terminal domain (BET) protein family inhibitor targeting BRD4, BRD3, BRD2 and BRDT. (S)-JQ-35 is orally active and can penetrate the blood-brain barrier. (S)-JQ-35 competitively binds to the bromodomain of BRD4, preventing it from binding to the Myc gene promoter, thereby inhibiting cancer cell proliferation and inducing cell apoptosis. (S)-JQ-35 can be used for targeted therapy research of malignant tumors such as NUT midline carcinoma and refractory solid tumors.
    (S)-JQ-35
  • HY-112149
    ZL0420
    		Inhibitor 98.0%
    ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2.
    ZL0420
  • HY-112718
    PROTAC BET Degrader-10
    		Inhibitor 99.39%
    PROTAC BET Degrader-10 is a potent BET protein BRD4 degrader extracted from patent WO2017007612A1, example 37, connected by ligands for Cereblon and BRD4, with a DC50 of 49 nM.
    PROTAC BET Degrader-10
  • HY-129917
    KB02-JQ1
    		Inhibitor 99.10%
    KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1.
    KB02-JQ1
  • HY-132197
    CBP/p300-IN-12
    		Inhibitor 99.72%
    CBP/p300-IN-12 is a potent and selective covalent histone acetyltransferases p300 (IC50 of 166 nM) and CBP inhibitor. CBP/p300-IN-12 decreases the levels of H3K27Ac of PC-3 cells (EC50 of 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450.
    CBP/p300-IN-12
  • 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-141890
    BAZ1A-IN-1
    		Inhibitor 99.91%
    BAZ1A-IN-1 is a potent inhibitor of BAZ1A (bromodomain-containing protein). BAZ1A-IN-1 shows a KD value of 0.52 μM against BAZ1A bromodomain. BAZ1A-IN-1 shows good anti-viability activity against cancer cell lines expressing a high level of BAZ1A, but weak or no activity against cancer cells with a low expression level of BAZ1A.
    BAZ1A-IN-1
  • HY-158764
    PROTAC BET Degrader-12
    		Degrader 98.10%
    PROTAC BET Degrader-12 (Compound 8b) is a PROTAC degrader for bromodomain and extra-terminal domain (BET)-containing proteins, which degrades the BRD3 and BRD4 in a DCAF11-dependent manner. PROTAC BET Degrader-12 inhibits cell viability of KBM7 with a DC50 of 305.2 nM. (Pink: ligand for target protein (+)-JQ-1 (HY-13030); Black: linker (HY-159077); Blue: ligand for E3 ligase (HY-159076))
    PROTAC BET Degrader-12
  • HY-19319
    MI-136
    		Inhibitor 99.04%
    MI-136 is an inhibitor of the menin-MLL protein-protein interaction (PPI), with an IC50 of 31 nM and a Kd of 23.6 nM. MI-136 shows to block AR signaling and has the potential for the study in castration-resistant tumors.
    MI-136
  • HY-111102
    FL-411
    		Inhibitor 99.05%
    FL-411 is a potent and selective BRD4 inhibitor with an IC50 of 0.43±0.09 μM for BRD4(1).
    FL-411
  • HY-115881
    SR-1114
    		Degrader 99.04%
    SR-1114 is a PROTAC degrader targeting ENL. SR-1114 degrades ENL in a CRBN-dependent manner and selectively downregulates ENL target genes. SR-1114 can promote the differentiation of acute myeloid leukemia cells. SR-1114 can be used in tumor research. (Pink: ENL ligand (HY-145409); Black: Linker; Blue: E3 Ligand (HY-14658)).
    SR-1114
  • HY-132234
    M-1211
    		Inhibitor 99.29%
    M‑1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression.
    M-1211
  • HY-125236
    BET-IN-19
    		Inhibitor 99.74%
    BET-IN-19 (Compound 146) is a BET inhibitor. BET-IN-19 inhibits hlL-6 mRNA transcription (IC50 ≤0.3 uM), and c-myc activity in human AML MV4-11 cell (IC50 ≤0.3 uM)。BET-IN-19 inhibits tetra-acetylated histone H4 binding to BRD4 bromodomain 1 (IC50 ≤0.3 uM).
    BET-IN-19
  • HY-147008
    XP-524
    		Inhibitor 98.02%
    XP-524 is a potent BET and EP300 inhibitor. XP-524 shows great tumoricidal activity in vivo. XP-524 prevents KRAS-induced, neoplastic transformation in vivo and extends survival in two transgenic mouse models of aggressive PDAC. XP-524 also enhances the presentation of self-peptide and tumor recruitment of cytotoxic T lymphocytes. XP-524 has the potential for the research of pancreatic ductal adenocarcinoma (PDAC).
    XP-524
  • HY-130622
    LT052
    		Inhibitor 98.77%
    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-161515
    BRD4/NAMPT-IN-1
    		Inhibitor 99.45%
    BRD4/NAMPT-IN-1 (Compound A2) shows strong inhibitory effects on NAMPT and BRD4 (IC50=35 nM (NAMPT) and 58 nM (BRD4)). BRD4/NAMPT-IN-1 inhibits the growth and migration of hepatocellular carcinoma cells and promotes apoptosis. BRD4/NAMPT-IN-1 also shows potent anticancer effects in HCCLM3 xenograft mouse model, with no obvious toxic effects.
    BRD4/NAMPT-IN-1
  • HY-163638
    BRD4 degrader-1
    		Degrader 99.85%
    BRD4 degrader-1 (Compound ML 1-50) is a monovalent and covalent molecular glue BRD4 degrader. BRD4 degrader-1 targets DCAF16 (E3 ligase) and degrades both the long and short isoforms of BRD4 in cells.
    BRD4 degrader-1
  • HY-148864
    JQ1-TCO
    		Inhibitor 99.95%
    JQ1-TCO is the double bond E configuration of JQ1-TCO (HY-148864A). JQ1-TCO (JQ1-trans-cyclooctene) is a derivative of JQ1 (HY-13030), an inhibitor of BET. JQ1-TCO is suitable for click chemistry and can be used as molecular probes in vitro and in vivo.
    JQ1-TCO
  • HY-P5763
    Phoenixin-20
    		99.66%
    Phoenixin-20 (PNX-20) is a bioactive peptide with hormone-like actions in vertebrates, and can stimulates hypothalamo-pituitary-gonadal hormones and regulate reproductive processes in mammals. Phoenixin-20 promotes neuronal mitochondrial biogenesis via CREB-PGC-1α pathway. Phoenixin-20 has anxiolytic effect.
    Phoenixin-20
Cat. No. Product Name / Synonyms Application Reactivity