2. Signaling Pathways
  3. Epigenetics
  4. Epigenetic Reader Domain

Epigenetic Reader Domain

Epigenetic Reader Domain

Related Products

PDF 3.95 MB

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-138555
    PROTAC BRD4 Degrader-8
    		Inhibitor 99.45%
    PROTAC BRD4 Degrader-8 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells.
    PROTAC BRD4 Degrader-8
  • HY-149458
    FHT-2344
    		Inhibitor 99.67%
    FHT-2344 is a SMARCA4/SMARCA2 ATPase inhibitor with IC50 values of 0.026 μM and 0.013 μM, respectively. FHT-2344 has anticancer activity.
    FHT-2344
  • HY-107477
    GSK8573
    		99.05%
    GSK8573 is an inactive control compound for GSK2801 (acetyl-lysine competitive inhibitor of BAZ2A and BAZ2B bromodomains). GSK8573 has binding activity to BRD9 with a Kd value of 1.04 μM and is inactive against BAZ2A/B and other bromodomain familiy. GSK8573 can be used as a structurally related negative control compound in biological experiments.
    GSK8573
  • HY-114204
    GSK8814
    		Inhibitor 99.60%
    GSK8814 is a potent, selective, and ATAD2/2B bromodomain chemical probe and inhibitor, with a binding constant pKd=8.1 and a pKi=8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with pIC50s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4 BD1.
    GSK8814
  • HY-15839
    UNC 669
    		Inhibitor 99.74%
    UNC 669, a ligand for a methyl-lysine binding domain, is a potent L3MBTL1 (IC50=4.2 uM) and L3MBTL3 (3.1 uM) inhibitor.
    UNC 669
  • 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-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-133737
    PROTAC BRD4 Degrader-5
    		Inhibitor 99.93%
    PROTAC BRD4 Degrader-5 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-5 can potent degrade BRD4 in HER2 positive and negative breast cancer cell lines.
    PROTAC BRD4 Degrader-5
  • HY-117491
    BRD4 Inhibitor-10
    		Inhibitor 99.52%
    BRD4 Inhibitor-10 is a potent BRD4-BD1 inhibitor extracted from patent WO2015022332A1, Compound II-25, has an IC50 of 8 nM.
    BRD4 Inhibitor-10
  • HY-114504
    RVX-297
    		Inhibitor
    RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models.
    RVX-297
  • 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-156568B
    SMD-3040 formate
    		Degrader 99.90%
    SMD-3040 formate is a potent and selective smarca2 protac degrader with strong in vivo antitumor activity.
    SMD-3040 formate
  • HY-157486
    KMI169
    		Inhibitor 98.00%
    KMI169 is a potent and selective bi-substrate inhibitor targeting the SAM and substrate binding pockets of KMT9. KMT9 monomethylates histone H4 lysine 12 and controls the proliferation of prostate cancer cells. KMI169 can be used for the research of prostate cancer.
    KMI169
  • HY-156214
    NICE-01
    		99.53%
    NICE-01 (AP1867-PEG2-JQ1; AP-PEG2-JQ1) is a bifunctional compound that bind to proteins in separate cellular compartments that can induce nuclear import of cytosolic cargoes, using nuclear-localized bromodomain-containing protein 4 (BRD4) as a “carrier” for co-import and nuclear trapping of cytosolic proteins.
    NICE-01
  • 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-133131
    PROTAC BRD4 Degrader-1
    		Inhibitor 99.12%
    PROTAC BRD4 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC50 of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression.
    PROTAC BRD4 Degrader-1
  • 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-145310
    ZL0590
    		Inhibitor 99.86%
    ZL0590 is a potent, orally active BRD4 BD1-selective inhibitor with an IC50 of 90 nM for human BRD4 BD1. ZL0590 exhibits significant anti-inflammatory activities.
    ZL0590
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity