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-153459
    IBG1
    		Degrader 98.83%
    IBG1 is a molecular glue degrader targeting BRD2 and BRD4 (DC50: 0.15 nM). IBG1 has no significant degradation effect on its paralogue BRD3. IBG1 can inhibit the growth of cancer cells and can be used in tumor research. (Pink: BRD2/BRD4 Ligand (HY-111139); Black: Linker; Blue: DCAF15 ligand-1 (HY-W037495)).
    IBG1
  • HY-101460
    Tz-Thalidomide
    		Degrader 98.60%
    Tz-Thalidomide is a tetrazine tagged Thalidomide (HY-14658) (Ligands for E3 Ligase). Tz-Thalidomide has binding affinity for BRD4, with IC50s of 46.25 μM (BRD4-1) and 62.55 μM (BRD4-2). Tz-Thalidomide is a click chemistry reagent, it contains a Tetrazine group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing TCO groups.
    Tz-Thalidomide
  • HY-15223
    MI-3
    		Inhibitor 99.58%
    MI-3 (Menin-MLL inhibitor 3) is a potent and high affinity menin-MLL inhibitor with an IC50 of 648 nM and a Kd of 201 nM.
    MI-3
  • 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-133131
    PROTAC BRD4 Degrader-1
    		Inhibitor 99.31%
    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-109050
    Alobresib
    		Inhibitor 98.04%
    Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc. Alobresib can be used in the metastatic castration-resistant prostate cancer (mCRPC) research.
    Alobresib
  • 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-103632
    PROTAC BRD9 Degrader-1
    		Inhibitor 99.16%
    PROTAC BRD9 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD9 (IC50=13.5 nM), which can be used as a selective probe useful for the study of BAF complex biology.
    PROTAC BRD9 Degrader-1
  • HY-144897
    FHT-1204
    		Inhibitor 99.81%
    FHT-1204 is a potent SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor with IC50s of ≤10 nM (WO2020160180A1; compound 70).
    FHT-1204
  • 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-114162A
    VTP50469 fumarate
    		Inhibitor 99.79%
    VTP50469 fumarate is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 fumarate has potently anti-leukemia activity.
    VTP50469 fumarate
  • HY-111976
    MT1
    		Inhibitor 99.69%
    MT1 is a bivalent chemical probe of BET bromodomains, with an IC50 of 0.789 nM for BRD4(1).
    MT1
  • HY-123911
    dBET23
    		Inhibitor
    dBET23 is a highly effective and selective PROTAC BRD4 degrader with a DC50/5h of ~ 50 nM for BRD4BD1 protein.
    dBET23
  • 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-153894
    SRX3177
    		Inhibitor 99.59%
    SRX3177 is a triple inhibitor of CDK4/6, PI3K, and BRD4, with IC50s of 33 nM (BRD4 BD1), 89 nM (BRD4 BD2), 79 nM (PI3Kα), 83 nM (PI3Kδ), 3.18 μM (PI3Kγ), <2.5 nM (CDK4), 3.3 nM (CDK6), respectively. SRX3177 blocks the interaction between the SARS-CoV-2 E protein and the BRD2/4 BD1 domain, restores E protein-attenuated NF-κB activity. SRX3177 exerts broad cytotoxic activity against cancer cells. SRX3177 can be used for the study of anti-SARS-CoV-2 and cancer.
    SRX3177
  • HY-107477
    GSK8573
    		99.53%
    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-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-141703A
    DC-BPi-11 hydrochloride
    		Inhibitor
    DC-BPi-11 hydrochloride is an inhibitor of bromodomain PHD finger transcription factor (BPTF), with an IC50 value of 698 nM. DC-BPi-11 hydrochloride shows remarkable inhibition against leukemia cell proliferation.
    DC-BPi-11 hydrochloride
  • 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-112316
    BAY1238097
    		Inhibitor 99.02%
    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 (IC50 <100 nM).
    BAY1238097
Cat. No. Product Name / Synonyms Application Reactivity