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-156568
    SMD-3040
    		Degrader 99.91%
    SMD-3040 is a potent and selective of SMARCA2 PROTAC degrader (DC50: 12 nM). SMD-3040 contains SMARCA2/4 ligand, linker and VHL ligand. SMD-3040 demonstrates excellent degradation selectivity for SMARCA2 protein over SMARCA4 protein.SMD-3040 achieves strong tumor growth inhibition in xenograft models.
    SMD-3040
  • 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 exerts broad cytotoxic activity against cancer cells, but acts friendly with normal epithelial cells.
    SRX3177
  • HY-153459
    PROTAC BRD4 Degrader-19
    		Degrader 98.83%
    PROTAC BRD4 Degrader-19 (compound 176) is a PROTAC that targets BRD4 protein for degradation. PROTAC BRD4 Degrader-19 can be used in cancer research.
    PROTAC BRD4 Degrader-19
  • HY-153714
    BN-104
    		Inhibitor 98.60%
    BN-104 (BNM-1192) is an effective selective brain membrane protein inhibitor with oral activity, and it's also a Menin inhibitor, it can block the Menin-MLL interaction and leads to the degradation of Menin protein. BN-104 is a weak hERG inhibitor, with an IC50 greater than 100 μM. BN-104 has anti-tumor activity and can be used in cancer research, such as for acute myeloid leukemia.
    BN-104
  • HY-115568
    BETd-246
    		Inhibitor 98.34%
    BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity.
    BETd-246
  • HY-16510
    UNC926
    		Inhibitor 99.82%
    UNC926 is a methyl-lysine (Kme) reader domain inhibitor that inhibits L3MBTL1 with an IC50 of 3.9 μM.
    UNC926
  • 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-112610
    CF53
    		Inhibitor 99.81%
    CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo.
    CF53
  • 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-107442
    PROTAC BRD4-binding moiety 1
    PROTAC BRD4-binding moiety 1 is a ligand for BRD4. PROTAC BRD4-binding moiety 1 binds to cereblon ligand via a linker to form PROTAC to degrade BRD4 (HY-133136). PROTAC BRD4-binding moiety 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    PROTAC BRD4-binding moiety 1
  • HY-B1428
    2-Ethoxybenzamide
    		Activator 99.82%
    2-Ethoxybenzamide (Ethenzamide) is a nonsteroidal anti-inflammatory agent that shows analgesic and antipyretic effects. 2-Ethoxybenzamide induces melanin synthesis via cAMP response element-binding protein (CREB) phosphorylation.
    2-Ethoxybenzamide
  • HY-151594
    iBRD4-BD1
    		Inhibitor 98.65%
    iBRD4-BD1 is selective BRD4 bromodomain inhibitor. iBRD4-BD1 has inhibition activity for BRD4 bromodomain with an IC50 value of 12 nM. iBRD4-BD1 can be used for the research of inflammation and oncology.
    iBRD4-BD1
  • 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-101027A
    GSK4028
    		98.06%
    GSK4028 is the enantiomeric negative control of GSK4027, which is a PCAF/GCN5 bromodomain chemical probe, the pIC50 of GSK4028 is 4.9 in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.
    GSK4028
  • HY-160499
    BRD4 Inhibitor-30
    		Inhibitor 99.89%
    BRD4 inhibitor-30 (Compound 1) is a BRD4 inhibitor with a IC50 value of 415 nM.
    BRD4 Inhibitor-30
  • HY-100697
    TPOP146
    		Inhibitor 98.98%
    TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.
    TPOP146
  • HY-136857
    BRD4 degrader-3
    		Degrader 99.43%
    BRD4 degrader-3 is a potent bromodomain BRD4 degrader extracted from patent WO2020055976A1, example 1a, has IC50s of 15.5 and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively. PROTAC BRD4 Degrader-7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    BRD4 degrader-3
  • HY-128347
    M‑89
    		Inhibitor 99.14%
    M-89 is a highly potent and specific menin inhibitor, with a Kd of 1.4 nM for binding to menin. M-89 inhibits the menin-mixed lineage leukemia (Menin-MLL) protein-protein interaction and has potential to treat MLL leukemia.
    M‑89
  • HY-130256
    β-NF-JQ1
    		Inhibitor 99.37%
    β-NF-JQ1 is a PROTAC that recruits Aryl Hydrocarbon Receptor E3 ligase to target proteins. β-NF-JQ1 is directed against bromodomain-containing (BRD) proteins using β-NF as an AhR ligand, induces the interaction of AhR and BRD proteins, and displays effective anticancer activity that correlated with protein knockdown activity.
    β-NF-JQ1
  • HY-111445
    CeMMEC1
    		Inhibitor 99.65%
    CeMMEC1 is an inhibitor of BRD4, and also has high affinity for TAF1, with an IC50 of 0.9 μM for TAF1, and a Kd of 1.8 μM for TAF1 (2).
    CeMMEC1
Cat. No. Product Name / Synonyms Application Reactivity