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.

Epigenetic Reader Domain Isoform Specific Products:

Epigenetic Reader Domain Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-180184
    DLG-41nc
    		Control
    DLG-41nc is the negative control for DLG-41 (HY-180183). DLG-41nc shows no GAS41 YEATS domain inhibition (IC50: >50 μM in AlphaLISA). DLG-41 has anticancer activity against NSCLC.
    DLG-41nc
  • HY-N1506R
    Ganodermanontriol (Standard)
    		Modulator
    Karbutilate (Standard) is the analytical standard of Karbutilate. This product is intended for research and analytical applications. Karbutilate (NIA-11092) is a nonselective soil-active herbicide which is used to kill one-leaf pinyon saplings.
    Ganodermanontriol (Standard)
  • HY-159456
    PROTAC SMARCA2/4-degrader-5
    		Degrader
    PROTAC SMARCA2/4-degrader-5 (Compound I-437) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-5 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 of 100-500 nM.
    PROTAC SMARCA2/4-degrader-5
  • HY-162815
    PROTAC SMARCA2/4-degrader-26
    PROTAC SMARCA2/4-degrader-26 (compound 6) is a PROTAC targeting SMARCA2/4. SMARCA2 and SMARCA4 are genes and cancer targets with complementary functions that catalyze nucleosome movement. PROTAC SMARCA2/4-degrader-25 is composed of PROTAC target protein ligand 2-(4-(3-Amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)acetic acid (HY-46618) (red part), E3 ligase ligand (2S,4R)-4-Hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (HY-W998248) (blue part), PROTAC linker (S)-2-Amino-3,3-dimethylbutanoic acid (HY-59140) (black part), and the conjugate composed of E3 ubiquitin ligase ligand + Linker is (S,R,S)-AHPC (HY-125845)[1].
    PROTAC SMARCA2/4-degrader-26
  • HY-181834
    PROTAC MLLT1 Degrader-1
    		Degrader
    PROTAC MLLT1 Degrader-1 is a PROTAC degrader targeting MLLT1. PROTAC MLLT1 Degrader-1 inhibits AML cell proliferation and viability, suppresses tumor growth in human AML xenograft models, and can block the oncogene transcriptional program. PROTAC MLLT1 Degrader-1 can be used for the research of MLL-rearranged acute myeloid leukemia (AML).
    PROTAC MLLT1 Degrader-1
  • HY-161710
    XYD129
    		Degrader
    XYD129 is an effective CBP/p300 PROTAC degrader. XYD129 has antiproliferative activity on MV4-11 cell line (IC 50=0.044 μM). XYD129 can be used for the study of acute myeloid leukemia (AML). (Structure Note: Pink, CBP/p300 ligand 5 (HY-161711); Blue, E3 ligase ligand (HY-41547); Black, Linker (HY-40178)).
    XYD129
  • HY-161889
    DCSM06-05
    		Inhibitor
    DCSM06-05 is a potent SMARCA2-BRD inhibitor with an IC50 value of 9 µM, a Kd value of 22.4 µM.
    DCSM06-05
  • HY-180923
    AB3145
    		Degrader
    AB3145 is a selective Brd4 BromoTag PROTAC degrader (DC50: 120-140 pM). AB3145 promotes the ubiquitination and degradation of Brd4. AB3145 can be used in cancer research.
    AB3145
  • HY-114207
    VinSpinIn
    		Inhibitor
    VinSpinIn is a Spindlin1 inhibitor (KD: 9.9 nM for SPIN149-262). VinSpinIn is a chemical probe for tudor domain of Spindlin1. VinSpinIn can be used to study chromatin function.
    VinSpinIn
  • HY-104072
    BRD4-IN-3
    		Inhibitor
    BRD4-IN-3 (compound 141) is a potent BRD4 inhibitor with an IC50 of <0.5 µM. BRD4-IN-3 shows cytoxicity for MYC-Raji with an IC50 value of >1 µM.
    BRD4-IN-3
  • HY-153593
    BET bromodomain inhibitor 3
    		Inhibitor
    BET bromodomain inhibitor 3 is BET bromodomain inhibitor. BET bromodomain inhibitor 3 has inhibitory effect against BrdT with Ki value of > 40 µM. BET bromodomain inhibitor 3 can be used for the research of contraception, cancer, and heart disease.
    BET bromodomain inhibitor 3
  • HY-182371
    BRD4 ligand 15
    		Ligand
    BRD4 ligand 15 (compound 5) is a BRD4 ligand and alkyne-modified chalcone derivative, which serves as a building block for the synthesis of BRD4-targeting PROTAC TKP-5 (HY-182370).
    BRD4 ligand 15
  • HY-W494890
    SMARCA2-IN-10
    		Inhibitor
    SMARCA2-IN-10 (Compound 4) is a highly selective SMARCA2 ATPase domain inhibitor (IC50=17.676 μM). SMARCA2-IN-10 induces cell death in SMARCA4-deficient tumors. SMARCA2-IN-10 is promising for research of SMARCA4-mutant non-small cell lung cancer, small cell ovarian carcinoma, and melanoma.
    SMARCA2-IN-10
  • HY-161884
    SMARCA2/4-IN-1
    		Inhibitor
    SMARCA2/4-IN-1 (compound 1) is a potent SMARCA2 inhibitor with IC50 values of 3.8, 1.7 µM for SMARCA2, SMARCA4, respectively.
    SMARCA2/4-IN-1
  • HY-182362
    TK-285
    TK-285 is a potent TSLP inhibitor that suppresses the production of TSLP and inhibits the expression of interleukin-33 mRNA. TK-285 exhibits a selective binding preference for the BD1 domains of BRD2, BRD3, BRD4 and BRDT. TK-285 can be used in research related to atopic dermatitis.
    TK-285
  • HY-176056
    Hedgehog IN-9
    		Agonist
    Hedgehog IN-9 (Compound 1) is a Hedgehog inhibitor. Hedgehog IN-9 prevents GLI1 expression and enhances cellular BRD2 protein levels. Hedgehog IN-9 inhibits growth of medulloblastoma spheroid cells and can be used for synthesis of photoaffinity labeling probe.
    Hedgehog IN-9
  • HY-115663
    C620-0696
    		Inhibitor
    C620-0696 is an inhibitor targeting the brom domain of BPTF, with a KD value of 35.5 μM. C620-0696 can exert cytotoxic effects on A549 and H358 cells, inhibiting the expression of c-Myc. C620-0696 inhibits cell migration and colony formation, and induces apoptosis and cell cycle arrest. C620-0696 can be used in the research of non-small cell lung cancer.
    C620-0696
  • HY-152469
    Eleven-Nineteen-Leukemia Protein IN-1
    		Inhibitor
    Eleven-Nineteen-Leukemia Protein IN-1 is an inhibitor of ENL YEATS domain with an IC50 value of 14.5 nM. Eleven-Nineteen-Leukemia Protein IN-1 interacts with ENL protein and enhances the thermal stability of ENL protein in vitro.
    Eleven-Nineteen-Leukemia Protein IN-1
  • HY-163108
    ATAD2-IN-1
    		Inhibitor
    ATAD2-IN-1 (compound 19f) is a potent ATAD2 inhibitor (IC50: 0.27 μM) and can induce apoptosis. ATAD2-IN-1 also inhibits c-Myc activation and BT-549 cell migration.
    ATAD2-IN-1
  • HY-151531
    PBRM1-BD2-IN-4
    		Inhibitor
    PBRM1-BD2-IN-4 is a PBRM1-BD2 inhibitor with an IC50 of 0.2 μM, and its Kd values for PBRM1-BD2 and PBRM1-BD5 are 5.5 μM and 11.1 μM, respectively. PBRM1-BD2-IN-4 selectively inhibits the proliferation of PBRM1-dependent prostate cancer cells. PBRM1-BD2-IN-4 can be used in studies related to prostate cancer.
    PBRM1-BD2-IN-4
Cat. No. Product Name / Synonyms Application Reactivity
Epigenetic Reader Domain Isoform Comparison

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