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-142674
    BRD4-BD1/2-IN-1
    		Inhibitor
    BRD4-BD1/2-IN-1 is a potent BRD4 inhibitor with IC50s of <100 nM for BRD4 BD-1 and BRD4 BD-2, respectively (US20150148375A1, compound 5).
    BRD4-BD1/2-IN-1
  • HY-15222A
    Menin-MLL inhibitor MI-2 dihydrochloride
    		Inhibitor
    Menin-MLL inhibitor MI-2 dihydrochloride is a competitive and selective Menin-MLL interaction inhibitor with an IC50 value of 446 nM and a Ki value of 158 nM. Menin-MLL inhibitor MI-2 dihydrochloride downregulates the expression of target genes such as HOXA9 and MEIS1, inhibits proliferation of leukemia cells and induces apoptosis and differentiation. Menin-MLL inhibitor MI-2 dihydrochloride is proming for rasearch of MLL-rearranged acute leukemias (e.g., AML, ALL).
    Menin-MLL inhibitor MI-2 dihydrochloride
  • HY-153945
    BET-IN-15
    		Inhibitor
    BET-IN-15 (compound 1) is a potent and orally active BET inhibitor with IC50 values of 0.64，0.25 nM for BRD4-BD1，BRD4-BD2，respectively. BET-IN-15 shows antiproliferative activity.
    BET-IN-15
  • HY-169355
    TrimTAC1
    		Degrader
    TrimTAC1 is a TRIM21-based PROTAC targeting BRD4. TrimTAC1 selectively degrads NUP98FG-mEGFP-BRD4BD2 nuclear condensates. TrimTAC1 does not degrade soluble mEGFP-BRD4BD2 in A549 cells. (Pink: target protein ligand (+)-JQ-1 (HY-13030); Blue:E3 ligase ligand Acepromazine-OTs (HY-169356); Black: PROTAC linker (HY-W088456); E3 ligase ligand + linker: HY-169357).
    TrimTAC1
  • HY-168635
    SJ46420
    		Inhibitor
    SJ46420, a SJ46421 (HY-168634) pro-drug variant, is a potent and selective BRD3 PROTAC degrader. SJ46420 degrads BRD3 in a KLHDC2-dependent manner, thereby partially reducing the levels of BRD2 or BRD4 (Pink: ligand for target protein (HY-13030); Black: linker (HY-20797); Blue: E3 ligase ligand (HY-159973)).
    SJ46420
  • HY-149806
    Bromodomain IN-2
    		Inhibitor
    BD-IN-1 is a pan bromodomain (BD) inhibitor with KD values of 250, 420, 130, 430, 67, 240, 970 nM for BRD4(1), CBP, BRPF1B, BRD7, BRD9, BRDT(1), CECR2 respectively. BD-IN-1 shows antiproliferative activity.
    Bromodomain IN-2
  • HY-151366
    HDAC8/BRPF1-IN-1
    		Inhibitor
    HDAC8/BRPF1-IN-1 (Compound 23a) is a dual inhibitor of HDAC8 and BRPF1 with an IC50 of 443 nM against human HDAC8 and a Kd of 67 nM against human BRPF1. HDAC8/BRPF1-IN-1 shows low in vitro activity against HDAC1 and 6.
    HDAC8/BRPF1-IN-1
  • HY-152209
    BRD4 Inhibitor-26
    		Inhibitor
    BRD4 Inhibitor-26 is a bromodomain protein 4 (BRD4) inhibitor/nitric oxide-donator. BRD4 Inhibitor-26 inhibits BRD4 (BD1) and BRD4 (BD2) with IC50 values of 0.82 μM and 1.94 μM, respectively. BRD4 Inhibitor-26 can be used for the research of ovarian cancer.
    BRD4 Inhibitor-26
  • HY-153573
    SRG-II-19F
    		Degrader
    SRG-II-19F (dCym-JQ1) is a bromodomain1 of BRDT (BRDTBD1) PROTAC degrader. SRG-II-19F can be used for testing the regulatory effect of ClpC2 on the ClpC1P1P2 protease.
    SRG-II-19F
  • HY-132128
    BRD4 Inhibitor-12
    		Inhibitor
    BRD4 Inhibitor-12 (Compound 9) is a BRD4 ligand, and can be used for research of cancer, infammation.
    BRD4 Inhibitor-12
  • HY-13031
    GW 841819X
    GW 841819X is a potent inducer of the ApoA1 report gene, with an EC170 of 0.22 µM, and its pIC50 for Brd2/3/4 is 5.9/6.2/6.3.
    GW 841819X
  • HY-163873
    PROTAC SMARCA2/4-degrader-20
    		Degrader
    PROTAC SMARCA2/4-degrader-20 (Compound I-405) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2. PROTAC SMARCA2/4-degrader-20 degrades SMARCA2 in A549 and MV411 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 of 100-500 nM. (Pink: Ligand for Target Protein (HY-159545); Black: Linker (HY-W006635); Blue: Ligand for E3 Ligase (HY-163932))
    PROTAC SMARCA2/4-degrader-20
  • HY-145909
    BRD4 Inhibitor-17
    		Inhibitor
    BRD4 Inhibitor-17 (Compound 5i) is a potent inhibitor of BRD4 with an IC50 of 0.33 μM. BRD4 Inhibitor-17 plays crucial role in regulating transcription of inflammatory, proliferation and cell cycle genes. BRD4 Inhibitor-17 serves as potential antidotes for arsenicals.
    BRD4 Inhibitor-17
  • HY-176369
    PROTAC BRD4 ligand-1-NH-PEG-phenol-PEG-COOtBu
    		Ligand
    PROTAC BRD4 ligand-1-NH-PEG-phenol-PEG-COOtBu is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for BRD4 and a PROTAC linker. PROTAC BRD4 ligand-1-NH-PEG-phenol-PEG-COOtBu can be used for synthesis of PROTAC BRD4 Degrader-14 (HY-138637).
    PROTAC BRD4 ligand-1-NH-PEG-phenol-PEG-COOtBu
  • HY-150516S
    BET-IN-12
    		Inhibitor
    BET-IN-12 is an orally avtive inhibitor of bromodomain and extra-terminal (BET) with an IC50 of 0.9 nM for BRD4.
    BET-IN-12
  • HY-175678
    PROTAC BRD2 BD1 Degrader-1
    		Degrader
    PROTAC BRD2 BD1 Degrader-1 (compound 21-1) is a potent and selective BRD2 BD1 PROTAC degrader. PROTAC BRD2 BD1 Degrader-1 induces the association of BRD2 BD1 and von Hippel–Lindau-elongin C-elongin B (VCB). (Pink: BRD2-BD1 Ligand (HY-175679); Blue: E3 ligase ligand (HY-125845); Black: Linker (HY-W069332)).
    PROTAC BRD2 BD1 Degrader-1
  • HY-143471
    WNY0824
    		Inhibitor
    WNY0824 (PLK1/BRD4-IN-1) is an orally active dual inhibitor of PLK1 and BET protein families, with IC50 values ​​of 22, 402.5, 150.7, 103.9, and 311.9 nmol/L for PLK1, BRD2, BRD3, BRD4, and BRDT, respectively. WNY0824 induces cell cycle arrest and apoptosis by inhibiting AR- and MYC-mediated transcriptional processes. In addition, WNY0824 also inhibits tumor growth in Enzalutamide (HY-70002) resistant CRPC xenograft tumor models.
    WNY0824
  • HY-175867
    PROTAC SMARCA2 degrader-34
    		Degrader
    PROTAC SMARCA2 degrader-34 (compound 52) is a selective SMARCA2 PROTAC degrader (DC50 in HeLa cell: < 0.1 μM for SMARCA2, > 1 μM for SMARCA4). PROTAC SMARCA2 degrader-34 can be used for study of cancer. (Pink: SMARCA2 ligand (HY-178414) ; Blue: E3 ligand (HY-168055) ; Black: linker).
    PROTAC SMARCA2 degrader-34
  • HY-173433
    JV8
    		Degrader
    JV8 is a BRD4 PROTAC degrader. JV8 promotes the ubiquitination and degradation of BRD4 and induces apoptosis. JV8 has antitumor activity in a mouse 4T1 orthotopic tumor model. (Pink: BRD4 ligand (HY-78695); Blue: E3 ligase VHL ligand (HY-173435); Black: Linker (HY-33366); E3 ligase VHL ligand-linker conjugate (HY-173436)).
    JV8
  • HY-174866
    BT-O2C
    		Inhibitor
    BT-O2C is a highly selective p300 PROTAC degrader. BT-O2C can significantly degrade the level of p300 in HAP1 cells. BT-O2C has significant cytotoxicity in CIC:DUX4 sarcoma (CDS) cell lines (IC50 ranges from 152 to 221 nM) and significantly reduces the expression of CDS target genes (ETV1, ETV4, ETV5). BT-O2C can be used for research on cancer. (Pink: p300 Ligand (HY-174868); Blue: CRBN Ligand (HY-W023573); Black: Linker; CRBN Ligand+Linker (HY-174869)).
    BT-O2C
Cat. No. Product Name / Synonyms Application Reactivity