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-177041
    PROTAC BRD4 Degrader-35
    		Degrader
    PROTAC BRD4 Degrader-35 (Compound 17) is a PROTAC degrader of BRD4. PROTAC BRD4 Degrader-35 can be studied in anticancer research. (Pink: BRD4 ligand (HY-78695); Black: linker; Blue: ligase).
    PROTAC BRD4 Degrader-35
  • HY-175767
    PROTAC BRD4 Degrader-39
    		Degrader
    PROTAC BRD4 Degrader-39 is a selective targeting Bromodomain protein 4 (BRD4) degrader with an DC50 value of 24.66 nM. PROTAC BRD4 Degrader-39 conjugates BRD PROTAC (ARV-771) (HY-100972) with carbohydrate. PROTAC BRD4 Degrader-39 selectively delivers to tumor cells with high GLUT1 expression, followed by GSH-triggered release of ARV-771 and degrades BRD4. PROTAC BRD4 Degrader-39 can inhibit tumor growth and show no significant toxicity. PROTAC BRD4 Degrader-39 can be used for the research of cancer, such as breast cancer. (Structure Note: Pink: BRD4 ligand (HY-78695); Blue: VHL ligand (HY-112078); Black: (HY-42427); BRD4 ligand-Linker: (HY-42429))
    PROTAC BRD4 Degrader-39
  • HY-152471
    Eleven-Nineteen-Leukemia Protein IN-3
    		Inhibitor
    Eleven-Nineteen-Leukemia Protein IN-3 is an orally active inhibitor of ENL YEATS domain with an IC50 value of 15.4 nM. Eleven-Nineteen-Leukemia Protein IN-3 down-regulates MYC expression through ENL in cells and can enhances the thermal stability of ENL protein in vitro.
    Eleven-Nineteen-Leukemia Protein IN-3
  • HY-142772
    Y08284
    		Inhibitor
    Y08284 is a potent, selective, oral active CBP bromodomain inhibitor with an IC50 of 4.21 nM. Y08284 suppresses the proliferation of prostate cancer cell lines LNCaP, C4-2B, and 22Rv1. Antitumor activity.
    Y08284
  • HY-142743
    Y08175
    		Inhibitor
    Y08175 is a potent CBP bromodomain inhibitor. Y08175 exhibits considerable inhibitory effect with IC50s of 37 and 178.15 nM against CBP bromodomain in AlphaScreen assay and HTRF assay, respectively. Y08175 can be used for the research of prostate cancer.
    Y08175
  • HY-174237
    PBRM1/SMARCA2,4 binder-1
    PBRM1/SMARCA2,4 binder-1 (Compound 17) is a binder of PBRM1, SMARCA2, and SMARCA4 (IC50: 0.083, 0.153, and 0.046 μM, respectively).
    PBRM1/SMARCA2,4 binder-1
  • HY-12625
    MIV-6
    		Inhibitor
    MIV-6 is a small molecule inhibitor that inhibits menin-mixed lineage leukemia (MLL) interaction and exhibits strong selective activity in MLL leukemia cells with IC50 = 56 nM.
    MIV-6
  • HY-157561
    K2-B4-3e
    		Degrader
    K2-B4-3e is a potent BRD4 PROTAC. K2-B4-3e induces BRD4 degradation with a DC50 value of 66 nM.
    K2-B4-3e
  • HY-146709
    BET bromodomain inhibitor 2
    		Inhibitor
    BET bromodomain inhibitor 2 is a potent BET bromodomain inhibitor with an IC50 of 14.1 µM.
    BET bromodomain inhibitor 2
  • HY-158331
    Gal-ARV-771
    		Degrader
    Gal-ARV-771, PROTAC prodrug, is a gal modified ARV-771 (HY-100972). Gal-ARV-771 can be activated in SA-β-Gal-expressed cancer senescent cells to release ARV-771. Gal-ARV-771 induces selective degradation of BRD4 protein by the ubiquitin-proteasome pathway in senescent cells. Gal-ARV-771 promotes apoptosis of senescent cancer cells.
    Gal-ARV-771
  • HY-168251
    PROTAC BRM/BRG1 degrader-3
    		Degrader
    PROTAC BRM/BRG1 degrader-3 (compound 304) is a PROTACs-based BRM/BRG1 degrader with a DC50 of less than 1 nM for BRM degradation in SW1573 cells and a DC50 of greater than 1 nM for BRG1 degradation in SW1573 cells. PROTAC BRM/BRG1 degrader-3 has anti-tumor activity and anti-proliferative activity against A549 cells (IC50=0.6 nM). (Structure Note: PINK, Target protein ligand (HY-168252); Blue, E3 (HY-168253); Black, linker (HY-69260)).
    PROTAC BRM/BRG1 degrader-3
  • HY-168247
    PROTAC BRM/BRG1 degrader-2
    		Degrader
    PROTAC BRM/BRG1 degrader-2 (Example.004) is a PROTAC BRM/BRG1 degrader (DC50: < 10 nM in A549 cell; IC50: 15 nM for A549). Blue: E3 ligase ligand (HY-112078), Black: linker (HY-168249), Pink: BRM/BRG1 inhibitor (HY-168248).
    PROTAC BRM/BRG1 degrader-2
  • HY-162892
    BRD4-IN-9
    		Inhibitor
    BRD4-IN-9 is an orally active BRD4 inhibitor with an IC50 value of 9.4 nM. BRD4-IN-9 can suppress tumor growth in a mouse melanoma xenograft model.
    BRD4-IN-9
  • HY-144318
    CREB-IN-1 TFA
    		Inhibitor
    CREB-IN-1 TFA is a potent, orally active CREB inhibitor (IC50=0.18 µM). CREB-IN-1 TFA inhibits breast cancer cell growth.
    CREB-IN-1 TFA
  • HY-161881
    SMARCA2-IN-9
    		Inhibitor
    SMARCA2-IN-9 (compound 11) is a SMARCA2, PBRM1 bromodomains 2 (PBRM1(2)), and PBRM1 bromodomains 5 (PBRM1(5)) inhibitor with Kd values of 1.6 μM, 2.5 μM, and 3.95 μM, respectively.
    SMARCA2-IN-9
  • HY-114322A
    cis-VZ185
    		Degrader
    cis-VZ185 is a VHL-based PROTACs degrader with the activity of degrading BRD9 and BRD7. cis-VZ185 can be optimized from suboptimal compounds by optimizing the connection mode and linker, and has efficient, rapid and selective degradation of BRD9 and its homologous protein BRD7.
    cis-VZ185
  • HY-159460
    PROTAC SMARCA2/4-degrader-8
    		Inhibitor
    PROTAC SMARCA2/4-degrader-8 (Compound I-502) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2. PROTAC SMARCA2/4-degrader-8 degrades SMARCA2 with DC50 <100 nM in A549 and in MV411, degrades SMARCA4 with DC50<100 nM in MV411(Pink: Ligand for target protein (HY-159545); Black: Linker (HY-W063924); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
    PROTAC SMARCA2/4-degrader-8
  • HY-148367A
    (1s,4s)-Menin-MLL inhibitor-23
    		Inhibitor
    (1s,4s)-Menin-MLL inhibitor-23 is the enantiomer of Menin-MLL inhibitor-23 (HY-148367). Menin-MLL inhibitor-23 (Example 99A) is a menin-MLL interaction inhibitor.
    (1s,4s)-Menin-MLL inhibitor-23
  • HY-147375
    Bromodomain inhibitor-10
    		Inhibitor
    Bromodomain inhibitor-10 (compound 128) is a potent bromodomain inhibitor with Kds of 15.0, 2500 nM for BRD4-1 and BRD4-2, respectively. Bromodomain inhibitor-10 inhibits the production of IL12p40.
    Bromodomain inhibitor-10
  • HY-163160
    BET-IN-23
    		Inhibitor
    Bet-in-23 (Compound 23) is a BD2-selective BET inhibitor with an IC50 of 2.9 nM. BET-IN-23 has anticancer activity and can significantly inhibit the proliferation of acute myeloid leukemia (AML) cell lines by inducing G0/G1 arrest and apoptosis in vitro.
    BET-IN-23
Cat. No. Product Name / Synonyms Application Reactivity