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-151972
    BRD4 Inhibitor-25
    		Inhibitor
    BRD4 Inhibitor-25 is a BRD4 inhibitor with IC50s of 0.82 μM, 1.94 μM for BD1 and BD2 domains of BRD4. BRD4 Inhibitor-25 induces apoptotic and autophagy cell death in ovarian cancer cells. BRD4 Inhibitor-25 can be used in the research of cancers, cardiovascular, neuromuscular and inflammatory disorders.
    BRD4 Inhibitor-25
  • HY-122573
    Bromodomain inhibitor-13
    		Inhibitor
    Bromodomain inhibitor-13 (Compound 1) is an analog of PFI-3 (HY-12409). Bromodomain inhibitor-13 is a bromodomain-containing protein (BCP) inhibitor. Bromodomain inhibitor-13 targets SMARCA2, SMARCA4, PB1(5), and second bromodomain of PB1 (PB1(2)) with KD values of 37, 53, 30, and 190 nM, respectively.
    Bromodomain inhibitor-13
  • HY-153519
    WWL0245
    		Inhibitor
    WWL0245 is a potent and seletive BRD4 PROTAC. WWL0245 selectively degrades BRD4 with sub-nanomolar DC50 (<1 nM) than BRD2/3 and PLK1 ( DC50>1 μM). WWL0245 shows excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-positive prostate cancer cell lines. WWL0245 is a promising drug candidate for AR-positive prostate cancer research and a valuable tool compound to study the biological function of BRD4.
    WWL0245
  • HY-145925C
    (S,R)-CFT8634
    		Inhibitor
    (S,R)-CFT8634 (compound 176) is a selective and orally active PROTAC-class BRD9 protein degrader. (S,R)-CFT8634 has the potential to study BRD9-mediated diseases, including but not limited to abnormal cell proliferation. (S,R)-CFT8634 consists of a target protein ligand (red part) BRD9 ligand-5 (HY-169988), an E3 ligase ligand (blue part) CRBN ligand-11 (HY-169989), and a PROTAC linker (black part) 1-(3,3-Difluoro-4-piperidinyl)piperazine (HY-169991). E3 ligase ligand and linker can form E3 Ligase Ligand-linker Conjugate 142 (HY-169990).
    (S,R)-CFT8634
  • HY-178041
    BRD4-BD1/2-IN-3
    		Inhibitor
    BRD4-BD1/2-IN-3 (Compound B6) is a selective BRD4 BD2 inhibitor with an IC50 of 0.41  nM for BRD4 BD2 over BRD4 BD1. BRD4-BD1/2-IN-3 significantly inhibits the LPS (HY-D1056)-induced expression of IL-6. BRD4-BD1/2-IN-3 shows anti-inflammatory activities by modulating the TNF and NF-κB signaling pathway. BRD4-BD1/2-IN-3 can be used for inflammatory diseases research.
    BRD4-BD1/2-IN-3
  • HY-152470
    Eleven-Nineteen-Leukemia Protein IN-2
    		Inhibitor
    Eleven-Nineteen-Leukemia Protein IN-2 (compound 23) is an Eleven-Nineteen-Leukemia Protein (ENL) inhibitor with an IC50 value of 10.7 nM. Eleven-Nineteen-Leukemia Protein IN-2 can be used for the research of leukemia.
    Eleven-Nineteen-Leukemia Protein IN-2
  • HY-161673
    CDC14A/B-IN-1
    		Inhibitor
    CDC14A/B-IN-1 (Compound 15) is an orally available inhibitor of CDC14A/B phosphatases with Ki values ??of 57.4 nM (CDC14A) and 90.0 nM (CDC14B), respectively.
    CDC14A/B-IN-1
  • HY-172416
    Balomenib
    		Inhibitor
    Balomenib is the inhibitor for menin-MLL interaction, that inhibits the interaction between men1-MLL4-43 with an IC50 < 0.075 μM. Balomenib inhibits the growth of MV4-11 (CC50 < 0.1 μM), MOLM-13 (CC50 0.1~0.5 μM) and HEK293 (CC50 < 2 μM). Balomenib exhibits antineoplastic activity.
    Balomenib
  • HY-153668
    Bromodomain inhibitor-12
    		Inhibitor
    Bromodomain inhibitor-12 (example 303) is a bromodomain inhibitor that can be used in the research of autoimmune and inflammatory diseases.
    Bromodomain inhibitor-12
  • HY-174920
    PROTAC BRD4 Degrader-34
    		Inhibitor
    PROTAC BRD4 Degrader-34 (Compound MZ2) is a selective BRD4 PROTAC degrader (pDC50 = 8.4). PROTAC BRD4 Degrader-34 can induce BD2 degradation mediated by VHL. PROTAC BRD4 Degrader-34 can be used for research on cancer. (Pink: BRD4-BD2 Ligand (HY-78695); Blue: VHL Ligand (HY-125845); Black: Linker (HY-130524)).
    PROTAC BRD4 Degrader-34
  • HY-169358
    L134
    		Inhibitor
    L134 is a potent PROTAC BRD4 degrader with a DC50 value of 7.36 nM. L134 mediates the degradation of BRD4 via the ubiquitin-proteasome system in a DCAF11-dependent manner (Blue: JQ-1 (carboxylic acid) (HY-78695), Black: linker (HY-W004640); Pink: E3 ligase ligand, L321 (HY-169359)).
    L134
  • HY-160018
    BAY-155
    		Inhibitor
    BAY-155 is a potent and selective menin-MLL tool inhibitor, with an IC50 of 8 nM. BAY-155 leads to a strong expression down-regulation of the MEIS1 gene and up-regulation of CD11b and MNDA genes. BAY-155 shows anti-proliferative effects in AML/ALL (acute myeloid/lymphoblastic leukemia) models.
    BAY-155
  • HY-121738
    TC AC 28
    		Inhibitor
    TC AC 28 is a high-affinity BET bromodomain ligand with Kd values of 40, 800 nM for Brd2(2), Brd2(1), respectively.
    TC AC 28
  • HY-114162B
    VTP50469 mesylate
    		Inhibitor
    VTP50469 mesylate is a potent, and selective Menin-MLL1 inhibitor that effectively targets MLL-rearranged and NPM1c+ leukemia. VTP50469 mesylate selectively kills cell lines with MLL rearrangements and NPM1c+ mutations. VTP50469 mesylate displaces Menin from protein complexes and inhibits MLL's chromatin occupancy at specific genes, leading to significant changes in gene expression, differentiation, and apoptosis. VTP50469 demonstrates dramatic reductions in leukemia burden in patient-derived xenograft models of MLL-r acute myeloid leukemia and MLL-r acute lymphoblastic leukemia, with some mice remaining disease-free for over a year post-treatment.
    VTP50469 mesylate
  • HY-157814
    Menin-MLL inhibitor-25
    		Inhibitor
    Menin-MLL inhibitor-25 (compound A6) is a potent Menin-MLL interaction inhibitor with an IC50 value of 0.38 µM. Menin-MLL inhibitor-25 shows anti-proliferative activity. Menin-MLL inhibitor-25 induces apoptosis and cell cycle arrest at G0/G1 phase. Menin-MLL inhibitor-25 reverses the differentiation arrest.
    Menin-MLL inhibitor-25
  • HY-142953
    UNC6349 (Ket2)
    		Inhibitor
    UNC6349 (Ket2), a diethyllysine (Ket2)-containing ligand, binds to wild-type CBX5, with a KD of 3.2 μM.
    UNC6349 (Ket2)
  • HY-146739
    BRD4 Inhibitor-19
    		Inhibitor
    BRD4 Inhibitor-19 is a BET inhibitor with an IC50 of 55 nM for BRD4-BD1. BRD4 Inhibitor-19 can be used for multiple myeloma research.
    BRD4 Inhibitor-19
  • HY-168628
    BET-IN-27
    		Inhibitor
    BET-IN-27 (compound 6C) is an oral BET inhibitor with the IC50 values of 3.3 nM (BRD4-BD2)、3.4 nM (BRD4-BD1)、4.1 nM (BRD2-BD1)、20.4 nM (BRD3-BD1) and 42.0 nM (BRDT-BD1), respectively. BET-IN-27 shows anti-proliferative activity.
    BET-IN-27
  • HY-170390
    AB3067
    		Degrader
    AB3067 is a PROTAC degrader for BET protein, that recruits two different E3 ligase Cereblon and VHL with good affinity (IC50=559 nM for VHL in live HEK293; IC50=190 nM for CRBN in live HEK293), and degrades BRD2, BRD3, BRD4 and CRBN with DC50 of 2.1~2.3, 1.6, 15 and 75 nM, respectively. AB3067 inhibits the proliferation of RKO cell with an EC50 of 111 nM. (Pink: ligand for target protein (HY-131633A); Black: linker (HY-170391); Blue: ligand for E3 ligase VHL (HY-112078) and CRBN(HY-W998346))
    AB3067
  • HY-169861
    PROTAC SMARCA2/4 degrader-37
    		Degrader
    PROTAC SMARCA2/4 degrader-37 (Example 4) is a PROTAC-based SMARCA2/4 degrader, with an IC50 of ≤0.1 μM (Pink: SMARCA2/4 lignad (HY-172446); Black: CRBN ligand (HY-41547); Linker (HY-N2407)).
    PROTAC SMARCA2/4 degrader-37
Cat. No. Product Name / Synonyms Application Reactivity