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-139861
    CBP/p300-IN-14
    		Inhibitor
    CBP/p300-IN-14 is a potent inhibitor of CBP/EP300 (lysine acetyltransferase) with an IC50 of 3.3 nM (extracted from patent WO2021213521A1, compound 27).
    CBP/p300-IN-14
  • HY-178510
    JQ1-S(GlcNAc)Cq
    		Degrader
    JQ1-S(GlcNAc)Cq is a sugar-coated BRD4 PROTAC degrader. JQ1-S(GlcNAc)Cq can inhibit the formation of the ternary complex between CRBN and BRD4(BD1/BD2). JQ1-S(GlcNAc)Cq can be used for the research of cancer. (Structure Note: Pink: BRD4 ligand (HY-78695); Blue: CRBN ligand (HY-178514); Black: linker (HY-W105727); BRD4 ligand-Linker: (HY-178519))
    JQ1-S(GlcNAc)Cq
  • HY-169994
    BC13
    		Inhibitor
    BC13 is a CDK6/BRD4 inhibitor with the IC50 values of 234 nM and 36 nM for CDK6 and BRD4, respectively. BC13 shows antiproliferative activity and induces cell apoptosis and DNA damage. BC13 increases in ROS levels.
    BC13
  • HY-142954
    UNC6212 (Kme2)
    		Inhibitor
    UNC6212 (Kme2), a dimethyllysine (Kme2)-containing ligand, has a KD for CBX5 of 5.7 μM.
    UNC6212 (Kme2)
  • HY-175224
    PROTAC BRD4 Degrader-36
    		Degrader
    PROTAC BRD4 Degrader-36 is a BRD4 PROTAC degrader. PROTAC BRD4 Degrader-36 has a DC50 of 0.649 nM and a Dmax of 71% in PANC-1 cells. PROTAC BRD4 Degrader-36 is cytotoxic to PANC-1 cells (GI50: 0.103 μM). PROTAC BRD4 Degrader-36 can be used in the study of cancer. (Pink: PROTAC BRD4 ligand-1 (HY-129939); Blue + Black: E3 ligase ligand + linker (HY-175241)).
    PROTAC BRD4 Degrader-36
  • HY-163811
    BRD9 Degrader-4
    		Inhibitor
    BRD9 Degrader-4 (BRD9c), a bifunctional molecular glue, is a potent BRD9 degrader with a DC50 of ≤25 nM. BRD9 Degrader-4 has anti-cancer effects.
    BRD9 Degrader-4
  • HY-181496
    (S)-JQ-35-Boc
    		Ligand
    (S)-JQ-35-Boc is a BRD4 ligand. (S)-JQ-35-Boc can be used to synthesize BRD4 degrader RAJQ14 (HY-181495). RAJQ14 can be used for cancer research.
    (S)-JQ-35-Boc
  • HY-183825
    Eleven-Nineteen-Leukemia Protein IN-4
    		Inhibitor
    Eleven-Nineteen-Leukemia Protein IN-4 is a ENL YEATS domain inhibitor with an IC50 of 62.0 nM and a Kd of 100.4 nM. Eleven-Nineteen-Leukemia Protein IN-4 downregulates MYC expression and inhibits cancer cell growth; it exerts a synergistic effect with the bromodomain inhibitor JQ-1 (HY-13030). Eleven-Nineteen-Leukemia Protein IN-4 can be used in the research of acute myeloid leukemia.
    Eleven-Nineteen-Leukemia Protein IN-4
  • HY-153632
    PROTAC BRD9 Degrader-6
    		Degrader 98.19%
    PROTAC BRD9 Degrader-6 is a potent degrader of BRD9 (IC50=0.13 nM), can be used for research of BAF complex-related disorders.
    PROTAC BRD9 Degrader-6
  • HY-145431
    (S)-GSK1379725A
    		Inhibitor
    (S)-GSK1379725A (compound AU1) is a selective bromodomain and PHD finger containing transcription factor (BPTF) bromodomain inhibitor with a Kd of 2.8 μM. (S)-GSK1379725A shows to be selective for BPTF over BRD4 bromodomain. (S)-GSK1379725A shows antimalarial activity.
    (S)-GSK1379725A
  • HY-161494
    XYD190
    		Inhibitor
    XYD190 (Compound 14g) is an orally active degrader for CBP/p300. XYD190 inhibits CBP/p300 bromodomain with IC50 of 483.7 nM. XYD190 exhibits antitumor activity against acute myeloid leukemia. (Structure: Pink, CBP/p300 ligand 4 (HY-161495); Blue, E3 ligase ligand (HY-14658); Black: linker (HY-161496)).
    XYD190
  • HY-176391
    Ad-JQ1
    		Inhibitor
    Ad-JQ1 (Compound 16) is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for BRD4 (HY-78695) and a PROTAC linker (HY-176390), which recruits E3 ligases. Ad-JQ1 can be used for synthesis of PROTAC β-NF-JQ1 (HY-130256).
    Ad-JQ1
  • HY-114164F
    Canine Thrombin
    Canine Thrombin is a Canine serine protease that plays a central role in blood coagulation. Canine Thrombin stimulates macrophages to polarize into a unique phenotype characterized by anti-inflammatory and pro-repair properties. Canine Thrombin activates PAR1, induces the production of MCP-1, MMP3 and VEGF in intervertebral discs, and causes degradation of the cartilage matrix and destruction of intervertebral disc structure. Canine Thrombin activity increases significantly in paraoxon-induced status epilepticus.
    Canine Thrombin
  • HY-183992
    CZL-149
    		Inhibitor
    CZL-149 is an orally active dual BET and p300/CBP bromodomains inhibitor with IC50s of 13 nM and 10.5 nM for BED4 BD1 and p300, respectively. CZL-149 reduces c-Myc and H3K27Ac levels. CZL-149 has good drug-like properties and metabolic characteristics, as well as good safety. CZL-149 can be used for the study of multiple myeloma.
    CZL-149
  • HY-181553
    PROTAC BRD4 Degrader-44
    		Degrader
    PROTAC BRD4 Degrader-44 is a BRD4 PROTAC degrader with a DC50 of 16 nM. PROTAC BRD4 Degrader-44 is applicable to studies on membrane-permeable PROTACs.
    PROTAC BRD4 Degrader-44
  • HY-175610
    PROTAC FLT3/JAK2/BRD4 Degrader-1
    		Degrader
    PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC50 values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC50 = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/JAK2/BRD4 ligand (HY-175611), Blue: CRBN Ligand (HY-W087383), Black: Linker, E3 ligase ligand-linker conjugate (HY-W897939)).
    PROTAC FLT3/JAK2/BRD4 Degrader-1
  • HY-160261S
    EP300/CBP-IN-2
    		Inhibitor
    EP300/CBP-IN-2 is a potent EP300/CBP inhibitor that has good activity in vivo. EP300/CBP-IN-2 can be used for the research of cancer.
    EP300/CBP-IN-2
  • HY-147571
    BET-IN-9
    		Inhibitor
    BET-IN-9 is a BET inhibitor extracted from patent WO2022012456A1, compound example 1.
    BET-IN-9
  • HY-143299
    BRD4-BD1-IN-1
    		Inhibitor
    BRD4-BD1-IN-1 (Compound 9a) is a BRD4-BD1 inhibitor with an IC50 of 38.20 μM.
    BRD4-BD1-IN-1
  • HY-138623
    GSK789
    		Inhibitor
    GSK789 is a selective inhibitor of BET BD1. GSK789 inhibits the growth of leukemia cell lines. GSK789 inhibits LPS-stimulated production of MCP-1, TNFα and IL-6 in human whole blood. GSK789 exhibits antiproliferative, anti-inflammatory and immunomodulatory activities. GSK789 can be used in research related to cancers such as leukemia, as well as inflammatory and immune diseases.
    GSK789
Cat. No. Product Name / Synonyms Application Reactivity