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-157460
    BRD4 Inhibitor-29
    BRD4 Inhibitor-29 (SQ-17) is a BRD4 inhibitor, with an IC50 of <100 nM. BRD4 Inhibitor-29 shows antiproliferative effect against prostate cancer cells.
    BRD4 Inhibitor-29
  • HY-156401
    BRD9 Degrader-1
    		Inhibitor
    BRD9 c-1 (Compound 13-7) is a PROTAC BRD9 degrader. BRD9 Degrader-1 has a micromolar binding affinity for BRD9 and a nanomolar affinity for the BRD9-VCB ternary complex. BRD9 Degrader-1 induces BRD9 proteasome degradation in HEK293T cells, which can be reversed by MLN4924 (HY-70062).
    BRD9 Degrader-1
  • HY-162651
    PROTAC BRD9 Degrader-8
    		Degrader
    PROTAC BRD9 Degrader-8 is a selective, orally active BRD9 PROTAC degrader with a DC50 of 16 pM.\nPROTAC BRD9 Degrader-8 induces cell cycle arrest at the G1 phase and promotes apoptosis. PROTAC BRD9 Degrader-8 can be used for research on acute myeloid leukemia and diffuse large B-cell lymphoma.
    PROTAC BRD9 Degrader-8
  • HY-183339
    IL-6/RIPK3-IN-1
    		Inhibitor
    IL-6/RIPK3-IN-1 is an inhibitor of IL-6, RIPK3 and BRD4, with IC50 values of 0.22, 1.32 and 5.91 μM, respectively. IL-6/RIPK3-IN-1 can be used in studies related to inflammation and tissue damage.
    IL-6/RIPK3-IN-1
  • HY-169151
    PROTAC BRD4-DCAF1 degrader-1
    PROTAC BRD4-DCAF1 degrader-1 (I-907) is a BRD4-DCAF1 PROTAC degrader, DC50 is 10~100 nM. .
    PROTAC BRD4-DCAF1 degrader-1
  • HY-163152
    PROTAC BRM degrader-1
    		Degrader
    PROTAC BRM degrader-1 (compound 17) is a PROTAC-based BRM and BRG1 degrader, with DC50 values of 93 pM and 4.9 nM, respectively.
    PROTAC BRM degrader-1
  • HY-16900G
    Rolipram (GMP)
    		Inhibitor
    Rolipram GMP is Rolipram (HY-16900) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Rolipram is a PDE4 inhibitor, with blood-brain barrier permeability, that reverses β-amyloid-induced learning and memory impairment in rats. Rolipram elevates intracellular cAMP and clevels and regulates the cAMP/CREB signaling pathway, thereby alleviating neuroinflammation and apoptotic responses. Rolipram promotes neuronal differentiation of human bone marrow mesenchymal stem cells and inhibits Methamphetamine- and morphine-induced hyperlocomotion in mice. Rolipram also reduces the viability of glioblastoma stem-like cells and enhances Bevacizumab (HY-P9906)-induced cell death. Rolipram inhibits the expression of proinflammatory cytokines and enhances central noradrenergic transmission. Rolipram is mainly used in studies related to various central nervous system diseases including Alzheimer's disease, major depressive disorder, glioblastoma multiforme, and multiple sclerosis.
    Rolipram (GMP)
  • HY-143270
    PROTAC BRD9-binding moiety 5
    PROTAC BRD9-binding moiety 5 is a selective BRD9 binder with an IC50 value of 4.20 μM, can be used for the synthesis of PROTACs. PROTAC BRD9-binding moiety 5 has antiproliferative activity against cancer cells.
    PROTAC BRD9-binding moiety 5
  • HY-147869
    DC-CPin7
    		Inhibitor
    DC-CPin7 is a potent inhibitor of CREB-binding protein (CBP) bromodomain with an IC50 of 2.5 μM.
    DC-CPin7
  • HY-159455
    PROTAC SMARCA2/4-degrader-4
    		Degrader
    PROTAC SMARCA2/4-degrader-4 (Compound I-434) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-4 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: Ligand for target protein (HY-159472); Black: Linker (HY-159478); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
    PROTAC SMARCA2/4-degrader-4
  • HY-176477
    BRD4/FKBP12 degrader-2
    		Degrader
    BRD4/FKBP12 degrader-2 (a1dj) is a BRD4/FKBP12 degrader and shows anticancer activity (BRD4 ligand: HY-78695, FKBP12 ligand: HY-176502, linker: HY-140212).
    BRD4/FKBP12 degrader-2
  • HY-175179
    LO-3-61
    		Degrader
    LO-3-61, a JQ-1 (HY-13030) analog bearing a truncated fumaramide handle, is a PROTAC (proteolysis-targeting chimeras)-like BRD4 degrader. LO-3-61 degrades both the long and short isoforms of BRD4 CUL4DcAr16-dependently in cells. LO-3-61 shows selectivity for BRD3 and BRD4 degradation in MDA-MB-231 cells.
    LO-3-61
  • HY-159602
    BET BD2-IN-3
    		Inhibitor
    BET BD2-IN-3 (compound I-58) is an inhibitor of BET, targeting the BD2 domain of BET. BET BD2-IN-3 can be radiolabeled with [11C] for positron emission tomography (PET) imaging. BET [11C]BD2-IN-3 showed suitable biodistribution in peripheral organs and tissues in PET applications in mice.
    BET BD2-IN-3
  • HY-163271
    XL-126
    		Inhibitor
    XL-126 (Compound 33) is a potent BD1-selective BET inhibitor, with a Kd of 8.9 nM. XL-126 leads to both the preservation of platelets and potent anti-inflammatory efficacy by BD1 selectivity.
    XL-126
  • HY-180152
    BRD4 ligand 14
    		Inhibitor
    BRD4 ligand 14 (Compound Y47) is a BRD4 inhibitor. BRD4 ligand 14 exhibits mild anticancer properties against acute myeloid leukemia by inhibiting BRD4. BRD4 ligand 14 can also be used as a ligand for target protein for PROTAC in the development and design of PROTAC BRD4 degraders, such as PROTAC BRD4 Degrader-42 (HY-180150).
    BRD4 ligand 14
  • HY-181164
    PROTAC BRD4 Degrader-43
    		Degrader
    PROTAC BRD4 Degrader-43 is a BRD4 PROTAC degrader. PROTAC BRD4 Degrader-43 recruits the DCAF1-DDB1-Cul4A E3 ligase complex via a Vpr-derived peptide moiety to induce BRD4 ubiquitination and degradation through the ubiquitin-proteasome system. PROTAC BRD4 Degrader-43 exhibits potent HIV latency-reversing activity. PROTAC BRD4 Degrader-43 can be used for the research of HIV-1 latent infection. (Pink: BRD4 ligand (HY-13030); Blue: Cul4A-DDB1-DCAF1 ligand (HY-P11640); Black: conjugate of PEG linker + cell-penetrating peptide (HY-P2483))
    PROTAC BRD4 Degrader-43
  • HY-168464
    Y16526
    		Inhibitor
    Y16526 is a potent inhibitor of CBP/p300 bromodomain , with the IC50 of 0.03 μM. Y16524 has the potential for the research of acute myeloid leukemia (AML).
    Y16526
  • HY-169488
    SMARCA2 ligand-12-3-methylazetidine
    		Inhibitor
    SMARCA2 ligand-12-3-methylazetidin is a target protein ligand-linker conjugate that incorporates a ligand for SMARCA2 (HY-169487), and a PROTAC linker (HY-W052601), which recruit E3 ligases. SMARCA2 ligand-12-3-methylazetidin can be used to synthesize PROTAC SMARCA2 degrader-25 (HY-169276).
    SMARCA2 ligand-12-3-methylazetidine
  • HY-171774
    PBRM1/SMARCA2,4-ligand-1
    PBRM1/SMARCA2,4-ligand-1 (Compound 4) is a Ligand for Target Protein for PROTAC that binds to PBRM1, SMARCA2, and SMARCA4. PBRM1/SMARCA2,4-ligand-1 is a potent SMARCA4 bromodomain inhibitor. PBRM1/SMARCA2,4-ligand-1 can be used to synthesize PROTAC AU-24118 (HY-163410).
    PBRM1/SMARCA2,4-ligand-1
  • HY-N16067
    Penipanoid C
    		Inhibitor
    Penipanoid C (Compound 9) is a BRD4 inhibitor. Penipanoid C can be isolated from marine sediment-derived fungus Penicillium paneum SD-44. Penipanoid C has anti-inflammatory activity and cytotoxic activity against the SMMC-7721 cells. Penipanoid C can be used for inflammatory diseases research.
    Penipanoid C
Cat. No. Product Name / Synonyms Application Reactivity
Epigenetic Reader Domain Isoform Comparison

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