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-174451
    KMT9-IN-2
    		Inhibitor
    KMT9-IN-2 (Compound 7b) is an active form of a KMT9 inhibitor (Kd of 10 nM). KMT9-IN-2 can be used in the research of colon cancer.
    KMT9-IN-2
  • HY-147572
    BET-IN-10
    		Inhibitor
    BET-IN-10 is a BET inhibitor with anticancer effects. BET-IN-10 inhibits the cell growth of MV4-11 cells with an IC50 of 26.5 nM (WO2022012456A1; example 6).
    BET-IN-10
  • HY-149519
    BRD4 Inhibitor-28
    		Inhibitor
    BRD4 Inhibitor-28 (Compound 18) is an orally active BRD4 Inhibitor. BRD4 Inhibitor-28 inhibits BRD40-BD1, BRD40-BD2 with IC50s of 15, 55 nM. BRD4 Inhibitor-28 also inhibits BRD2-BD1, BRD3-BD1, BRDT-BD1 with IC50s of 19, 25, 68 nM. BRD4 Inhibitor-28 has anti-melanoma activity.
    BRD4 Inhibitor-28
  • HY-163282
    NB512
    		Inhibitor
    NB512 (compound 39a) is a dual inhibitor for BET and HDAC, which exhibits a efficient binding affinity with BRD4 bromodomains and HDAC1/2, with EC50s of 100-400 nM. NB512 exhibits an anti-proliferative activity towards cancer cells PaTu8988T and NMC.
    NB512
  • HY-162245
    PROTAC SMARCA2 degrader-3
    		Inhibitor
    PROTAC SMARCA2 degrader-3 is a PROTAC degrader of the SWI/SNF ATPase subunits, SMARCA2. PROTAC SMARCA2 degrader-3 has anticancer effects (WO2023244764A1; Compound 153).
    PROTAC SMARCA2 degrader-3
  • HY-149098
    SJ1461
    		Inhibitor
    SJ1461 is a potent and orally active BET inhibitor. SJ1461 inhibits BRD2 (BD1), and BRD2 (BD2), BRD4 (BD1), and BRD4 (BD2) with IC50 values of 1.6 nM, 0.1 nM, 6.5 nM, and 0.2 nM, respectively.
    SJ1461
  • HY-134598
    653-47
    		Inhibitor
    653-47, a potentiator, significantly potentiates the cAMP-response element binding protein (CREB) inhibitory activity of 666-15. 653-47 is also a very weak CREB inhibitor with IC50 of 26.3 μM.
    653-47
  • HY-114902
    Y02224
    		Inhibitor
    Y02224 is a potent BRD4 inhibitor and exhibits reasonable antiproliferative effect on leukemia cells.Y02224 has the potential for? CRPC research.
    Y02224
  • HY-139294
    PROTAC BRD4 Degrader-15
    		Inhibitor
    PROTAC BRD4 Degrader-15 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 7.2 nM and 8.1 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-15 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells.
    PROTAC BRD4 Degrader-15
  • HY-142705
    BRD4 D1-IN-2
    		Inhibitor
    BRD4 D1-IN-2 (compound 26) is a potent and selective BRD4 D1 inhibitor (IC50<0.092 µM). BRD4 D1-IN-2 has 15 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC.
    BRD4 D1-IN-2
  • HY-163460
    MS8535
    		Inhibitor
    MS8535 is a SPIN1 selective inhibitor, with an IC50 of 0.2 μM.
    MS8535
  • HY-168242
    PROTAC BRM/BRG1 degrader-1
    		Inhibitor
    PROTAC BRM/BRG1 degrader-1 (Example 253) is a PROTAC BRM/BRG1 degrader, with DC50 of 10-100 nM for BRM, > 1 μM for BRG1. PROTAC BRM/BRG1 degrader-1 can be used for cancer research. Blue: E3 ligase ligand (HY-168243), black: linker (HY-168244). Red: BRM/BRG1 inhibitor (HY-W539427).
    PROTAC BRM/BRG1 degrader-1
  • HY-129937
    (S)-GNE-987
    		Inhibitor
    (S)-GNE-987 (compound 4), the GNE-987 (a chimeric BET degrader) hydroxy-proline epimer, abrogates binding to von Hippel-Lindau and does not degrade BRD4 protein. (S)-GNE-987 binds to the BRD4 BD1(IC50=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC).
    (S)-GNE-987
  • HY-169170
    PARP1/BRD4-IN-3
    		Inhibitor
    PARP1/BRD4-IN-3 (compound HF4) is a potent BRD4 and PARP1 inhibitor with IC50 values of 1210, 2019 nM for BRD4, PARP1, respectively. PARP1/BRD4-IN-3 shows antiproliferative activities. PARP1/BRD4-IN-3 induces apoptosis and cell cycle arrest at G0/G1 phase. PARP1/BRD4-IN-3 causes DNA damage and reduces the protein expression of Rad51. PARP1/BRD4-IN-3 shows antitumor efficacy.
    PARP1/BRD4-IN-3
  • HY-160662
    BRD4-IN-5
    		Inhibitor
    BRD4-IN-5 (example 51) is a BRD4 inhibitor. The Ki values of the two BRD4 domains BDI_K57-E168 and BDII_E352-M457 are 9.7 nM and 16.1 nM, respectively. BRD4-IN-5 can be used in cancer research.
    BRD4-IN-5
  • HY-177141
    CDD-1154
    		Inhibitor
    CDD-1154 is an aminopyrimidine analog. CDD-1154 is a BRDT-BD2 inhibitor (IC50: 139 nM). CDD-1154 is used in male contraceptive research.
    CDD-1154
  • 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-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-163152
    PROTAC BRM degrader-1
    		Inhibitor
    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)
Cat. No. Product Name / Synonyms Application Reactivity
Epigenetic Reader Domain Isoform Comparison

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