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-169487
    SMARCA2 ligand-12
    		Inhibitor
    SMARCA2 ligand-12 is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). SMARCA2 ligand-12 can be used for synthesis PROTAC SMARCA2 degrader-25 (HY-169276).
    SMARCA2 ligand-12
  • HY-W192171
    BRD4 Inhibitor-34
    		Inhibitor
    BRD4 Inhibitor-34 (Compound 12a) is a BRD4 inhibitor with an IC50 of 24 μM.
    BRD4 Inhibitor-34
  • HY-122645
    SMARCA2-IN-4
    		Inhibitor
    SMARCA2-IN-4 (Compound 26) is an inhibitor for SWI/SNF chromatin remodeling complexe SMARCA by targeting the bromodomains. SMARCA2-IN-4 exhibits high affinity for PB1(5), SMARCA2B and SMARCA4 with Kd of 124, 262 and 417 nM.
    SMARCA2-IN-4
  • HY-180957
    NEP108
    		Degrader
    NEP108 is a GID4 E3 ligase-based BRD4 PROTAC degrader, with its DC50 value approximately 3.8 μM. NEP108 has a strong affinity for GID4, with a KD value of 0.22 μM, and the KD value of its trimeric complex is 2.85 μM. NEP108 can be used for cancer research.
    NEP108
  • HY-183247
    BRDT-IN-1
    		Inhibitor
    BRDT-IN-1 is a BRDT-BD1 and BRDT-T inhibitor with BRDT-BD1 IC50 19 nM, Ki 8.8 nM, Ka 1.6 nM, and BRDT-T IC50 56 nM, Ka 5.0 nM. BRDT-IN-1 displays in vitro metabolic stability and limited cellular permeability in MDCK-MDR1 cells. BRDT-IN-1 can be used for the research of multiple myeloma.
    BRDT-IN-1
  • HY-161495
    CBP/p300 ligand 4
    		Inhibitor
    CBP/p300 ligand 4 (Compound 4) is an orally active inhibitor for CBP/p300 bromodomain, with IC50 of 91.4 nM. CBP/p300 ligand 4 serves as a ligand for target protein XYD190 (HY-161495). XYD190 is a PROTAC degrader for CBP/p300.
    CBP/p300 ligand 4
  • HY-155393
    PROTAC BRD4 Degrader-22
    		Degrader
    PROTAC BRD4 Degrader-22 (Compd 44h) is a PROTAC-based BRD4 degrader, with a pDC50 (MOLT4, 24 h) of 9.2.
    PROTAC BRD4 Degrader-22
  • HY-115727
    BET-IN-1
    		Inhibitor
    BET-IN-1 is a potent BET inhibitor that has excellent brain penetration and reasonable metabolic stability.
    BET-IN-1
  • HY-173256
    Hyp-dBET1
    		Degrader
    Hyp-dBET1 is a PROTAC degrader targeting BRD4. Hyp-dBET1 has an IC50 value of 3.4 μM in MDA-MB-231 cells. Hyp-dBET1 can be activated by hypoxia and recruit the E3 ubiquitin ligase and degrade BRD4 through ubiquitin-proteasome system. Hyp-dBET1 can be used for anti-tumor study.
    Hyp-dBET1
  • HY-177729
    PROTAC BRD9 Degrader-9
    		Degrader
    PROTAC BRD9 Degrader-9 (Compound 16) is an efficient and selective targeting BRD9 PROTAC degrader. PROTAC BRD9 Degrader-9 does not cause significant cytotoxicity. PROTAC BRD9 Degrader-9 can be used for cancer research
    PROTAC BRD9 Degrader-9
  • HY-124859
    CeMMEC2
    CeMMEC2 is a direct BRD4 inhibitor with an IC50 of 0.9 μM.
    CeMMEC2
  • HY-160670
    BRD4-IN-6
    		Inhibitor
    BRD4-IN-6 (compound 116) is a BRD4 inhibitor (extracted from patent CN107721975A).
    BRD4-IN-6
  • HY-171438
    ATF4 agonist-1
    ATF4 agonist 1 (Compound 298) is a ATF4 agonist and integrated stress pathway modulator.
    ATF4 agonist-1
  • HY-162748
    PROTAC SMARCA2/4-degrader-30
    		Degrader
    PROTAC SMARCA2/4-degrader-30 (Compound I-291) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-30 degrades SMARCA2 in A549 and in MV411 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: ligand for target protein (HY-163926); Black: linker (HY-159684); Blue: ligand for E3 ligase (HY-W382038)).
    PROTAC SMARCA2/4-degrader-30
  • HY-180831
    BRD4 D1-IN-3
    		Inhibitor
    BRD4 D1-IN-3 (compound 39) is a potent, selective, and cell-active BRD4-D1 inhibitor (IC50 = 39 nM, Ki = 2.4 nM) with >1700-fold selectivity over BRD2-D1. BRD4 D1-IN-3 reduces the expression of pro-inflammatory chemokines CXCL1 and CCL2 in an LPS (HY-D1056)-mediated cellular model of liver inflammation. BRD4 D1-IN-3 can be used for liver inflammation research.
    BRD4 D1-IN-3
  • HY-177730
    PROTAC BRD4 Degrader-40
    		Degrader
    PROTAC BRD4 Degrader-40 is a Bromodomain protein 4 (BRD4) PROTAC degrader. PROTAC BRD4 Degrader-40 can induce BRD4 degradation in cancer cells. PROTAC BRD4 Degrader-40 can be used for the research of cancer, such as leukemia. (Structure Note: Pink: BRD4 ligand (HY-78695); Blue: CRBN ligand (HY-163927))
    PROTAC BRD4 Degrader-40
  • HY-179734
    PROTAC BRD4 Degrader-41
    		Degrader
    PROTAC BRD4 Degrader-41 (Compound A5) is a BRD4 PROTAC degrader with a DC50 of 0.97 nM. PROTAC BRD4 Degrader-41 exhibits potent anti-proliferative activity against various types of cancer cells such as AML, lymphoma, breast cancer, ovarian cancer, and non-small cell lung cancer. PROTAC BRD4 Degrader-41 can induce G0/G1 phase arrest and apoptosis in MV4-11 cells. PROTAC BRD4 Degrader-41 downregulates the transcriptional level of c-Myc.
    PROTAC BRD4 Degrader-41
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Epigenetic Reader Domain Isoform Comparison

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