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-114971
    CREBBP-IN-1
    CREBBP-IN-1 (Compound 10) exhibits good affinity with CREBBP bromodomain with Kd of 0.77 μM.
    CREBBP-IN-1
  • HY-153574
    BI01826025
    		Degrader
    BI01826025 (pArg-JQ1) is a bromodomain1 of BRDT (BRDTBD1) PROTAC degrader. BI01826025 can be used for testing the regulatory effect of ClpC2 on the ClpC1P1P2 protease.
    BI01826025
  • HY-155078
    BRD4 Inhibitor-27
    		Inhibitor
    BRD4 Inhibitor-27 (compound 6) is a BRD4 inhibitor with IC50 of 9.6 and 11.3 μM for BRD4 BD1 and BRD4 BD2, respectively. BRD4 Inhibitor-27 has the potential to study cancer.
    BRD4 Inhibitor-27
  • HY-168148S
    CZL-046
    		Inhibitor
    CZL-046 (compund 29) is an oral p300 bromodomain inhibitor.
    CZL-046
  • HY-159449
    PROTAC SMARCA2 degrader-5
    		Degrader
    PROTAC SMARCA2 degrader-5 (Compound I-425) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2. PROTAC SMARCA2 degrader-5 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 with DC50 of 100-500 nM. (Pink: Ligand for target protein (HY-159531); Black: Linker (HY-159538); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
    PROTAC SMARCA2 degrader-5
  • HY-176521
    Antiproliferative agent-71
    		Inhibitor
    Antiproliferative agent-71 (Compound II-5) is an orally active dual inhibitor against the androgen receptor (AR) and bromodomain-containing protein 4 (BRD4). Antiproliferative agent-71 effectively inhibits tumor cell growth and proliferation by simultaneously blocking the functions of AR and BRD4. Antiproliferative agent-71 is promising for research of prostate cancer.
    Antiproliferative agent-71
  • HY-172126
    JQ-1 (carboxylic acid)-NH-C2-NH-AMPRO-222
    JQ-1 (carboxylic acid)-NH-C2-NH-AMPRO-222 incorporates a ligand for BRD4, and a PROTACs linker that can be used in the synthesis of PROTAC BRD4 Degrader-29 (HY-172124).
    JQ-1 (carboxylic acid)-NH-C2-NH-AMPRO-222
  • HY-114205
    TP-238
    		Inhibitor
    TP-238 is a potent and selective dual CECR2/BPTF probe with IC50 values of 30 nM and 350 nM, respectively. TP-238 also inhibits BRD9 with a pIC50 of 5.9 and is less active against other 338 kinases.
    TP-238
  • HY-178484
    BRM/BRG1 ATP-IN-6
    		Inhibitor
    BRM/BRG1 ATP-IN-6 (Compound 105) is a BRG1/BRM inhibitor. BRM/BRG1 ATP-IN-6 acts on the BAF complex, which is involved in chromatin regulation and gene expression via ATP-dependent chromatin remodeling. BRM/BRG1 ATP-IN-6 demonstrates anti-tumor potential, particularly in cancers associated with BAF complex disorders.
    BRM/BRG1 ATP-IN-6
  • HY-169279
    PROTAC SMARCA2/4-degrader-34
    		Degrader
    PROTAC SMARCA2/4-degrader-34 (compound 38) is a potent is a potent SMARCA2 and SMARCA4 PROTAC degrader. PROTAC SMARCA2/4-degrader-34 shows PXR binding affinity with DC50 value of 85.1 nM. PROTAC SMARCA2/4-degrader-34 decreases the protein expression of 3xFLAG-PXR. (Pink: Ligand for target protein (HY-169280); Black: Linker (HY-43048); Blue: Ligand for E3 ligase (HY-125845).
    PROTAC SMARCA2/4-degrader-34
  • HY-172562
    BTR2004
    		Inhibitor
    BTR2004 is a selective BET family (BRD2/3/4) protein PROTAC degrader. BTR2004 forms a ternary complex with BRD proteins and KLHL20, inducing ubiquitination and proteasomal degradation through the UPS pathway. BTR2004 is promising for research of PC3 prostate cancer and MDA-MB-231 breast cancer cell lines. Pink: (+)-JQ1-OH (HY-161125); Blue: BTR2000 (HY-172563); Black: Linker (HY-W015236).
    BTR2004
  • HY-N2020R
    Anacardic Acid (Standard)
    		Inhibitor
    Anacardic Acid (Standard) is the analytical standard of Anacardic Acid. This product is intended for research and analytical applications. Anacardic Acid, extracted from cashew nut shell liquid, is a histone acetyltransferase inhibitor, inhibits HAT activity of p300 and PCAF, with IC50s of ～8.5 μM and ～5 μM, respectively.
    Anacardic Acid (Standard)
  • HY-161885
    SMARCA2-IN-6
    		Inhibitor
    SMARCA2-IN-6 is a SMARCA2 (also known as BRM) inhibitor, with IC50s less than 5 nM for SMARCA2 and SMARCA4. SMARCA2-IN-6 inhibits KRT80 gene expression in H1299 cells (IC50: 26 nM). SMARCA2-IN-6 inhibits proliferation in BRG1-mutant SKMEL5 cells (IC50: 13 nM).
    SMARCA2-IN-6
  • HY-116237
    CREBBP-IN-9
    		Inhibitor
    CREBBP-IN-9 (Compound 9) is an inhibitor for CREBBP with an Kd of 29 μM.
    CREBBP-IN-9
  • HY-145347
    GSK232
    		Inhibitor
    GSK232 is a highly selective, cellularly penetrant CECR2 inhibitor with excellent physicochemical properties.
    GSK232
  • HY-160671
    BRD4-IN-7
    		Inhibitor
    BRD4-IN-7 (compound 120) is a BRD4 inhibitor(extracted from patent CN107721975A).
    BRD4-IN-7
  • HY-111937
    MI-1
    		Inhibitor
    MI-1 inhibits Menin-MLL interaction with an IC50 of 1.9 μM.
    MI-1
  • HY-147374
    Bromodomain inhibitor-9
    		Inhibitor
    Bromodomain inhibitor-9 is a Bromodomains inhibitor that selectively inhibits BRD4-1 (Kd: 12 nM). Bromodomain inhibitor-9 can be used in the research of diseases or conditions associated with systemic or tissue inflammation, lipid metabolism, fibrosis or chronic autoimmune diseases.
    Bromodomain inhibitor-9
  • HY-116349
    Bromodomain IN-1
    		Inhibitor
    Bromodomain IN-1 is a Bromodomain inhibitor extracted from patent WO2016069578A1, compound 4 .
    Bromodomain IN-1
  • HY-176251
    CBP/p300-IN-22
    		Inhibitor
    CBP/p300-IN-22 is a selective CBP/EP300-BRD inhibitor with an IC50 of 4 nM. CBP/p300-IN-22 is highly selective over BRD4(1). CBP/p300-IN-22 reduces TNF-α-induced cytokine expression and subsequent immune cell recruitment by inhibiting NF-κB signaling, and has anticancer activity. CBP/p300-IN-22 can be used for the research of rheumatoid arthritis (RA) and other TNF-α-mediated inflammatory conditions.
    CBP/p300-IN-22
Cat. No. Product Name / Synonyms Application Reactivity