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-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-180804
    CZL-077
    		Inhibitor
    CZL-077 is a potent, selective, and orally active p300/CBP bromodomain (BRD) inhibitor (p300 IC50 = 0.034 μM, CBP IC50 = 0.052 μM) exhibiting high selectivity over the BRDs of BET proteins (BRD2/3/4). CZL-077 inhibits cell growth with IC50 values of 0.024 μM and 5.6 μM in OPM-2 and 22RV1 cells, respectively. CZL-077 shows antitumor efficacy in OPM-2 and 22RV1 xenograft mouse models. CZL-077 can be used for multiple myeloma and prostate cancer research.
    CZL-077
  • 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-183575
    JQ1-JX5
    		Degrader
    JQ1-JX5 is a DCAF16-based BRD4 PROTAC degrader. JQ1-JX5 covalently modifies Cys58 of DCAF16, promotes ternary complex formation with BRD4, enables BRD4 ubiquitination and proteasomal degradation. JQ1-JX5 induces time-dependent degradation of BRD4 long and short isoforms in AGS cells with DC50 of 43.97 and 16.77 nM. JQ1-JX5 can be used for the research of cancer, such as acute myeloid leukemia.
    JQ1-JX5
  • HY-181505
    BRD4-IN-12
    		Inhibitor
    BRD4-IN-12 is a potent and orally active BRD4 inhibitor with an IC50 of 7.9 nM. BRD4-IN-12 downregulates the expression of c-MYC, BCL-2, CDK4 and upregulates p21. BRD4-IN-12 inhibits tumor cell proliferation and promotes apoptosis. BRD4-IN-12 exhibits excellent antitumor effects in the HCT-116 colorectal cancer xenograft model. BRD4-IN-12 can be used for the study of colorectal cancer (CRC).
    BRD4-IN-12
  • 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-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-179588
    PROTAC BET Degrader-14
    		Degrader
    PROTAC BET Degrader-14 is a highly efficient PROTAC targeting BET (bromodomain and extra-terminal domain). PROTAC BET Degrader-14 can degrade all BET (BRD2, BRD3, BRD4) family proteins. PROTAC BET Degrader-14 potently degrades BET proteins in U2OS osteosarcoma cell lines (BRD4 DC50 = 130 nM) and KYSE180 esophageal squamous cell carcinoma cell lines (DC50 = 40 nM). PROTAC BET Degrader-14’s dependence on the ubiquitin-proteasome system. PROTAC BET Degrader-14 decreases levels of BET-regulated gene products c-Myc, RUNX2, and KRT14. PROTAC BET Degrader-14 can be used for the study of osteosarcoma.
    PROTAC BET Degrader-14
  • 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-183922
    SRX3212
    		Inhibitor
    SRX3212 is a potent PI3Kα/BRD4 inhibitor with human IC50 values of 22 nM, 3.7 nM, and 32 nM for PI3Kα, BRD4BD1, and BRD4BD2, respectively. SRX3212 inhibits PI3K kinase activity and blocks acetyllysine binding function of BRD4BD1 and BRD4BD2. SRX3212 can be used for the research of mantle cell lymphoma, colon carcinoma, neuroblastoma, prostate cancer[1].
    SRX3212
Cat. No. Product Name / Synonyms Application Reactivity
Epigenetic Reader Domain Isoform Comparison

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