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-143339
    CBP/p300-IN-15
    		Inhibitor
    CBP/p300-IN-15 (compound 13a) is a potent p300/CBP inhibitor, with IC50 values of 2.50 and 28.0 nM, respectively. CBP/p300-IN-15 shows good activity against OVCAR-3 and A2780 cell line, with EC50 values of 0.865 and 2.71 μM, respectively. CBP/p300-IN-15 can be used for ovarian cancer research.
    CBP/p300-IN-15
  • HY-153668A
    Bromodomain inhibitor-12 (edisylate)
    		Inhibitor
    Bromodomain inhibitor-12 edisylate (example 303) is a bromodomain inhibitor that can be used in the research of autoimmune and inflammatory diseases.
    Bromodomain inhibitor-12 (edisylate)
  • HY-176724
    ZnPc-O3-JQ1
    		Degrader
    ZnPc-O3-JQ1 is a light-triggered BRD4 degrader. Under illumination, ZnPc-O3-JQ1 generates reactive oxygen species (ROS) that degrades BRD4. The degradation of BRD4 results in downregulation of HIF-1α, thereby counteracting the photodynamic therapy (PDT) resistance induced by tumor hypoxia. ZnPc-O3-JQ1 exhibits both Type I and Type II PDT mechanisms. The structure of ZnPc-O3-JQ1 consists of three parts: BRD4 ligand (HY-78695); Linker (HY-W040165); Photosensitizer (HY-176725).
    ZnPc-O3-JQ1
  • HY-178043
    BTR2038
    		Degrader
    BTR2038 is a BRD9 degrader. BTR2038 consistis of a BRD9 bromodomain ligand (Bl-7273 analoag), a linker and BTR2000 (HY-172563). BTR2038 induces targeted degradation of V5-tagged human BRD9. BTR2038 can be used for the study of biological processes and diseases associated with abnormal BRD9 protein function.
    BTR2038
  • HY-139804
    CTK7A
    CTK7A is a curcumin derivative with anticancer activity by inhibiting the HAT activity of p300 and reducing the autoacetylation of p300, thereby affecting its interaction with HIF-1α. The inhibition of CTK7A leads to decreased HIF-1α accumulation and activity, which can be used for cancer research.
    CTK7A
  • HY-169272
    PROTAC SMARCA2 degrader-21
    		Degrader
    PROTAC SMARCA2 degrader-21 (Compound I-5) is a PROTAC degrader for SMARCA, that degrades SMARCA2 with a DC50 of 10-50 nM in A549 cell, and degrades SMARCA2 and SMARCA4 in MV411 with DC50 of <1 nM and >100 nM, respectively.
    PROTAC SMARCA2 degrader-21
  • HY-153948
    CBP-IN-1
    CBP-IN-1 (compound 12) is a potent CBP inhibitor, with an IC50 of 1.5 nM. CBP-IN-1 also inhibits CBP BRET and BRD4(1), with IC50 values of 690 and 3100 nM, respectively.
    CBP-IN-1
  • HY-181003
    GSK785
    		Inhibitor
    GSK785 is a BRD2/4-selective, BRD3-sparing bivalent BET inhibitor. GSK785 inhibits production of the MCP1 cytokine in human whole blood. GSK785 can be used for the research of cancer.
    GSK785
  • HY-141703
    DC-BPi-11
    		Inhibitor
    DC-BPi-11 is an inhibitor of bromodomain PHD finger transcription factor (BPTF), with an IC50 value of 698 nM. DC-BPi-11 shows remarkable inhibition against leukemia cell proliferation.
    DC-BPi-11
  • HY-134921
    MI-nc dihydrochloride
    		Inhibitor 99.9%
    MI-nc dihydrochloride is a weak inhibitor of the Menin-MLL fusion protein interaction with an IC50 of 193 μM. MI-nc dihydrochloride can be used as a negative control compound of MI-2.
    MI-nc dihydrochloride
  • HY-179589
    JQ-1 (carboxylic acid)-amine-PEG8-cyanogen
    		Degrader
    JQ-1 (carboxylic acid)-amine-PEG8-cyanogen is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for BRD4 (HY-78695) and a PROTAC linker, which recruits E3 ligases. JQ-1 (carboxylic acid)-amine-PEG8-cyanogen can be used for the synthesis of PROTAC BET Degrader-14 (HY-179588 ).
    JQ-1 (carboxylic acid)-amine-PEG8-cyanogen
  • HY-161887
    SMARCA2-IN-8
    		Inhibitor
    SMARCA2-IN-8 (Compound 13) is an orally active inhibitor for SWI/SNF chromatin remodeling complexe SMARCA2 (also known as Brahma homologue, BRM) and SMARCA4 (also known as Brahma-related gene 1, BRG1) with IC50 of 5 and 6 nM. SMARCA2-IN-8 inhibits the proliferation of SMARCA2 mutated cancer cell SKMEL5 with AAC50 of 5 nM. SMARCA2-IN-8 downregulates the SMARCA2-dependent KRT80 gene expression with AAC50 of 10 nM. SMARCA2-IN-8 exhibits antitumor efficacy and good pharmacokinetic characteristics in mice.
    SMARCA2-IN-8
  • HY-173257
    Cath-L-dBET1
    		Degrader
    Cath-L-dBET1 is a PROTAC degrader targeting BRD4. Cath-L-dBET1 has an IC50 value of 2.8 μM in MDA-MB-231 cells. Cath-L-dBET1 can be activated by cathepsin L (Cath-L) and recruit the E3 ubiquitin ligase and degrade BRD4 through ubiquitin-proteasome system. Hyp-dBET1 can be used for anti-tumor study.
    Cath-L-dBET1
  • HY-173327
    BRD4 degrader-6
    		Degrader
    BRD4 degrader-6 is a dimeric BDR4 PROTAC degrader (DC50: < 0.1 μM). BRD4 degrader-6 promotes the ubiquitination and degradation of BDR4 and has anticancer activity.
    BRD4 degrader-6
  • HY-181735
    BET-IN-30
    		Inhibitor
    BET-IN-30 (Compound 11d) is a BTE family protein inhibitor, which can act as a BRD2/BRD3/BRD4 target protein ligand and be used for the synthesis of PROTACs, such as PROTAC BET Degrader-15 (HY-181729). BET-IN-30 exhibits potent anti-proliferative activity against acute myeloid leukemia (AML) cells such as MV4-11. BET-IN-30 can be used for the study of AML.
    BET-IN-30
  • HY-159457
    PROTAC SMARCA2/4-degrader-6
    		Degrader
    PROTAC SMARCA2/4-degrader-6 (compound I-438) is a SMARCA2/4 degrader. PROTAC SMARCA2/4-degrader-6 has the potential for the research of cancer. (Pink: SMARCA2/4 ligand, (HY-159545); Black: linker (HY-W006635); Blue: VHL ligand (HY-112078)).
    PROTAC SMARCA2/4-degrader-6
  • HY-160733
    Menin-MLL-IN-32
    		Inhibitor
    Menin-MLL-IN-32 (compound 51) is a Menin-MLL interaction inhibitor with an IC50 of 0.042 nM in HTRF assay. Menin-MLL-IN-32 inhibits MEIS1 mRNA expression with an IC50 of 11 nM. Menin-MLL-IN-32 shows anti-proliferative effects, with IC50 values of 8 nM, 24 nM and 1900 nM for MOLM14 cells, OCI-AML3 cells and KO-52 cells, respectively. Menin-MLL-IN-32 can be used for the study of leukemia.
    Menin-MLL-IN-32
  • HY-162240
    SJH1-51B
    		Degrader
    SJH1-51B is a SKP1-recruiting BRD4 PROTAC degrader. SJH1-51B binds to SKP1 in the SKP1-FBXO7-CUL1-RBX1 complex, but shows no or weak binding to monomeric SKP1. SJH1-51B induces proteasome- and SKP1-dependent degradation of BRD4, and this degradation process relies on the neddylation modification of Cullin-RING E3 ligase. SJH1-51B induces proteasome-mediated degradation of the short isoform of BRD4 in non-cancer cells, while it induces proteasome-mediated degradation of both the long and short isoforms of BRD4 in breast cancer cells. SJH1-51B can be used for breast cancer research.
    SJH1-51B
  • HY-168235
    (S,R,S)-AHPC-Me-amide-C9-acid
    		Degrader
    (S,R,S)-AHPC-Me-amide-C9-acid is a E3 ligase ligand-linker conjugate, used for the synthesis of PROTAC SMARCA2 degrader-31 (HY-168234).
    (S,R,S)-AHPC-Me-amide-C9-acid
  • HY-130612
    PROTAC BRD2/BRD4 degrader-1
    		Inhibitor
    PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. PROTAC BRD2/BRD4 degrader-1 effectively inhibits solid tumors with low cytotoxic effect.
    PROTAC BRD2/BRD4 degrader-1
Cat. No. Product Name / Synonyms Application Reactivity
Epigenetic Reader Domain Isoform Comparison

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