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-117365
    MI-1481
    		Inhibitor
    MI-1481 is a highly potent inhibitor of the Menin-MLL1 interaction with IC50 of 3.6 nM. MI-1481 markedly reduces cell growth of murine bone marrow cells transformed and inhibits leukemia progression.
    MI-1481
  • HY-175354
    PROTAC BET Degrader-13
    		Degrader
    PROTAC BET Degrader-13 (Compound 34) is a TRIM21-based PROTAC (TRIMTAC) degrader targeting BET. PROTAC BET Degrader-13 significantly degrades PML-eGFP-BRD4 fusion protein with a near-complete loss of EGFP+ nuclear puncta with an EC50 of 1.4 μM. Pink: BET ligand (HY-13030); Blue: E3 ligase ligand (HY-W1125585); Black: linker
    PROTAC BET Degrader-13
  • HY-149421
    BRD7-IN-3
    		Inhibitor
    BRD7-IN-3 (compound 1-78) is a dual inhibitor of bromodomain-containing proteins BRD7/BRD9 with IC50s of 1.6 μM and 2.7 μM respectively.
    BRD7-IN-3
  • HY-175242
    PROTAC BRD4 ligand-4
    		Ligand
    PROTAC BRD4 ligand-4 is a BRD4 ligand, which can be used to synthesize PROTAC BRD4 Degrader-37 (HY-175225).
    PROTAC BRD4 ligand-4
  • HY-182801
    PROTAC BRD4 Degrader-46
    		Degrader
    PROTAC BRD4 Degrader-46 is a heterobifunctional BRD4 PROTAC degrader. PROTAC BRD4 Degrader-46 binds to both BRD4 and CRBN, thereby triggering ubiquitination and proteasomal degradation of BRD4. PROTAC BRD4 Degrader-46 downregulates the levels of downstream BRD2, BRD3 and MYC. PROTAC BRD4 Degrader-46 can be used in the research of cancers such as multiple myeloma.
    PROTAC BRD4 Degrader-46
  • HY-151533
    PBRM1-BD2-IN-6
    		Inhibitor
    PBRM1-BD2-IN-6 is a potent PBRM1 bromodomain inhibitor with an IC50 value of 0.22 μM. PBRM1-BD2-IN-6 shows antiproliferation activity. PBRM1-BD2-IN-6 has the potential for the research of PBRM1-dependent cancer.
    PBRM1-BD2-IN-6
  • HY-151528
    PBRM1-BD2-IN-1
    		Inhibitor
    PBRM1-BD2-IN-1 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-1 has binding affinity and inhibitory activity for PBRM1-BD2 with Kd and IC50 values of 0.7 μM and 0.2 μM, respectively. PBRM1-BD2-IN-1 can be used for the research of cancer.
    PBRM1-BD2-IN-1
  • HY-163809
    BRD9 Degrader-2
    		Degrader
    BRD9 Degrader-2 (Compound B11) is a BRD9 degrader (DC50 ≤1.25 nM; Dmax≥75%). BRD9 Degrader-2 can be used for research of cancers.
    BRD9 Degrader-2
  • HY-181495
    RAJQ14
    		Degrader
    RAJQ14 is a BRD4 PROTAC-like CAP-TAC (Proteasome Cap Targeting Chimeras) degrader. RAJQ14 binds to 19S proteasome cap subunits RPN1, RPN10, RPN13, and USP14 to recruit target proteins to the proteasome for ubiquitination-independent, proteasome-dependent degradation. RAJQ14 can be used for the research of cancer (Pink: BRD4 Ligand (HY-181496); Blue: Proteasome Ligand (HY-128978); Black: Linker).
    RAJQ14
  • HY-184151
    KBD-1
    		Degrader
    KBD-1 is a muscle-specific BRD4 PROTAC degrader with human KDs of 27.04 nM and 37.36 µM against BRD4 and KLHL4L, respectively. KBD-1 recruits the muscle-specific E3 ligase KLHL41, mediating Cullin-RING ligase (CRL)-dependent ubiquitination and proteasome degradation of BRD4. KBD-1 can be used for the research of myosarcoma.
    KBD-1
  • HY-115541
    BRD4-IN-41
    		Inhibitor
    BRD4-IN-41 is a BRD4 inhibitor with an IC50 of 34 nM. BRD4-IN-41 also inhibits JAK2, FLT3, RET, ROS1, NTRK3, PDGFRb, and FGFR1 kinases with IC50 values ranging from 0.9 nM to 43 nM. BRD4-IN-41 inhibits acetyl-lysine binding site of BRD4, downregulates c-MYC, reduces phosphorylated STAT3 levels, induces G1 cell cycle arrest and apoptosis, thereby inhibiting cancer cells growth. BRD4-IN-41 can be used for the research of cancer, such as multiple myeloma and acute myeloid leukemia.
    BRD4-IN-41
  • HY-178481
    BRM/BRG1 ATP-IN-5
    		Inhibitor
    BRM/BRG1 ATP-IN-5 (Compound 6) is a BRG1/BRM inhibitor. BRM/BRG1 ATP-IN-5 acts on the BAF complex, which is involved in chromatin regulation and gene expression via ATP-dependent chromatin remodeling. BRM/BRG1 ATP-IN-5 demonstrates anti-tumor potential, particularly in cancers associated with BAF complex disorders.
    BRM/BRG1 ATP-IN-5
  • HY-168236
    PROTAC SMARCA2 degrader-28
    		Degrader
    PROTAC SMARCA2 degrader-28 (Compound 158) is a PROTAC degrader for SMARCA2, that degrades SMARCA2 with a DC50 of 3 nM in HiBiT A549 cells. (Pink: Ligand for target protein (HY-168237); Black: Linker (HY-168238); Blue: Ligand for E3 ligase (HY-W087383))
    PROTAC SMARCA2 degrader-28
  • HY-170841
    HDAC3/BRD4-IN-1
    		Inhibitor
    HDAC3/BRD4-IN-1 (compound 26n) is an inhibitor of HDAC3/BRD4 with an IC50 of 8 nM for HDAC3 (IC50s are 220 nM and 120 nM for HDAC1 and HDAC2, respectively). HDAC3/BRD4-IN-1 has anti-tumor and anti-proliferative effects by upregulating Ac-H3 and downregulating c-Myc. The half-life of HDAC3/BRD4-IN-1 in human liver microsomes is 29.36 min.
    HDAC3/BRD4-IN-1
  • HY-156130
    Menin-MLL inhibitor 29
    		Inhibitor
    Menin-MLL inhibitor 29 (Compound C1) is a Menin-MLL PPI inhibitor. Menin-MLL inhibitor 29 binds to Menin with a KD value of 138 nM, and inhibits the binding of Menin to MBM1 (Menin-binding motif 1) with an IC50 value of 46 nM. Menin-MLL inhibitor 29 inhibits HepG2 and Hep3B hepatoma cell proliferation (IC50s: 0.31 μM and 0.71 μM). Menin-MLL inhibitor 29 inhibits tumor growth.
    Menin-MLL inhibitor 29
  • HY-183077
    BRD4 degrader-7
    		Degrader
    BRD4 degrader-7 (Compound ZZ1) is a CTLH-dependent BRD4 degrader and c-Glue with a DC50 of 489 nM. BRD4 degrader-7 converts to a sulfinic acid derivative inside cells, interacts with the basic pocket of YPEL5, mediates the bridging of BRD4 BD1 to the YPEL5 subunit of the CTLH E3 ubiquitin ligase, and thereby promotes the formation of a ternary complex. BRD4 degrader-7 can be used in research on Ewing's sarcoma and leukemia.
    BRD4 degrader-7
  • HY-161888
    DCSM06
    		Inhibitor
    DCSM06 is an inhibitor for the bromodomain of SWI/SNF chromatin remodeling complexe SMARCA2 with an IC50 of 9.7 μM
    DCSM06
  • HY-183061
    MrTAC-8
    		Degrader
    MrTAC-8, methylarginine-targeting chimera (MrTAC), is a BRD4 degrader with DC50 values of 46 nM in HeLa cells. MrTAC-8 recruits PRMT1, PRMT3, PRMT4, PRMT5, and PRMT7 to target proteins, inducing arginine methylation that triggers lysosomal degradation. MrTAC-8 degrades proteins across diverse subcellular localizations and independent of native proteolytic routes. MrTAC-8 can be used for the research of cervical cancer, glioblastoma.
    MrTAC-8
  • HY-180150
    PROTAC BRD4 Degrader-42
    		Degrader
    PROTAC BRD4 Degrader-42 (Compound P6) is a PROTAC-based BRD4 degrader with a DC50 of 1.11 μM. PROTAC BRD4 Degrader-42 promotes the ubiquitination and degradation of BRD4. PROTAC BRD4 Degrader-42 downregulates c-Myc expression and induces Apoptosis by upregulating BAD and BAX protein expression. PROTAC BRD4 Degrader-42 also exhibits anticancer activity against myeloid monocytic leukemia.
    PROTAC BRD4 Degrader-42
  • HY-177139
    CDD-1349
    		Inhibitor
    CDD-1349 (Compound 15) is a BRDT-BD2/BRD4-BD2 selective inhibitor. CDD-1349is an analog with sixfold selectivity for BRDT-BD2 versus BRD4-BD2. CDD-1349 has an IC50 of 22 nM against BRDT. CDD-1349 can be studied in research on nonhormonal contraceptive agent.
    CDD-1349
Cat. No. Product Name / Synonyms Application Reactivity
Epigenetic Reader Domain Isoform Comparison

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