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-161960
    EP300/CBP ligand 2
    EP300/CBP ligand 2 (compound S19) is a ligand targeting the bromodomain of CREB binding protein (CBP) and E1A-associated protein (EP300). EP300/CBP ligand 2 can be used as a target protein ligand in the PROTAC structure, and can be coupled to the E3 ubiquitin ligase ligand through the PTOTAC Linker to synthesize PROTAC molecules with degradation effects. For example, EP300/CBP ligand 2 can be coupled with the conjugate (E3 ubiquitin enzyme ligand + Linker) Thalidomide-NH-C10-Boc (HY-161961) to produce the PROTAC molecule dCE-2 (HY-161958).
    EP300/CBP ligand 2
  • HY-157426
    GSPT1 degrader-3
    		Degrader
    GSPT1 degrader-3 (Pro-2) is a CRBN-based PROTAC degrader for BRD, with a DC50 of 21.1 nM (4h).
    GSPT1 degrader-3
  • HY-42429
    CPI-203-PEG1-C3-O-COOH
    CPI-203-PEG1-C3-O-COOH is a conjugate of the BRD4 ligand (HY-78695) and the linker (HY-42427). CPI-203-PEG1-C3-O-COOH can be used for synthesizing PROTAC BRD4 degrader ARV-771 (HY-100972).
    CPI-203-PEG1-C3-O-COOH
  • HY-175186
    LO-3-62
    		Degrader
    LO-3-62 is a PROTAC-like SMARCA2/4 degrader with a truncated fumaramide handle. LO-3-62 degrades SMARCA2/4 in cells.
    LO-3-62
  • HY-175225
    PROTAC BRD4 Degrader-37
    		Degrader
    PROTAC BRD4 Degrader-37 (Compound TrimTAC-2) is a PROTAC BRD4 degrader. PROTAC BRD4 Degrader-37 has a DC50 of 36.4 nM and a Dmax of 73% in PANC-1 cells. PROTAC BRD4 Degrader-37 exhibits cytotoxicity against PANC-1 cells (GI50: 0.282 μM). PROTAC BRD4 Degrader-37 can be used in the research of tumors. (Pink: PROTAC BRD4 ligand-4 (HY-175242); Blue + Black: E3 ligase ligand + linker (HY-175241)).
    PROTAC BRD4 Degrader-37
  • HY-168234
    PROTAC SMARCA2 degrader-31
    		Inhibitor
    PROTAC SMARCA2-degrader-36 (compound 38) is a SMARCA2 degrader and can reach the the degradation rate of 99 % at the 100 nM in H929 cells. PROTAC SMARCA2-degrader-36 shows anti-proliferative activity and can be used for study of cancer(Structure Note: PINK SMARCA2 ligand HY-44012; Blue, VHL ligand (HY-112078); Black, linker HY-W014125).
    PROTAC SMARCA2 degrader-31
  • HY-111575
    DCB29
    		Inhibitor
    DCB29 is a selective inhibitor of the BPTF bromodomain, with an IC50 value of 13.2 μM. DCB29 can be used for the study of the treatment of BPTF-related diseases (such as bladder cancer, colorectal cancer, melanoma, leukemia, and other cancers).
    DCB29
  • HY-161883
    JP-2-249
    		Degrader
    JP-2-249 is a molecular glue that acts as a potent degrader of SMARCA2. JP-2-249 shows decreasing protein level of SMARCA2 in MV-4-11 cells at 1-10 μM.
    JP-2-249
  • HY-176449
    PROTAC BRD4 Degrader-32
    		Inhibitor
    PROTAC BRD4 Degrader-32 (Compound 22) is a BRD4 PROTAC degrader (DC50: 0.20 nM). PROTAC BRD4 Degrader-32 connects the BRD4-binding domain and CRBN-binding domain through a unique carbon-carbon linked linker to form a ternary complex, inducing ubiquitination of BRD4 for proteasomal degradation. PROTAC BRD4 Degrader-32 is promising for research of BRD4-related cancers (such as hematological malignancies). (Pink: GSK1324726A (HY-13960); Black: linker (HY-176450); Blue: Lenalidomide-5-Br (HY-W072954)).
    PROTAC BRD4 Degrader-32
  • HY-159451
    PROTAC SMARCA2 degrader-7
    		Inhibitor
    PROTAC SMARCA2 degrader-7 (Compound I-428) is a PROTAC degrader for SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily A (SMARCA) SMARCA2. PROTAC SMARCA2 degrader-7 degrades SMARCA2 and SMARCA4 in MV411 with DC50 of <100 and 100-500 nM. (Pink: Ligand for target protein (HY-159542); Black: Linker (HY-159538); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
    PROTAC SMARCA2 degrader-7
  • HY-172095
    BRD4 Inhibitor-39
    		Inhibitor
    BRD4 Inhibitor-39 (compound 12m) is an orally available BRD4 inhibitor with an IC50 value of 0.02 μM. BRD4 Inhibitor-39 induces apoptosis. BRD4 Inhibitor-39 has anti-tumor activity.
    BRD4 Inhibitor-39
  • HY-136794
    SB-284851-BT
    		Inhibitor
    SB-284851-BT is an inhibitor of BRD4/p38α/BRDT. SB-284851-BT inhibits BRD4-BD1 (IC50=1.7 µM), p38α (Kd=0.47 nM), BRDT (1) (IC50=18 µM) and BRD4 (1)(IC50=3.7 µM). SB-284851-BT reduces IL-8 production by inhibiting p38α, as well as inhibiting BRD4 to down-regulates c-Myc and NF-κB gene pathways in cancer. SB-284851-BT can combined with the bromine domain and extra terminal (BET).
    SB-284851-BT
  • HY-W265951
    3-Methylcarbostyril
    		Inhibitor
    3-Methylcarbostyril (compound 5) is a BRD4 BD1 inhibitor with a pIC50 of 4.4.
    3-Methylcarbostyril
  • HY-161886
    SMARCA2-IN-7
    SMARCA2-IN-7 (compound 12), a dual inhibitor of BRM and BRG1 (IC50 < 0.005 for both), has an anti-tumor proliferation effect that inhibits BRG1-deleted SKMEL5 tumor proliferation with a cell proliferation activity AAC50 of 13 nM in SKMEL5. The cell proliferation activity AAC50 of KRT880 in H1299 cells was 42 nM.
    SMARCA2-IN-7
  • HY-168463
    Y16524
    		Inhibitor
    Y16524 is a potent inhibitor of CBP/p300 bromodomain , with the IC50 of 0.01 μM. Y16524 has the potential for the research of acute myeloid leukemia (AML).
    Y16524
  • HY-173450
    ZL0516
    		Inhibitor
    ZL0516 is a potent, selective, and orally active BRD4 BD1 inhibitor. ZL0516 suppresses inflammatory bowel disease (IBD) by inhibiting BRD4/NF-κB signaling.
    ZL0516
  • HY-177145
    CDD-1132
    		Inhibitor
    CDD-1132 (Compound 8) is a potent inhibitor of BRDT-BD2. CDD-1132 has an IC50 of 13 nM against BRDT-BD2. CDD-1132 can be studied in research on nonhormonal contraceptive agent.
    CDD-1132
  • HY-169269
    PROTAC SMARCA2 degrader-18
    		Degrader
    PROTAC SMARCA2 degrader-18 (Example144) is a PROTAC SMARCA2 degrader. PROTAC SMARCA2 degrader-18 has the potential for the research of non-small cell lung cancer (NSCLC).
    PROTAC SMARCA2 degrader-18
  • HY-160527
    BRD4 degrader-4
    		Degrader
    BRD4 degrader-4 (Compound 1-f) is a BRD4 degrader. BRD4 degrader-4 can be used for the research of cancer and other bromodomain related diseases.
    BRD4 degrader-4
  • HY-176822
    SGC-BRDVIII-NC
    		Inhibitor
    SGC-BRDVIII-NC (Compound 35) is a negative control compound of SMARCA2/4 and PB1 bromodomain (BRD) inhibitor. SGC-BRDVIII-NC completely abolishes protein-ligand binding capacity with the methylation of the phenolic hydroxyl moiety. SGC-BRDVIII-NC can be used for adipogenesis research.
    SGC-BRDVIII-NC
Cat. No. Product Name / Synonyms Application Reactivity