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-162875
    PROTAC BRD4 Degrader-27
    PROTAC BRD4 Degrader-27 (compound 6b) is a PROTAC that selectively targets BRD4 (rather than BRD2/BRD3) and can also inhibit the expression of KLF5 transcription factor and exert anti-cancer activity. PROTAC BRD4 Degrader-27 is composed of E3 ubiquitinase ligand Thalidomide-4-OH (HY-103596) (red part), PROTAC Linker γ-Aminobutyric acid (HY-N0067) (black part) and PROTAC target protein ligand PROTAC BRD4 ligand-3 (HY-162876) (blue part), of which the active control of the target protein ligand is Mivebresib (HY-100015), and the conjugate of E3 ubiquitin ligase ligand + Linker is Pomalidomide 4'-alkylC3-acid (HY-131875)[1].
    PROTAC BRD4 Degrader-27
  • HY-155809
    BET-IN-17
    BET-IN-17 (compound 16) is a pan-inhibitor of BET with pIC50s of 7.8 and 7.6 for BET BD1 and BET BD2, respectively.
    BET-IN-17
  • HY-146291
    BET-IN-7
    		Inhibitor
    BET-IN-7 (Compound 1) is a potent inhibitor of BET with a Ki and Kd of 12.27 and 89.3 μM, respectively. BET-IN-7 has the potential for the research of sepsis.
    BET-IN-7
  • HY-168453
    dBAZ2B
    		Degrader
    dBAZ2B is a BAZ2B PROTAC degrader, with a DC50 of 19 nM. (Pink: BAZ2A/B ligand (HY-168449); Black: linker (HY-168450); Blue: VHL Ligand (HY-125905))
    dBAZ2B
  • HY-150613
    PARP1/BRD4-IN-2
    		Inhibitor
    PARP1/BRD4-IN-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC).
    PARP1/BRD4-IN-2
  • HY-157430
    BET-IN-21
    		Inhibitor
    BET-IN-21 (compound 16) is a blood-brain barrier-permeable extra terminal domain (BET) inhibitor with the Ki of 230 nM. BET-IN-21 inhibits microglia activation and has ameliorative effects on experimental autoimmune encephalomyelitis mice.
    BET-IN-21
  • HY-181756
    LGF308
    		Degrader
    LGF308 is a PROTAC degrader of BRD4 that exhibits selective cytotoxicity toward cancer cells over normal cells. LGF308 mediates the formation of a ternary complex between BRD4 and DCAF11 to achieve BRD4 degradation. LGF308 induces tumor cell apoptosis by upregulating apoptosis-related proteins. LGF308 inhibits tumor cell proliferation and migration in breast cancer and triple-negative breast cancer cell lines. LGF308 can be used for the research of breast cancer.
    LGF308
  • HY-N10319R
    Artepillin C (Standard)
    		Inhibitor
    Artepillin C (Standard) is the analytical standard of Artepillin C (HY-N10319). This product is intended for research and analytical applications. Artepillin C is an orally active CREB/CRTC2 inhibitor and TRPA1 covalent agonist (EC50=1.8 μM). Artepillin C inhibits CREB/CRTC2-mediated gene transcription and downregulates BMAL1 expression to regulate glucose and lipid metabolism. Artepillin C can also activate TRPA1 channels to induce spicy taste signals. Artepillin C can inhibit tumor cell proliferation, induce apoptosis, improve insulin resistance and inhibit liver lipid synthesis. Artepillin C can be used in the study of metabolic syndrome, tumor prevention and treatment, and inflammation.
    Artepillin C (Standard)
  • 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
    PROTAC BET Degrader-19
    		Degrader
    PROTAC BET Degrader-19 (Pro-2) is a CRBN-based PROTAC degrader for BRD, with a DC50 of 21.1 nM (4h).
    PROTAC BET Degrader-19
  • 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-155891
    BET-IN-18
    		Inhibitor
    BET-IN-18 (Compound 3) is a pan-BET bromodomain small-molecule inhibitor, with Ki values of 0.69 μM and 0.37 μM, and Kd values of 1.6 μM and 8.4 μM against BrdT (1) and Brd4 (1) bromodomains, respectively. BET-IN-18 potently and competitively inhibits the binding of the known BET inhibitor (+)-JQ1 (HY-13030) to Brd4 (1) and BrdT (1), with IC50 values of 1.0 μM and 2.3 μM, respectively. BET-IN-18 also competitively inhibits the binding of acetylated histone substrates to Brd4 (1) (IC50 = 0.90 μM). BET-IN-18 can be used in the research of multiple myeloma.
    BET-IN-18
  • 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-181279
    PCAF/GCN5 ligand 1
    PCAF/GCN5 ligand 1 is a PCAF/GCN5 ligand with high binding affinity. PCAF/GCN5 ligand 1 shows no functional effect on PCAF/GCN5 activity. PCAF/GCN5 ligand 1 undergoes optimization into a potent and selective PCAF/GCN5 ligand GSK4027 (HY-101027).
    PCAF/GCN5 ligand 1
  • 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-D3393
    JQ1-FITC TFA
    JQ1-FITC TFA is a BRD4-binding fluorescent tracer. JQ1-FITC TFA binds to BRD4 BD1, BD2, recombinant bromodomains, and endogenous BRD4 in cell lysates. JQ1-FITC TFA can be used for the research of breast cancer and cancer (Ex/Em = 495/525 nm).
    JQ1-FITC TFA
  • 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 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
Cat. No. Product Name / Synonyms Application Reactivity
Epigenetic Reader Domain Isoform Comparison

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