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-135558
    PROTAC BRD4 Degrader-3
    		Inhibitor
    PROTAC BRD4 Degrader-3 (compound 1004.1) is an efficacious PROTAC connected by ligands for von Hippel-Lindau and BRD4.
    PROTAC BRD4 Degrader-3
  • HY-143317
    XY153
    		Inhibitor
    XY153 (compound 8l) is a BD2-selective BET inhibitor and selectively binds to BRD4 BD2. XY153 binds to BRD4 BD2, BRD3 BD2 and BRD2 BD2 with IC50s of 0.79, 5.31 and 5.09 nM, respectively. XY153 shows potent antiproliferative activity against multiple tumor cell lines. XY153 can be used for the research of acute myeloid leukemia (AML) and cancer.
    XY153
  • HY-170686
    BRD4 Inhibitor-38
    		Inhibitor
    BRD4 Inhibitor-38 (Compound 25) is an orally active inhibitor of BRD4 with IC50 values of 3.64 μM and 0.12 μM against BRD4 BD1 and BRD4 BD2, respectively. BRD4 Inhibitor-38 also exhibits anti-inflammatory activity, with an IC50 value of 1.98 μM for inhibiting nitric oxide (NO) production.
    BRD4 Inhibitor-38
  • HY-168246
    PROTAC SMARCA2 degrader-29
    		Degrader
    PROTAC SMARCA2 degrader-29 (Example 87) is a PROTAC SMARCA2 (BRM) degrader, with DC50 of 10-100 nM (BRM) and > 1 μM (BRG1, also known as SMARCA2) respectively.
    PROTAC SMARCA2 degrader-29
  • HY-163413
    BRD4-BD1-IN-3
    		Inhibitor
    BRD4-BD1-IN-3 (Compound 4g) is a BRD4-BD1 inhibitor. BRD4-BD1-IN-3 can be used for research of inflammatory disease.
    BRD4-BD1-IN-3
  • HY-168255
    PROTAC BRM/BRG1 degrader-4
    		Inhibitor
    PROTAC BRM/BRG1 degrader-4 (example 047) is a potent BRM and BRG1 PROTAC degrader, with DC50 values of 0.21 nM and 3.4 nM in SW1573 cells, respectively (Pink: ligand for target protein (HY-168252); Black: linker (HY-28911); Blue: E3 ligase ligand (HY-168253)).
    PROTAC BRM/BRG1 degrader-4
  • HY-174812
    BRD4 ligand 8
    		Inhibitor
    BRD4 ligand 8 (Compound J558) is a BRD4 inhibitor. BRD4 ligand 8 can be used for synthesis of PROTAC BRD4 Degrader-33 (HY-174811).
    BRD4 ligand 8
  • HY-N10802
    6-O-Isobutyrylbritannilactone
    		Inhibitor
    6-O-Isobutyrylbritannilactone is a natural melanogenesis inhibitor. 6-O-Isobutyrylbritannilactone, a sesquiterpene, can be isolated from the flowers of Inula britannica. 6-O-Isobutyrylbritannilactone inhibits IBMX (HY-12318)-induced melanin production in B16F10 cells. 6-O-Isobutyrylbritannilactone also regulates ERK, PI3K/AKT, and CREB, shows antimelanogenic activity in zebrafish embryos models.
    6-O-Isobutyrylbritannilactone
  • HY-161498
    XYD198
    		Inhibitor
    XYD198 (Compound 14h) is an orally active degrader for CBP/p300. XYD198 inhibits CBP/p300 bromodomain with IC50 of 213.5 nM. XYD198 exhibits antitumor activity against acute myeloid leukemia. (Structure: Pink, CBP/p300 ligand 4 (HY-161495); Blue, E3 ligase ligand (HY-14658); Black: linker (HY-161499))
    XYD198
  • HY-163543
    Progranulin modulator-2
    		Inhibitor
    Progranulin modulator-2 (compound 18A) is a bromodomain and extra-terminal domain (BET) inhibitor. Progranulin modulator-2 enhances PGRN expression by targeting members of the BET protein family. Progranulin modulator-2 can be used to study the role of BET protein in neurodevelopment, neuroplasticity and neurodegeneration.
    Progranulin modulator-2
  • HY-15846A
    (Rac)-CPI-203
    		Inhibitor
    (Rac)-CPI-203 is a racemate of CPI-203 (HY-15846) (BET bromodomain inhibitor)
    (Rac)-CPI-203
  • HY-N1506R
    Ganodermanontriol (Standard)
    		Modulator
    Karbutilate (Standard) is the analytical standard of Karbutilate. This product is intended for research and analytical applications. Karbutilate (NIA-11092) is a nonselective soil-active herbicide which is used to kill one-leaf pinyon saplings.
    Ganodermanontriol (Standard)
  • HY-159456
    PROTAC SMARCA2/4-degrader-5
    		Degrader
    PROTAC SMARCA2/4-degrader-5 (Compound I-437) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-5 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 of 100-500 nM. (Pink: Ligand for target protein (HY-159545); Black: Linker (HY-159557); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
    PROTAC SMARCA2/4-degrader-5
  • HY-162815
    PROTAC SMARCA2/4-degrader-26
    PROTAC SMARCA2/4-degrader-26 (compound 6) is a PROTAC targeting SMARCA2/4. SMARCA2 and SMARCA4 are genes and cancer targets with complementary functions that catalyze nucleosome movement. PROTAC SMARCA2/4-degrader-25 is composed of PROTAC target protein ligand 2-(4-(3-Amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)acetic acid (HY-46618) (red part), E3 ligase ligand (2S,4R)-4-Hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (HY-W998248) (blue part), PROTAC linker (S)-2-Amino-3,3-dimethylbutanoic acid (HY-59140) (black part), and the conjugate composed of E3 ubiquitin ligase ligand + Linker is (S,R,S)-AHPC (HY-125845)[1].
    PROTAC SMARCA2/4-degrader-26
  • HY-161710
    XYD129
    		Degrader
    XYD129 is an effective CBP/p300 PROTAC degrader. XYD129 has antiproliferative activity on MV4-11 cell line (IC 50=0.044 μM). XYD129 can be used for the study of acute myeloid leukemia (AML). (Structure Note: Pink, CBP/p300 ligand 5 (HY-161711); Blue, E3 ligase ligand (HY-41547); Black, Linker (HY-40178)).
    XYD129
  • HY-161889
    DCSM06-05
    		Inhibitor
    DCSM06-05 is a potent SMARCA2-BRD inhibitor with an IC50 value of 9 µM, a Kd value of 22.4 µM.
    DCSM06-05
  • HY-114207
    VinSpinIn
    		Inhibitor
    VinSpinIn is a Spindlin1 inhibitor (KD: 9.9 nM for SPIN149-262). VinSpinIn is a chemical probe for tudor domain of Spindlin1. VinSpinIn can be used to study chromatin function.
    VinSpinIn
  • HY-104072
    BRD4-IN-3
    		Inhibitor
    BRD4-IN-3 (compound 141) is a potent BRD4 inhibitor with an IC50 of <0.5 µM. BRD4-IN-3 shows cytoxicity for MYC-Raji with an IC50 value of >1 µM.
    BRD4-IN-3
  • HY-153593
    BET bromodomain inhibitor 3
    		Inhibitor
    BET bromodomain inhibitor 3 is BET bromodomain inhibitor. BET bromodomain inhibitor 3 has inhibitory effect against BrdT with Ki value of > 40 µM. BET bromodomain inhibitor 3 can be used for the research of contraception, cancer, and heart disease.
    BET bromodomain inhibitor 3
  • HY-W494890
    SMARCA2-IN-10
    		Inhibitor
    SMARCA2-IN-10 (Compound 4) is a highly selective SMARCA2 ATPase domain inhibitor (IC50=17.676 μM). SMARCA2-IN-10 induces cell death in SMARCA4-deficient tumors. SMARCA2-IN-10 is promising for research of SMARCA4-mutant non-small cell lung cancer, small cell ovarian carcinoma, and melanoma.
    SMARCA2-IN-10
Cat. No. Product Name / Synonyms Application Reactivity