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-131203
    PROTAC BRD4 Degrader-6
    		Inhibitor
    PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule BRD4PROTAC degrader with IC50 value of 2.7 nM for BRD4 BD1. PROTAC BRD4 Degrader-6 potently degrades BRD4 protein and inhibits the expression of c-Myc. PROTAC BRD4 Degrader-6 inhibits the proliferation of pancreatic cancer cell line BxPC3 and induces apoptosis. PROTAC BRD4 Degrader-6 can be used for human pancreatic cancer research (Pink: Mivebresib (HY-100015); Black: linker, Azido-PEG1-CH2CO2H (HY-108369); Blue: Lenalidomide (HY-A0003)).
    PROTAC BRD4 Degrader-6
  • HY-173237
    CDK4/6/BRD4-IN-1
    		Inhibitor
    CDK4/6/BRD4-IN-1 (B15) is an inhibitor of CDK4, CDK6 and BRD4, with IC50 values of 220 nM, 146 nM, 106 nM and 85 nM for BRD4-BD2, BRD4-BD1, CDK6 and CDK4, respectively. CDK4/6/BRD4-IN-1 (B15) can be used in the study of NSCLC (Non-Small Cell Lung Cancer). CDK4/6/BRD4-IN-1 (B15) induces cell cycle arrest and apoptosis.
    CDK4/6/BRD4-IN-1
  • HY-N15522
    Bi-magnolignan
    Bi-magnolignan is a BRD4 inhibitor that induces DNA damage and apoptosis. Bi-magnolignan inhibits HCT116 cell proliferation with an IC50 value of 2.9 μM.
    Bi-magnolignan
  • HY-169270
    PROTAC SMARCA2 degrader-19
    		Degrader
    PROTAC SMARCA2 degrader-19 (Compound 46) is a PROTAC degrader for SMARCA2, that degrades SMARCA2 in cell A549 and MV411 with a DC50 < 100 nM. PROTAC SMARCA2 degrader-19 degrades SMARCA4 in cell MV411 with a DC50 > 1000 nM.
    PROTAC SMARCA2 degrader-19
  • HY-100670
    Olinone
    		Inhibitor
    Olinone is a selective BRD4 BrD1 inhibitor. Olinone accelerates the progression of mouse primary oligodendrocyte progenitors toward differentiation.
    Olinone
  • HY-169271
    PROTAC SMARCA2 degrader-20
    		Degrader
    PROTAC SMARCA2 degrader-20 (Compound I-40) is a PROTAC SMARCA2 degrader. PROTAC SMARCA2 degrader-20 has the potential for the research of cancer.
    PROTAC SMARCA2 degrader-20
  • HY-170832
    Menin–KMT2A-IN-1
    		Inhibitor
    Menin–KMT2A-IN-1 (Compound 20) is the inhibitor for menin–KMT2A that binds to menin with an IC50 of 8 nM, and inhibits the interaction between menin and lysine methyltransferase 2A (KMT2A). Menin–KMT2A-IN-1 inhibits hERG with an IC50 of 65 μM. Menin–KMT2A-IN-1 inhibits cell MV4-11 with an IC50 of 74 nM. Menin–KMT2A-IN-1 exhibits good pharmacokinetic characteristics in CD-1 mouse with an orally bioavailability of 74%.
    Menin–KMT2A-IN-1
  • HY-143327
    PROTAC BRD4 Degrader-16
    		Degrader
    PROTAC BRD4 Degrader-16 is a potent PROTAC BRD4 Degrader, with IC50 values of 34.58 nM (BRD4 (BD1)) and 40.23 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-16 ignificantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-16 significantly induces apoptosis in MV-4-11 cells.
    PROTAC BRD4 Degrader-16
  • HY-161387
    EBET-590
    		Inhibitor
    EBET-590 is a BET inhibitor, and can be used for cancer research
    EBET-590
  • HY-112149A
    (E/Z)-ZL0420
    		Inhibitor
    (E/Z)-ZL0420 is a racemic compound of (Z)-ZL0420 and (E)-ZL0420 isomers. (E)-ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2.
    (E/Z)-ZL0420
  • HY-170808
    PROTAC BRD4 Degrader-28
    		Degrader
    PROTAC BRD4 Degrader-28 (Compound 4) is a PROTAC degrader targeting BRD4. PROTAC BRD4 Degrader-28 is promising for research of cancers (Pink: target protein ligand JQ-1 (carboxylic acid) (HY-78695); Black+ Blue: E3 ubiquitin ligase ligand-Linker conjugate Thalidomide-O-amido-C3-NH2 (HY-115560)).
    PROTAC BRD4 Degrader-28
  • HY-160694
    cBu-Cit-GAL-02-221
    		Degrader
    cBu-Cit-GAL-02-221 is a PROTAC that degrades BRD4 by association with cBu-Cit. cBu-Cit-GAL-02-221 can effectively inhibit BRD4 in HER2 positive and negative breast cancer cell lines. cBu-Cit-GAL-02-221 has a single bond and can be conjugated to an ADC antibody to form a PAC.
    cBu-Cit-GAL-02-221
  • 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-149100
    PLK1-IN-6
    		Inhibitor
    PLK1-IN-6 is a potent and selective PLK1 inhibitor, with an IC50 of 0.45 nM. PLK1-IN-6 shows significant anti-proliferative activities against cancer cells.
    PLK1-IN-6
  • 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-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)
Cat. No. Product Name / Synonyms Application Reactivity