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Histone Methyltransferase

Histone methyltransferase inhibitors target the enzymes that methylate lysine residues on histone tails. Lysine methyltransferases transfer methyl groups from S-adenosylmethionine to defined lysines, most often on histone H3. Methylation of lysine 27 of histone H3 (H3K27) by enhancer of zeste homolog 2 (EZH2) is linked to Polycomb gene silencing, while H3K9 methylation marks heterochromatin. Most compounds here target EZH2, including GSK126, GSK343 and tazemetostat, which compete with S-adenosylmethionine. UNC0642 inhibits G9a and G9a-like protein (GLP), pinometostat targets the H3K79 methyltransferase disruptor of telomeric silencing 1-like (DOT1L), and chaetocin acts on suppressor of variegation 3-9 homolog (SUV39H) enzymes. Inhibitors of arginine-directed enzymes are listed under Protein Arginine Methyltransferases.

3 Items

  • PRMT5 ligand 1
    Cat. No.
    A26606
    CAS No.
    1616393-25-9

    PRMT5 ligand 1

    PRMT5 ligand 1 is a specific ligand for the enzyme PRMT5, which plays a crucial role in the regulation of various cellular processes through protein arginine methylation. This compound serves as a valuable tool in the development of proteolysis-targeting chimeras (PROTACs), particularly in synthesizing the degrader MS4322. Its application in research facilitates the investigation of PRMT5's biological functions and its potential as a therapeutic target in cancer and other diseases.

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  • EZH2 ligand-1
    Cat. No.
    A26608
    CAS No.
    2641602-26-6

    EZH2 ligand-1

    EZH2 ligand-1 is a small molecule that specifically binds to the Enhancer of Zeste Homolog 2 (EZH2), a key component of the PRC2 complexes involved in epigenetic regulation through histone methylation. This compound serves as a valuable tool for synthesizing PROTACs aimed at targeted protein degradation and is relevant for studying oncogenic processes linked to EZH2 dysregulation. Its application in research contributes to the understanding of cancer biology and the development of novel therapeutic strategies.

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  • EZH2 ligand-3
    Cat. No.
    A57758
    CAS No.
    3034875-47-0

    EZH2 ligand-3

    EZH2 ligand-3 functions as a ligand targeting the Enhancer of Zeste Homolog 2 (EZH2) protein. This compound plays a crucial role in the synthesis of PROTAC EZH2 Degrader-35, facilitating the selective degradation of EZH2 in cellular models. It is valuable for research applications focused on epigenetic regulation and targeted protein degradation strategies.

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