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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.

1 Item

  • AR420626
    Cat. No.
    A23991
    CAS No.
    1798310-55-0

    AR420626

    AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3, also known as GPR41), with an IC₅₀ of 117 nM. It demonstrates anti-inflammatory, antitumor, and antidiabetic activities. AR420626 improves neurogenic diarrhea by modulating neural pathways mediated by nicotinic acetylcholine receptors (nAChRs). In cancer models, it suppresses the growth of HepG2 xenografts and inhibits hepatoma cell proliferation through apoptosis induction. Additionally, AR420626 mitigates allergic asthma and eczema and enhances glucose uptake by activating FFAR3-mediated Ca²⁺ signaling, offering potential therapeutic benefits in metabolic disorders such as diabetes.

    In stock View Details
    5 mg
    $77.00
    10 mg
    $132.00
    All 4 sizes

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