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DNA Methyltransferases

DNMT inhibitors block the DNA methyltransferases that add methyl groups to cytosine residues in genomic DNA. DNA methyltransferase (DNMT) activity at cytosine-guanine (CpG) sites helps silence genes, transposable elements and imprinted loci. DNMT1 copies existing methylation patterns after replication, and its loss causes embryonic lethality in mice. DNMT3A and DNMT3B establish new patterns during development, a role shown in knockout mice in 1999. Cytidine analogs were linked to the inhibition of DNA methylation and to cell differentiation as early as 1980. The category includes the nucleoside analogs azacitidine, decitabine, zebularine and guadecitabine, together with the non-nucleoside inhibitor RG108.

1 Item

  • MS9024
    Cat. No.
    A57719
    CAS No.
    3107482-42-5

    MS9024

    MS9024 is a selective degrader of DNA methyltransferase 1 (DNMT1), facilitating its degradation in HCT116 cells through the ubiquitin-proteasome pathway, achieving a DC50 of 35 nM. In additional cell lines, such as MDA-MB-468 and H1299, MS9024 shows DC50 values of 254 nM and 101 nM, respectively. Furthermore, it exhibits inhibitory activity against DNMT1 with an IC50 of 0.43 μM, making it a valuable tool for studying the role of DNMT1 in epigenetic regulation and its implications in cancer research.

    In stock View Details
    5 mg
    $215.00
    10 mg
    $355.00
    All 4 sizes

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