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MS-453

Chemical Structure : MS-453

CAS No.: 2059892-29-2

MS-453 (MS453;MS 453)

Catalog No.: PC-60300Not For Human Use, Lab Use Only.

MS-453 (MS453) is a potent, selective and covalent protein lysine methyltransferase SETD8 inhibitor with IC50 of 804 nM.

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    Biological Activity

    MS-453 (MS453) is a potent, selective and covalent protein lysine methyltransferase SETD8 inhibitor with IC50 of 804 nM.
    MS-453 exhibits selectivity for SETD8 against 28 other methyltransferases.
    MS-453 does not causes significant reduction in the H4K20me in HeLa cells at up to 10 uM.
    MS-453 shows poor membrane permeability (4.4 nm/s) and high efflux ratio (137).

    Physicochemical Properties

    M.Wt 385.468
    Formula C20H27N5O3
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    N-(3-((6,7-dimethoxy-2-(pyrrolidin-1-yl)quinazolin-4-yl)amino)propyl)acrylamide

    References

    1. Butler KV, et al. J Med Chem. 2016 Nov 10;59(21):9881-9889.

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