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SMYD3 inhibitor 29

Chemical Structure : SMYD3 inhibitor 29

CAS No.: 2095160-79-3

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SMYD3 inhibitor 29

Catalog No.: PC-72992Not For Human Use, Lab Use Only.

SMYD3 inhibitor 29 is a highly potent, selective, covalent inhibitor of histone methyltransferase SMYD3 with IC50 of 1.7 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    SMYD3 inhibitor 29 is a highly potent, selective, covalent inhibitor of histone methyltransferase SMYD3 with IC50 of 11.7 nM.
    SMYD3 inhibitor 29 exhibits high potency by inhibiting SMYD3's enzymatic activity and showing antiproliferative activity against HepG2 in 3D cell culture (GI50=1.04 uM).
    SMYD3 inhibitor 29 inhibits cellular MAP3K2 methylation.
    SMYD3 inhibitor 29 displayed high selectivity when tested against a panel of methyltransferases, namely, SMYD1-2, G9a, PRDM9, and PRMT5.

    Physicochemical Properties

    M.Wt 491.032
    Formula C28H31ClN4O2
    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

    (R)-1-(4-(2-(4-(1-aminocyclopropyl)phenyl)-4-chloroquinoline-7-carbonyl)-2-methylpiperazin-1-yl)butan-1-one

    References

    1. Huang C, et al. ACS Med Chem Lett. 2019 May 23;10(6):978-984.

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