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EML741

Chemical Structure : EML741

CAS No.: 2328074-38-8

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EML741 (EML-741)

Catalog No.: PC-22921Not For Human Use, Lab Use Only.

EML741 is a potent, selective inhibitor of H3K9-specific methyltransferases G9a/G9a-like protein (G9a/GLP) with IC50 of 23 nM (G9a), KD of 1.13 uM in MST assays.

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    Biological Activity

    EML741 is a potent, selective inhibitor of H3K9-specific methyltransferases G9a/G9a-like protein (G9a/GLP) with IC50 of 23 nM (G9a), KD of 1.13 uM in MST assays.
    EML741 shows high selectivity against a panel of other epigenetic enzymes (KMT5A/SETD8, KDM4A/JMJD2A, PRMT1, PRMT3, KAT3B/p300).
    EML741 (0.5 and 5 μM) induced a marked and both concentration- and time-dependent reduction in the dimethylation of lysine H3K9 in MCF-7 and MDA-MB-231 human breast adenocarcinoma cells.

    Physicochemical Properties

    M.Wt 523.77
    Formula C31H49N5O2
    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

    2-Cyclohexyl-7-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-8-[3-(1-pyrrolidinyl)propoxy]-3H-1,4-benzodiazepin-5-amine

    References

    1. Ciro Milite, et al. J Med Chem. 2019 Mar 14;62(5):2666-2689.

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