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MNKI-8e

Chemical Structure : MNKI-8e

CAS No.: 1610886-04-8

MNKI-8e (MNK inhibitor 8e)

Catalog No.: PC-63074Not For Human Use, Lab Use Only.

MNKI-8e (MNK inhibitor 8e) is a potent, selective MNK inhibitor that inhibits Mnk2 with Ki of 0.37 uM, displays >34-fold and 4-fold over CDK2 (Ki>10 uM) and CDK9 (Ki=1.66 uM).

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

    Biological Activity

    MNKI-8e (MNK inhibitor 8e) is a potent, selective MNK inhibitor that inhibits Mnk2 with Ki of 0.37 uM, displays >34-fold and 4-fold over CDK2 (Ki>10 uM) and CDK9 (Ki=1.66 uM).
    MNKI-8e potently inhibits leukemia cells with GI50 of 1.23-7.36 uM (MV4-11 GI50=1.32 uM and KG-1 GI50=1.23 uM).
    MNKI-8e blocks phosphorylation of eIF4E, downregulates anti-apoptotic protein Mcl-1 and induces apoptosis in AML cells.
    MNKI-8e suppresses the Ara-C-induced MAPK activity and enhances apoptosis in MV4-11 cells.

    Physicochemical Properties

    M.Wt 358.416
    Formula C17H18N4O3S
    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

    5-(2-((2,4-dimethoxyphenyl)amino)pyrimidin-4-yl)-3,4-dimethylthiazol-2(3H)-one

    References

    1. Diab S, et al. ChemMedChem. 2014 May;9(5):962-72.

    2. Li P, et al. Oncotarget. 2016 Aug 30;7(35):56811-56825.

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