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Nek2 inhibitor (R)-21

Chemical Structure : Nek2 inhibitor (R)-21

CAS No.: 1364269-10-2

Nek2 inhibitor (R)-21

Catalog No.: PC-61483Not For Human Use, Lab Use Only.

A potent and selective NIMA-related Kinase 2 (NEK2) inhibitor with IC50 of 22 nM, >200-fold selectivity over Plk1, Mps1, Aurora A and CDK2.

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    Biological Activity

    Nek2 inhibitor (R)-21 is a potent and selective NIMA-related Kinase 2 (NEK2) inhibitor with IC50 of 22 nM, >200-fold selectivity over Plk1, Mps1, Aurora A and CDK2.
    Nek2 inhibitor (R)-21 also shows >100-fold selectivity over a panel of 24 kinases.
    Nek2 inhibitor (R)-21 down-regulates C-Nap1 phosphoryation with IC50 of 0.8 uM, shows antiproliferative effect on U2OS, MDA-MB-231, HeLa and MCF7 cell with GI50 of 1.82, 4.16, 0.59 and 2.17 uM, respectively.
    Nek2 inhibitor (R)-21 is a valuable tool for investigating the role of Nek2 in the cell cycle and its function in mitotic organization.

    Physicochemical Properties

    M.Wt 490.545
    Formula C24H25F3N4O2S
    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)-(Z)-4-(2-Amino-5-(4-((dimethylamino)methyl)thiophen-2-yl)pyridin-3-yl)-2-((5,5,5-trifluoropent-3-en-2-yl)oxy)benzamide

    References

    1. Innocenti P, et al. J Med Chem. 2012 Apr 12;55(7):3228-41.

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