Chemical Name: N-[(3Z)-3-[(2-Ethyl-4-methyl-1H-imidazol-5-yl)methylene]-2,3-dihydro-2-oxo-1H-indol-5-yl]-2-propynamide
Biological ActivityJH 295 is an irreversible Nek2 inhibitor (IC50=770 nM). Inhibits Nek2 via alkylation of residue Cys22. Displays 5-fold selectivity for Nek2 over Cdk1. Exhibits no significant effect on Aurora B or Plk1 kinases, bipolar spindle assembly or spindle assembly checkpoint. Cell permeable.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Irreversible Nek2 kinase inhibitors with cellular activity.
Henise et al.
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