Nek2 inhibitor (R)-21

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; also shows >100-fold selectivity over a panel of 24 kinases; 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; is a valuable tool for investigating the role of Nek2 in the cell cycle and its function in mitotic organization.

References 1. Innocenti P, et al. J Med Chem. 2012 Apr 12;55(7):3228-41. View Related Products by Target Hec1/Nek2