JH295 hydrate

JH295hydrate是一种有效，不可逆和选择性的NIMA-relatedkinase2(Nek2)抑制剂，IC50为770nM。JH295hydrate通过Cys22的烷基化抑制细胞Nek2。JH295hydrate对有丝分裂激酶Cdk1，AuroraB或Plk1没有活性，并且不会干扰双极纺锤体组件或纺锤体组件检查点。

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Background

JH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint[1].

JH295 (Compound 16; 0.08-20 μM; 45 minutes; RPMI7951 cells) treatment inhibits WT Nek2 in cells with an IC50 of ~1.3 μM, whereas it has little effect on the C22V mutant[1]. Western Blot Analysis[1] Cell Line: RPMI7951 cells

[1]. Jeffrey C Henise, et al. Irreversible Nek2 kinase inhibitors with cellular activity. J Med Chem. 2011 Jun 23;54(12):4133-46.