| Bioactivity | 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]. | |||||||||
| Target | IC50: 770 nM (Nek2) | |||||||||
| Invitro | 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: | |||||||||
| Name | JH295 hydrate | |||||||||
| Formula | C18H18N4O3 | |||||||||
| Molar Mass | 338.36 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Jeffrey C Henise, et al. Irreversible Nek2 kinase inhibitors with cellular activity. J Med Chem. 2011 Jun 23;54(12):4133-46. |