JH295 hydrate |
Katalog-Nr.GC60959 |
JH295-Hydrat ist ein potenter, irreversibler und selektiver Hemmer der NIMA-verwandten Kinase 2 (Nek2) mit einem IC50 von 770 nM. JH295-Hydrat hemmt zellulÄres Nek2 durch Alkylierung von Cys22. JH295-Hydrat ist gegen die mitotischen Kinasen Cdk1, Aurora B oder Plk1 inaktiv und stÖrt die bipolare Spindelanordnung oder den Spindelanordnungs-Checkpoint nicht.
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Sample solution is provided at 25 µL, 10mM.
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.
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