JH 295
Names
[ CAS No. ]:
1311143-71-1
[ Name ]:
JH 295
[Synonym ]:
N-{(3Z)-3-[(2-Ethyl-4-methyl-1H-imidazol-5-yl)methylene]-2-oxo-2,3-dihydro-1H-indol-5-yl}-2-propynamide
2-Propynamide, N-[(3Z)-3-[(2-ethyl-4-methyl-1H-imidazol-5-yl)methylene]-2,3-dihydro-2-oxo-1H-indol-5-yl]-
Biological Activity
[Description]:
JH295 is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 inhibits cellular Nek2 via alkylation of Cys22. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint[1].
[Related Catalog]:
[Target]
IC50: 770 nM (Nek2)[1]
[In Vitro]
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 Concentration: 0.08 μM, 0.25 μM, 0.74 μM, 2.2 μM, 6.6 μM, 20 μM Incubation Time: 45 minutes Result: Inhibited WT Nek2 in cells with an IC50 of ~1.3 μM, whereas had little effect on the C22V mutant.
[References]
Chemical & Physical Properties
[ Density]:
1.4±0.1 g/cm3
[ Molecular Formula ]:
C18H16N4O2
[ Molecular Weight ]:
320.345
[ Exact Mass ]:
320.127319
[ PSA ]:
86.88000
[ LogP ]:
1.21
[ Index of Refraction ]:
1.716