JH 295

Names

[ 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]:

Research Areas >> Cancer

Signaling Pathways >> Others >> Others

[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]

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

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

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.