JH 295

Modify Date: 2024-01-04 07:37:17

JH 295 Structure
JH 295 structure
Common Name JH 295
CAS Number 1311143-71-1 Molecular Weight 320.345
Density 1.4±0.1 g/cm3 Boiling Point N/A
Molecular Formula C18H16N4O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of JH 295


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].

 Names

Name (Z)-N-(3-((2-ethyl-4-methyl-1H-imidazol-5-yl)methylene)-2-oxoindolin-5-yl)propiolamide
Synonym More Synonyms

 JH 295 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

[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

 Synonyms

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]-