1311143-71-1

1311143-71-1 structure

Name: JH 295
Chemical Name: (Z)-N-(3-((2-ethyl-4-methyl-1H-imidazol-5-yl)methylene)-2-oxoindolin-5-yl)propiolamide
CAS Number: 1311143-71-1
Molecular Formula: C₁₈H₁₆N₄O₂
Molecular Weight: 320.345
Catalog: Signaling Pathways Others Others
Create Date: 2018-05-16 08:39:22
Modify Date: 2024-01-04 07:37:17
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].

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

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.