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JH295

Chemical Structure : JH295

CAS No.: 1311143-71-1

JH295 (JH-295)

Catalog No.: PC-20309Not For Human Use, Lab Use Only.

JH295 (JH-295) is a potent, selective and irreversible Nek2 kinase inhibitor with IC50 of 770 nM, inhibits Nek2 via alkylation of residue Cys22, does not inhibit Cdk1/CycB (IC50>20 uM).

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Biological Activity

JH295 (JH-295) is a potent, selective and irreversible Nek2 kinase inhibitor with IC50 of 770 nM, inhibits Nek2 via alkylation of residue Cys22, does not inhibit Cdk1/CycB (IC50>20 uM).
JH295 selectively and irreversibly inhibits cellular Nek2 without affecting the mitotic kinases, Cdk1, Aurora B, or Plk1, does not perturb bipolar spindle assembly or the spindle assembly checkpoint.
JH295 inhibits cellular Nek2 in a Cys22-dependent manner, inhibits WT Nek2 in cells with IC50 of 1.6 uM in IP kinase assays, shows little effect on the C22V mutant.
JH295 does not perturb bipolar spindle assembly or chromosome congression. 

Physicochemical Properties

M.Wt 320.35
Formula C18H16N4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-[(3Z)-3-[(2-Ethyl-4-methyl-1H-imidazol-5-yl)methylene]-2,3-dihydro-2-oxo-1H-indol-5-yl]-2-propynamide

References

1. Henise JC, et al. J Med Chem. 2011 Jun 23;54(12):4133-46.

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