JH 295

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Cat.No. 4322 - JH 295 | C18H16N4O2 | CAS No. 1311143-71-1
Description: Irreversible Nek2 inhibitor
Chemical Name: N-[(3Z)-3-[(2-Ethyl-4-methyl-1H-imidazol-5-yl)methylene]-2,3-dihydro-2-oxo-1H-indol-5-yl]-2-propynamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Irreversible Nek2 inhibitor (IC50=770 nM). Inhibits Nek2 via alkylation of residue Cys22. Displays 5-fold selectivity for Nek2 over Cdk1. Exhibits no significant effect on Aurora B or Plk1 kinases, bipolar spindle assembly or spindle assembly checkpoint. Cell permeable.

Technical Data

M. Wt 320.35
Formula C18H16N4O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1311143-71-1
PubChem ID 53262909
InChI Key ORKOHXAJFGRZCL-LCYFTJDESA-N
Smiles O=C2NC1=CC=C(NC(C#C)=O)C=C1/C2=C/C3=C(C)N=C(CC)N3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 32.03 100

Preparing Stock Solutions

The following data is based on the product molecular weight 320.35. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.12 mL 15.61 mL 31.22 mL
5 mM 0.62 mL 3.12 mL 6.24 mL
10 mM 0.31 mL 1.56 mL 3.12 mL
50 mM 0.06 mL 0.31 mL 0.62 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Henise et al (2011) Irreversible Nek2 kinase inhibitors with cellular activity. J.Med.Chem. 54 4133 PMID: 21627121


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Keywords: JH 295, supplier, JH295, Nek2, inhibitor, inhibits, irreversible, alkylation, Nek2, Kinase, Nek2, Kinase, Tocris Bioscience

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