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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)
Biological Activity for JH 295
JH 295 is an 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 for JH 295
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for JH 295
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 32.03 | 100 |
Preparing Stock Solutions for JH 295
The following data is based on the product molecular weight 320.35. Batch specific molecular weights may vary from batch to batch due to the degree 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 for JH 295
References for JH 295
References are publications that support the biological activity of the product.
Henise et al (2011) Irreversible Nek2 kinase inhibitors with cellular activity. J.Med.Chem. 54 4133 PMID: 21627121
If you know of a relevant reference for JH 295, please let us know.
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Keywords: JH 295, JH 295 supplier, JH295, Nek2, inhibitor, inhibits, irreversible, alkylation, Kinase, 4322, Tocris Bioscience
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