Biological Activity
Eukaryotic elongation factor 2 (eEF-2) kinase (CaMK III) inhibitor (IC50 = 60 nM) that displays 125-fold, > 1300-fold and > 1500-fold selectivity over PKC, PKA and CaMK II respectively. Decreases the viability of a variety of cancer cell lines (IC50 values are 0.7 - 4.8 μM) and blocks G1/S cell cycle progression. Shown to induce eEF-2 phosphorylation in cancer cells. Also an effective antibacterial agent; inhibits histidine protein kinase in vitro (IC50 = 6.6 μM) and in vivo.
Technical Data
| M. Wt | 524.56 |
| Formula | C27H45IN2 |
| Storage | Desiccate at -20°C |
| CAS Number | 278603-08-0 |
| PubChem ID | 10436839 |
| InChI Key | RVWOHCBHAGBLLT-UHFFFAOYSA-M |
| Smiles | CC1=[N+](CCCCCCCCCCCCCCCC)C=CN1CC2=CC=CC=C2.[I-] |
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 | 52.46 | 100 | |
| ethanol | 39.34 | 75 |
Preparing Stock Solutions
The following data is based on the product molecular weight 524.56. 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 | 1.91 mL | 9.53 mL | 19.06 mL |
| 5 mM | 0.38 mL | 1.91 mL | 3.81 mL |
| 10 mM | 0.19 mL | 0.95 mL | 1.91 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.38 mL |
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References
References are publications that support the products' biological activity.
Yamamoto et al (2001) Antibacterial agents that inhibit histidine protein kinase YycG of Bacillus subtilis. Biosci.Biotechnol.Biochem. 65 2306 PMID: 11758928
Arora et al (2003) Identification and characterization of an inhibitor of eukaryotic elongation factor 2 kinase against human cancer cell lines. Cancer Res. 63 6894 PMID: 14583488
Arora et al (2004) P-glycoprotein mediates resistance to histidine kinase inhibitors. Mol.Pharmacol. 66 460 PMID: 15322237
Chen (2011) 1-Benzyl-3-cetyl-2-methylimidazolium iodide (NH125) induces phosphorylation of eukaryotic elongation factor-2 (eEF2): a cautionary note on the anticancer mechanism of an eEF2 kinase inhibitor. J.Biol.Chem. 286 43951 PMID: 22020937
Keywords: NH 125, supplier, CaM, kinase, III, CAMK, eEF-2, inhibitors, inhibits, Histidine, protein, kinases, Calmodulin-Activated, calmodulin-dependent, Protein, NH125, CaM, Kinase, Other, Kinases, CaM, Kinase, Tocris Bioscience
