Cat. No. 3439
Chemical Name: 1-Hexadecyl-2-methyl-3-(phenylmethy
Biological ActivityEukaryotic 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.
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.
Certificate of Analysis / Safety Data Sheet
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.
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Keywords: NH 125, supplier, CaM, kinase, III, CAMK, eEF-2, inhibitors, Histidine, protein, kinases, Calmodulin-Activated, calmodulin-dependent, Protein, NH125, Tocris Bioscience, Calmodulin-Dependent Kinase Inhibitors
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March 14 - 16, 2016
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