NH 125

Biological Activity

NH 125 is an 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

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.

Background References

1. Inhibition of elongation factor-2 kinase augments the antitumor activity of Temozolomide against glioma.
   Liu, Xiao-Yua, Zhang, Li, Wu, Jianping, Zhou, Lei, Ren, Yi-Jie, Yang, Wei-Qion, Ming, Zi-Jun, Chen, Bo, Wang, Jianrong, Zhang, Yi, Yang, Jin-Ming
   PLoS ONE, 2013;8(11):e81345.
2. 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.
   Chen
   J.Biol.Chem., 2011;286:43951
3. Antibacterial agents that inhibit histidine protein kinase YycG of Bacillus subtilis.
   Yamamoto et al.
   Biosci.Biotechnol.Biochem., 2001;65:2306
4. Identification and characterization of an inhibitor of eukaryotic elongation factor 2 kinase against human cancer cell lines.
   Arora et al.
   Cancer Res., 2003;63:6894
5. P-glycoprotein mediates resistance to histidine kinase inhibitors.
   Arora et al.
   Mol.Pharmacol., 2004;66:460

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