NH125
Eukaryotic elongation factor 2 (eEF-2) kinase inhibitor / NH125 was originally discovered as an antibacterial agent active against various Gram-positive and -negative bacteria via inhibition of histidine protein kinase.1 It was also found to be a potent inhibitor of eukaryotic elongation factor 2 (eEF-2) kinase (IC50 = 60 nM) with efficacy against a broad spectrum of human cancer cell lines.2 Other studies have linked the anticancer effects of NH125 to induction of eEF2 phosphorylation.3,4 NH125 has also been shown to engage the EIF2a-ATF4-CHOP axis resulting in induction of DR5 expression.5 Treatment of glioma stem cells with NH125 resulted in a sustained decrease in tumor volume via activation of integrated stress response (ISR) and GADD45 pathways.5
Biochemicals & reagents
278603-08-0
1) Yamamoto et al. (2000), Identification and Characterization of a Potent Antibacterial Agent, NH125, against Drug-resistant Bacteria; Biosci. Biotechnol. Biochem. 64 919 2) 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 3) Chen et al. (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 4) Devkota et al. (2012), Investigating the kinetic mechanism of inhibition of elongation factor 2 kinase by NH125: evidence of a common in vitro artifact; Biochemistry 51 2100 5) Sheikh et al. (2019), An Integrated Stress Response Agent that Modulates DR5-Dependent TRAIL Synergy Reduces Patient-Derived Glioma Stem Cell Viability; Mol. Cancer Res. 17 1102
-20°C
TARGET: Kinase; Antibiotic -- PATHWAY: DNA damage; Protein synthesis -- RESEARCH AREA: Cancer Stem Cells -- DISEASE AREA: Cancer; Infectious disease