NH125 | Eukaryotic elongation factor 2 (eEF-2) kinase inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $65.00 | ||
| 25 mg | $220.00 |
NH125 (278603-08-0) 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
References/Citations:
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
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
NH125 (278603-08-0) 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
References/Citations:
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
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