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NH125 | Eukaryotic elongation factor 2 (eEF-2) kinase inhibitor

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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Catalog#  10-4840-0005

$65.00
Quantity
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CAS:
278602-08-0
Catalog Number:
10-4840
Activity:
Eukaryotic elongation factor 2 (eEF-2) kinase inhibitor
Chemical Name:
1-Hexadecyl-2-methyl-3-(phenylmethyl)-1H-imidazlium iodide
Molecular Weight:
524.56
Molecular Formula:
C27H45IN2
Solubility:
Soluble in DMSO (up to at least 25 mg/ml) or in Ethanol (up to at least 25 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20° (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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