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Biological Activity for NH 125
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 for NH 125
|Storage||Desiccate at -20°C|
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.
Solubility Data for NH 125
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for NH 125
The following data is based on the product molecular weight 524.56. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.91 mL||9.53 mL||19.06 mL|
|5 mM||0.38 mL||1.91 mL||3.81 mL|
|10 mM||0.19 mL||0.95 mL||1.91 mL|
|50 mM||0.04 mL||0.19 mL||0.38 mL|
References for NH 125
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for NH 125, please let us know.
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Keywords: NH 125, NH 125 supplier, CaM, kinase, III, CAMK, eEF-2, inhibitors, inhibits, Histidine, protein, kinases, Calmodulin-Activated, calmodulin-dependent, Protein, NH125, Kinase, Other, Kinases, 3439, Tocris Bioscience
4 Citations for NH 125
Citations are publications that use Tocris products. Selected citations for NH 125 include:
Xu et al (2017) Neurons secrete miR-132-containing exosomes to regulate brain vascular integrity. Cell Res 27 882 PMID: 28429770
Francis et al (2013) Mechanistic insight into inhibition of two-component system signaling. Medchemcomm 4 269 PMID: 23336064
Cheng et al (2013) Integrated regulation of autophagy and apoptosis by EEF2K controls cellular fate and modulates the efficacy of curcumin and vel. against tumor cells. Autophagy 9 208 PMID: 23182879
Kim et al (2015) Identification of an Antimicrobial Agent Effective against Methicillin-Resistant Staphylococcus aureus Persisters Using a Fluorescence-Based Screening Strategy. PLoS One 10 e0127640 PMID: 26039584
Do you know of a great paper that uses NH 125 from Tocris? Please let us know.
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Literature in this Area
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