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| 2mg |
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| 25mg |
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Purity: ≥98%
NH125 (NH-125; NH 125) is a potent and selective eEF-2 (eukaryotic elongation factor 2) kinase inhibitor with antibacterial activity against various Gram-positive and -negative bacteria. It inhibits eEF-2 with an IC50 of 60 nM, and showed >125-fold selectivity over PKC, PKA, and CaMKI. NH125 is also a potent histidine kinase inhibitor. When tested with a panel of 10 cancer cell lines (C6, T98-G, U-138 MG, and so forth), NH125 treatment inhibited cell viability with IC50 value ranges from 0.7 to 4.8 μM. NH125 decreased the cellular content of p-eEF-2 without affecting total content eEF-2 and arrested cell in G0-G1 phase in C6 glioma cells. When tested with a panel of human cancer cell lines (glioblastoma, breast cancer, and so on), NH125 sensitized cells at the dose of 0.25 μM which thus reinforced the efficacy of ER stress-inducing drug by inhibiting eEF-2.
| ln Vitro |
NH125 exhibits relative selectivity over other protein kinases, including protein kinase C (IC50 = 7.5 μM), protein kinase A (IC50 = 80 μM), and calmodulin-dependent kinase II (IC50 > 100 μM). It also inhibits eEF-2 kinase activity (IC50 = 60 nM) in vitro and prevents eEF-2 from being phosphorylated in intact cells. Ten cancer cell lines with IC50s ranging from 0.7 to 4.7 μM are less viable when exposed to NH125. In a glioma cell line, forced overexpression of eEF-2 kinase results in 10-fold resistance to NH125. In conclusion, these results suggest that identification of potent inhibitors of eEF-2 kinase may lead to the development of new types of anticancer drugs[1]. Anticancer effect of NH125 is not mediated through inhibition of eEF2K. Inhibition of cell growth correlates with induction of peEF2[2].
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| ln Vivo |
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| References |
[1]. Arora S, et al. Identification and characterization of an inhibitor of eukaryotic elongation factor 2 kinase against human cancer cell lines. Cancer Res. 2003 Oct 15;63(20):6894-9.
[2]. Chen Z, et al. 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. 2011 Dec 23;286(51):43951-8. |
| Molecular Formula |
C27H45IN2
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| Molecular Weight |
524.56
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| CAS # |
278603-08-0
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| Related CAS # |
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| SMILES |
[I-].N1(C=C[N+](CC2C=CC=CC=2)=C1C)CCCCCCCCCCCCCCCC
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| InChi Key |
RVWOHCBHAGBLLT-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C27H45N2.HI/c1-3-4-5-6-7-8-9-10-11-12-13-14-15-19-22-28-23-24-29(26(28)2)25-27-20-17-16-18-21-27;/h16-18,20-21,23-24H,3-15,19,22,25H2,1-2H3;1H/q+1;/p-1
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| Chemical Name |
1-Hexadecyl-2-methyl-3-(phenylmethyl)-1H-imidazolium iodide
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9064 mL | 9.5318 mL | 19.0636 mL | |
| 5 mM | 0.3813 mL | 1.9064 mL | 3.8127 mL | |
| 10 mM | 0.1906 mL | 0.9532 mL | 1.9064 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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