NH125 is a potent and selective inhibitor of eukaryotic elongation factor 2 kinase (eEF-2K/CaMKIII), also can induce eEF2 phosphorylation, with an IC50 of 60 nM for eEF-2K.

Product information

CAS Number: 278603-08-0

Molecular Weight: 524.56

Formula: C27H45IN2

Chemical Name: 3-benzyl-1-hexadecyl-2-methyl-1H-imidazol-3-ium iodide

Smiles: [I-].CC1N(CCCCCCCCCCCCCCCC)C=C[N+]=1CC1C=CC=CC=1

InChiKey: RVWOHCBHAGBLLT-UHFFFAOYSA-M

InChi: 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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 160 mg/mL (305.02 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

NH125 inhibits eEF-2 kinase activity (IC50 = 60 nM) in vitro, blocks the phosphorylation of eEF-2 in intact cells, and shows relative selectivity over other protein kinases: protein kinase C (IC50 = 7.5 μM), protein kinase A (IC50 = 80 μM), and calmodulin-dependent kinase II (IC50 > 100 μM). NH125 decreases the viability of 10 cancer cell lines with IC50s ranging from 0.7 to 4.7 μM. Forced overexpression of eEF-2 kinase in a glioma cell line produces 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. Anticancer effect of NH125 is not mediated through inhibition of eEF2K. Inhibition of cell growth correlates with induction of peEF2.

Products are for research use only. Not for human use.