eEF-2 Kinase Inhibitor
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eEF-2 Kinase Inhibitor

1-Hexadecyl-2-methyl-3-(phenylmethyl)-1H-imidazolium iodide (NH125)
eEF-2 Kinase Inhibitor (inhibitor of eukaryotic elongation factor 2 kinase against human cancer cell lines & potent antibacterial agent against drug-resistant bacteria)
histidine protein kinase and 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. Exhibits anticancer activity in a variety of malignant cell lines (IC50 values are 0.7 - 4.8 ?M) and blocks G1/S cell cycle progression. Also is an effective antibacterial agent in vitro (IC50 = 6.6 ?M) and in vivo

**Tautomeric double bonds in the structure **

OTAVAchemicals Catalogue Number: 7070707012
CAS Registry Number: 278603-08-0
Purity: 97%+ (CHN analysis, 13C NMR & 1H NMR)

Ref. 1: Arora et al. Identification and Characterization of an Inhibitor of Eukaryotic Elongation Factor 2 Kinase against Human Cancer Cell Lines. Cancer Research (2003), 63, 6894-6899

Abstract: NH125 inhibited eEF-2 kinase activity (IC50 = 60 nM) in vitro, blocked the phosphorylation of eEF-2 in intact cells, and showed relative selectivity over other protein kinases: protein kinase C (IC50 = 7.5 mM), protein kinase A (IC50 = 80 mM), and calmodulin-dependent kinase II (IC50 > 100 mM). NH125 decreased the viability of 10 cancer cell lines with IC50s ranging from 0.7 to 4.7 mM. Forced overexpression of eEF-2 kinase in a glioma cell line produced 10-fold resistance to NH125. These results suggest that identification of potent inhibitors of eEF-2 kinase may lead to the development of new types of anticancer drugs.

Ref. 2: Yamamoto et al. Identification and characterization of a potent antibacterial agent, NH125, against drug-resistant bacteria. Bioscience,

Biotechnology, and Biochemistry (2000), 64, 919-923

Abstract: New imidazole compounds were synthesized to develop a novel and effective antibacterial agent: 1-benzyl-3-cetyl-2-methylimidazolium iodide (NH125). In vitro experiments demonstrated that NH125 effectively inhibited a number of different histidine protein kinases. Furthermore, oxacillin-resistant Staphylococcus aureus (ORSA), vancomycin-resistant Enterococcus faecalis (VRE), penicillin-resistant Streptococcus pneumoniae (PRS), and other Gram-positive and Gram-negative bacteria were found to be very sensitive to NH125.