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NH125

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Category Hepatitis C Virus (HCV)
CAS 278603-08-0
Description NH125 is a potent and selective eEF-2 kinase inhibitor with an IC50 of 60 nM, and also a potent histidine kinase inhibitor. It shows >125-fold selectivity over PKC, PKA, and CaMKII.
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Product Information

Synonyms 3-Benzyl-1-hexadecyl-2-methyl-1H-imidazol-3-ium Iodide; 1-hexadecyl-2-methyl-3-(phenylmethyl)-1H-Imidazolium iodide; NSC717205; 1-Benzyl-3-cetyl-2-methylimidazolium iodide; 1H-Imidazolium, 1-hexadecyl-2-methyl-3-(phenylmethyl)-, iodide (1:1)
IUPAC Name 1-benzyl-3-hexadecyl-2-methylimidazol-1-ium;iodide
Molecular Weight 524.56
Molecular Formula C27H45IN2
Canonical SMILES CCCCCCCCCCCCCCCCN1C=C[N+](=C1C)CC2=CC=CC=C2.[I-]
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
InChIKey RVWOHCBHAGBLLT-UHFFFAOYSA-M
Melting Point 88.2-94.9°C
Purity >98%
Solubility Soluble in DMSO
Appearance White to Off-white Solid
Storage Store at 2-8°C, sealed storage, away from moisture
Complexity 364
Exact Mass 524.26275
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.
PSA 8.81000
Target CaMK III: 60 nM (IC50)

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