NH-125

SKU: orb1225444

Description

A potent eukaryotic eEF-2 kinase (eEF2K) inhibitor with IC50 of 60 nM in vitro and blocks the phosphorylation of eEF-2 in intact cells; shows relative selectivity over other protein kinases: PKC (IC50=7.5 uM), PKA (IC(50=80 uM), and CaMKII (IC50>100 uM); shows efficacious anti-proliferation activityt against different cancer cells.

Key Properties

• CAS Number: 278603-08-0
• MW: 524.56
• Purity: >98% (HPLC)
• Formula: C₂₇H₄₅IN₂
• SMILES: CC1=[N+](CC2=CC=CC=C2)C=CN1CCCCCCCCCCCCCCCC.[I-]
• Target: eIF
• Solubility: DMSO: 52.5 mg/mL (100 mM); Ethanol: 39.3 mg/mL (75 mM) （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NH 125 | NH125

Quick Database Links

Gene Symbol

eIF