324515-M

eEF-2 Kinase Inhibitor, NH125

The eEF-2 Kinase Inhibitor, NH125, also referenced under CAS 278603-08-0, controls the biological activity of eEF-2 Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonyme(s) : eEF-2 Kinase Inhibitor, NH125, 1-Benzyl-3-cetyl-2-methylimidazolium iodide, 1-Cetyl-3-benzyl-2-methylimidazolium iodide, CaM-Dependent Kinase III Inhibitor, NH125
• Formule empirique (notation de Hill): C₂₇H₄₅IN₂
• Numéro CAS: 278603-08-0
• Poids moléculaire : 524.56
• Numéro MDL: MFCD07370143
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (NMR)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; desiccated (hygroscopic); protect from light
• Couleur: white to yellow
• Solubilité: DMSO: 20 mg/mL; 70% ethanol: 5 mg/mL
• Température de stockage: 2-8°C
• 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
• Clé InChI: RVWOHCBHAGBLLT-UHFFFAOYSA-M

Description

Description générale

A cell-permeable imidazolium compound that inhibits the activity of bacterial histidine kinases (EnvZ, PhoQ, BvgS, and EvgS) and eukaryotic eEF-2 (elongation factor 2) kinase/CaMKIII (IC₅₀ = 60 nM), while exhibiting much lower potency against PKC, PKA, and CaMKII (IC₅₀ = 7.5, 80, and >100 µM, respectively). NIH125 is a known P-gp substrate, which limits its in vivo efficacy as an anticancer and antimicrobial agent.

Actions biochimiques/physiologiques

Primary Target
Bacterial histidine kinases (EnvZ, PhoQ, BvgS, and EvgS) and eukaryotic eEF-2 (elongation factor 2) kinase/CaMKIII

Target IC₅₀: 60 nM against the activity of bacterial histidine kinases (EnvZ, PhoQ, BvgS, and EvgS) and eukaryotic eEF-2 (elongation factor 2) kinase/CaMKIII

Avertissement

Toxicity: Irritant (B)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Autres remarques

Arora, S., et al. 2004. Mol. Pharmacol.66, 460.
Arora, S., et al. 2003. Cancer Res.63, 6894.
Yamamoto, K., et al. 2000. Biosci. Biotechnol. Biochem.64, 919.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable