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.

• Sinônimo(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
• Fórmula empírica (Notação de Hill): C₂₇H₄₅IN₂
• Número CAS: 278603-08-0
• Peso molecular: 524.56
• Número MDL: MFCD07370143
• Código UNSPSC: 12352200

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥95% (NMR)
• forma: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; desiccated (hygroscopic); protect from light
• cor: white to yellow
• solubilidade: DMSO: 20 mg/mL; 70% ethanol: 5 mg/mL
• temperatura de armazenamento: 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
• chave InChI: RVWOHCBHAGBLLT-UHFFFAOYSA-M

Descrição

Descrição geral

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.

Ações bioquímicas/fisiológicas

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

Advertência

Toxicity: Irritant (B)

Reconstituição

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

Outras notas

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.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable