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.
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.
生化/生理作用
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
警告
Toxicity: Irritant (B)
重構
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他說明
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.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany