Merck, 5062910001, Lactimidomycin

General description
A glutarimide based 12-membered macrolide antibiotic with antifungal properties. Acts as a potent inhibitor of cell migration, cell proliferation, and protein synthesis (IC₅₀ = 37.82 nM), but does not affect RNA synthesis even at high concentrations (IC₅₀ >10 µM). Acts as a potent inhibitor of translation and appears to block the first translocation step without affecting tRNA binding or peptide bond formation. It exhibits about 10-fold greater potency than cycloheximide (Cat. No. 239763 and 239764). Binds to the same site on the 60S ribosomal subunit with high affinity (Kd = 500 nM vs 15 µM for cycloheximide). Shown to extend the survival of mice bearing P388 lymphoma by blocking cell growth, however, it does not significantly affect non-tumorigenic MCF10A breast cell lines. Also shown to retard the growth of MDA MB231 cells in nude mice (~0.6 /mg/kg).
Lactimidomycin, CAS 134869-15-1, inhibits cell migration, proliferation, & protein synthesis (IC₅₀ = 37.8 nM). Blocks the first translocation step and has no effect on tRNA binding.
Biochem/physiol Actions
Primary Target
Ribosome
Reversible: yes
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Schneider-Poetsch, T., et al. 2010. Nat. Chem. Biol.6, 209.
Micoine, K., et al. 2010. J. Am. Chem. Soc.132, 14064.
Ju, J., et al. 2009. J. Am. Chem. Soc.131, 1370.
Sugawara, K., et al. 1992. J. Antibiot.45, 1433.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)