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Beschreibung

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 µ,M). 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 µ,M 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 (IC₅,₀, = 37.8 nM). Blocks the first translocation step and has no effect on tRNA binding.