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Beschreibung

A cell-permeable phthalimide compound that is reported to inhibit dynamin GTPase activity (IC50 = 17.4 and 63 µ,M using purified sheep brain dynamin I and recombinant dynamin II, respectively) in a GTP-competitive manner. Shown to block K+-induced SVE (synaptic vesicle endocytosis) of FM4-64 dye into rat brain synaptosomes (IC50 = 12.9 µ,M), while being ineffective at 30 µ,M against RME (receptor-mediated endocytosis) of transferrin into human osteosarcoma epithelial U2OS cells, presumably due to poor dynamin II inhibitory potency and/or rapid efflux and/or limited permeability in this cell line.

Strukturformel

SAF-324412-10MG

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