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Furin is a proprotein convertase, converting precursor proteins to functional proteins within the Golgi/trans-Golgi secretory pathway. Naphthofluorescein is a cell-permeable inhibitor of furin (IC50 = 12 μM). It inhibits furin-mediated cleavage of the pro-form of membrane type-1 matrix metalloproteinase (MT1-MMP), resulting in decreased levels of active MT1-MMP. This, in turn, suppresses MMP-2 activation and reduces cell motility in CHO cells expressing proMT1-MMP. Napthofluorescein significantly inhibits the invasion of Matrigel by the human fibrosarcoma cell line, HT1080. The effects of this furin inhibitor on other furin-mediated processes, in vivo or in vitro, remain to be determined.

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