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编 号:F618710
分子式:C30H36F12N12O10
分子量:952.66
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生物活性:
SSM3 tetraTFA is a potent synthetic furin inhibitor with an EC50 and a Ki of 54 nM and 12 nM, respectively. SSM3 tetraTFA is able to block furin-dependent cell surface processing of anthrax protective antigen-83?in vitro.

体外研究:
SSM3 tetraTFA is against furin cleavage of the Pyr-RTKR-AMC substrate with an EC50 of 54 nM in vitro?cleavage assays and cell-based tests.SSM3 tetraTFA (0.1-25 μM) inhibits the furin-dependent conversion of PA83 into PA63 in a dose dependent manner, it inhibits PA83 processing in the cleavage reactions.SSM3 tetraTFA shows comparable potency against furin (Ki=0.012 μM) and PC6B (Ki=0.004 μM), these compounds preferentially inhibited furin over PACE4 (Ki=0.041 μM) by 2- to 10-fold and over PC7 (Ki=0.595 μM) by 11- to 76-fold. In addition, it inhibits LF (Ki=1.241 μM) 25- to 167-fold less effectively than in furin and shows no measurable inhibition against trypsin and MT1-MMP.
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