SSM 3 trifluoroacetate

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[1][2].

Research Areas >> Infection

Signaling Pathways >> Others >> Others

EC50: 54 nM (furin) Ki: 12 nM (furin)[1]

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[2]. 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[2]. 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[2].

[1]. Albert G Remacle, et al. Selective and Potent Furin Inhibitors Protect Cells From Anthrax Without Significant Toxicity. Int J Biochem Cell Biol

[2]. Guan-Sheng Jiao, et al. Synthetic Small Molecule Furin Inhibitors Derived From 2,5-dideoxystreptamine. Proc Natl Acad Sci U S A. 2006 Dec 26;103(52):19707-12.