BOS-318 (BOS318) is a potent, highly selective, cell-permeable furin inhibitor with IC50 of 1.9 nM, Ki of 0.4 nM.
BOS-318 displays 13 times more potent against furin than PCSK5 (IC50 =25.3 nM), 24 times more potent than PCSK7 (IC50 =45.8 nM), and 110 times more potent than PCSK6 (IC50 =209.4 nM).
BOS-318 reduces endogenous proteases in the Golgi compartment in U2OS cells with IC50 of 23.5 nM.
BOS-318 provides protection against PEA-mediated cytotoxicity in a dose-dependent manner in CuFi-1 cells, over a period of 72 h, with an EC50 of 47.8 nM.
BOS-318 reduces ENaC-mediated Na+ absorption in CF HBECs after short- (2-h) and long-term (48-h) treatment and protects against NE- and CF sputum-sol-mediated activation of the ENaC.
