Biological Activity
BOS-318 is a potent, slowly dissociating, highly selective, and cell-permeable furin inhibitor with IC50 value of 1.9 nM. BOS-318 protects ENaC from subsequent activation by neutrophil elastase. BOS-318 can be used for the rsearch for CF lung disease[1][2].
BOS-318 (0.001-1 μM, 72 hours) provides cytoprotection against toxicity in CuFi-1 cells induced by P aeruginosa exotoxin A (PEA)[1].BOS-318 (U2OS cells) to be approximately 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) [1].BOS-318 (0.3 μM, 2 hours or 48 hours) reduces ENaC-mediated Na+ absorption in CF HBECs and protects against NE- and CF sputum-sol-mediated activation of the ENaC[1].
References
[1]. Douglas LEJ, et al. A highly selective, cell-permeable furin inhibitor BOS-318 rescues key features of cystic fibrosis airway disease. Cell Chem Biol. 2022 Jun 16;29(6):947-957.e8.
[2]. Nayak D, et al. Clearing the air: Uniquely engaging furin as an approach to cystic fibrosis therapy. Cell Chem Biol. 2022 Jun 16;29(6):927-929.
