For research use only. Not for therapeutic Use.
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].
| Catalog Number | I043518 |
| CAS Number | 2387633-15-8 |
| Synonyms | 2-[1-[[2-(3,5-dichlorophenyl)-6-[2-(4-methylpiperazin-1-yl)pyrimidin-5-yl]oxypyridin-4-yl]methyl]piperidin-4-yl]acetic acid |
| Molecular Formula | C28H32Cl2N6O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C28H32Cl2N6O3/c1-34-6-8-36(9-7-34)28-31-16-24(17-32-28)39-26-11-20(18-35-4-2-19(3-5-35)12-27(37)38)10-25(33-26)21-13-22(29)15-23(30)14-21/h10-11,13-17,19H,2-9,12,18H2,1H3,(H,37,38) |
| InChIKey | AZEJIKZNBHEXCM-UHFFFAOYSA-N |
| SMILES | CN1CCN(CC1)C2=NC=C(C=N2)OC3=CC(=CC(=N3)C4=CC(=CC(=C4)Cl)Cl)CN5CCC(CC5)CC(=O)O |
| Reference | [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. |
