BOS-318 |
Catalog No.GC64637
One-Click Copy Product Info
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BOS-318 is a cell-permeable, potent, and highly selective inhibitor of furin (IC50=1.9nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2387633-15-8
Sample solution is provided at 25 µL, 10mM.
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BOS-318 is a cell-permeable, potent, and highly selective inhibitor of furin (IC50=1.9nM)[1-2]. BOS-318 is applicable for research in cystic fibrosis (CF) lung disease and can serve as an adjunctive therapy to CFTR modulators such as ETI[3-4].
In vitro, treatment of differentiated cystic fibrosis human bronchial epithelial cells (CF HBECs) with BOS-318 (0.3µM) for 2 or 48 hours significantly inhibited epithelial sodium channel (ENaC)-mediated sodium absorption. A 2- or 48-hour pretreatment of CF HBECs with BOS-318 (0.3µM), followed by stimulation with neutrophil elastase (NE; 2.5µg/mL) or CF sputum supernatant. BOS-318 protected ENaC from activation by NE. Treatment of CuFi-1 cells with BOS-318 (0.001–1µM) for 72 hours conferred dose-dependent protection against Pseudomonas aeruginosa exotoxin A (PEA; 500ng/mL)-mediated cytotoxicity[5]. In BRAF-mutated human melanoma cell lines (A375M6 and M21), a 24-hour treatment with BOS-318 (5nM) reduced the expression of TGFβ1 and phosphorylated SMAD2. When combined with pirfenidone (8.1mM), BOS-318 synergistically increased p21 expression and elevated the proportion of cells entering late apoptosis[6].
In vivo, in a mouse model of acute lung injury induced by Pseudomonas aeruginosa (PA103) or exotoxin A (Exo-A), a single administration of BOS-318 (5mM; i.p.; 200µL; and 0.874mM; intratracheal; 50µL) 1 hour prior to infection significantly improved survival at 96 hours post-infection, attenuated hypothermia and body weight loss, reduced protein and inflammatory cytokine levels in bronchoalveolar lavage fluid (BALF), and accelerated bacterial clearance[7]. In adult C57BL/6 mice, a single oral dose of BOS-318 (10mg/kg) administered 24 hours before electrophysiological experiments. BOS-318 significantly inhibited furin activity in tissues and prevented the PAR1 agonist TFLLR-NH2-induced potentiation of neuromuscular transmission[8].
References:
[1] Douglas LEJ, Reihill JA, Martin SL. BOS-318 treatment enhances elexacaftor-tezacaftor-ivacaftor-mediated improvements in airway hydration and mucociliary transport. ERJ Open Res. 2025 Feb 25;11(1):00445-2024.
[2] Nayak D, Wasmuth EV, Olsen SK. Clearing the air: Uniquely engaging furin as an approach to cystic fibrosis therapy. Cell Chem Biol. 2022 Jun 16;29(6):927-929.
[3] Ducrocq GP, Anselmi L, Stella SL Jr, et al. Inhibition and potentiation of the exercise pressor reflex by pharmacological modulation of TRPC6 in male rats. J Physiol. 2025 Sep;603(18):5027-5052.
[4] Ridgway H, Orbell JD, Matsoukas MT, et al. W254 in furin functions as a molecular gate promoting anti-viral drug binding: Elucidation of putative drug tunneling and docking by non-equilibrium molecular dynamics. Comput Struct Biotechnol J. 2023 Sep 9;21:4589-4612.
[5] Douglas LEJ, Reihill JA, Ho MWY, 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.
[6] Marchese M, La Regina G, Amato R, et al. The unexplored mechanism of antitumoral effect of pirfenidone in melanoma cells. Sci Rep. 2025 Aug 1;15(1):28071.
[7] Bernard O, Kwon M, Looney MR, et al. Furin Inhibition Protects Against Acute Lung Injury in a Mouse Model of Pseudomonas Aeruginosa Infection. Am J Respir Cell Mol Biol. 2026 Feb 15:aanag024.
[8] Molchanova, A.I., Shepelev, E.I., Gaydukov, A.E. PAR1-Mediated Retrograde Action of Brain-Derived Neurotrophic Factor and Its Prodomain in Mature Mouse Motor Synapses is Provided by Furin Activity. Neurochem J. 2025; 19: 717–727.
| Cell experiment [1]: | |
Cell lines | A375M6 and M21 human BRAF-mutated melanoma cell lines |
Preparation Method | Melanoma cells were cultured in DMEM supplemented with 10% FBS. Cells were exposed to BOS-318 (5nM) and/or pirfenidone (PFD) for 24 hours in complete standard medium. |
Reaction Conditions | 5μM; 24h. |
Applications | BOS-318 treatment reduced the expression of TGFβ1 and phospho-SMAD2. When combined with pirfenidone (8.1mM), BOS-318 synergistically increased p21 expression and raised the proportion of cells entering late apoptosis. |
| Animal experiment [2]: | |
Animal models | Adult C57BL/6 mice of both sexes |
Preparation Method | Mice were administered a single oral dose of BOS-318 (10mg/kg) 24 hours before electrophysiological experiments. Administration was performed by voluntary swallowing using a standard replaceable tip and an automatic pipette, with a maximum volume of 100µL of the solution. |
Dosage form | 10mg/kg; oral administration; single dose. |
Applications | Oral administration of BOS-318 significantly inhibited furin activity in tissues and prevented the PAR1 agonist TFLLR-NH2-induced potentiation of neuromuscular transmission. |
References: | |
| Cas No. | 2387633-15-8 | SDF | |
| Formula | C28H32Cl2N6O3 | M.Wt | 571.5 |
| Solubility | DMSO : 50 mg/mL (87.49 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7498 mL | 8.7489 mL | 17.4978 mL |
| 5 mM | 350 μL | 1.7498 mL | 3.4996 mL |
| 10 mM | 175 μL | 874.9 μL | 1.7498 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)