| Bioactivity | Cathepsin C-IN-5 (compound SF38) is a potent, selective and orally active Cathepsin C inhibitor with IC50s of 59.9 nM, 4.26 µM, >5 µM, >5 µM, >5 µM for Cat C, Cat L, Cat S, Cat B, Cat K, respectively. Cathepsin C-IN-5 inhibits the Cat C activity in bone marrow and blood. Cathepsin C-IN-5 decreases the activation of NSPs (neutrophil serine proteases). Cathepsin C-IN-5 shows anti-inflammatory activity[1]. |
| Target | IC50: 59.9 nM (Cat C); 4.26 µM (Cat L); >5 µM (Cat S); >5 µM (Cat B); >5 µM (Cat K) |
| Invitro | Cathepsin C-IN-5 (compound SF38) shows inhibition in THP-1 and U937 cells with IC50s of 115.4, 70.2 nM, respectively[1]. |
| In Vivo | Cathepsin C-IN-5 (1500 mg/kg) shows no significant weight loss or toxic reaction within 7 days after the administration in ICR mice[1].Cathepsin C-IN-5 (10 mg/kg for p.o.; 2 mg/kg for i.v.) shows good bioavailability with F=42.07%[1].Cathepsin C-IN-5 (2, 10, 50 mg/kg; p.o.) shows effective antiinflammatory activity and potential protective effect in an animal model of ALI[1]. Animal Model: |
| Name | Cathepsin C-IN-5 |
| CAS | 2825567-97-1 |
| Formula | C21H17ClN6OS |
| Molar Mass | 436.92 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| Reference | [1]. Chen X, et al. Non-peptidyl non-covalent cathepsin C inhibitoEEr bearing a unique thiophene-substituted pyridine: Design, structure-activity relationship and anti-inflammatory activity in vivo. Eur J Med Chem. 2022 Jun 5;236:114368. |