Cathepsin C-IN-5

• CAT Number: I043612
• CAS Number: 2825567-97-1
• Molecular Formula: C21H17ClN6OS
• Molecular Weight: 436.92
• Purity: ≥95%
• Synonyms: N-[3-[[5-chloro-2-[(5-thiophen-3-ylpyridin-2-yl)amino]pyrimidin-4-yl]amino]phenyl]acetamide
• InChI: InChI=1S/C21H17ClN6OS/c1-13(29)25-16-3-2-4-17(9-16)26-20-18(22)11-24-21(28-20)27-19-6-5-14(10-23-19)15-7-8-30-12-15/h2-12H,1H3,(H,25,29)(H2,23,24,26,27,28)
• InChIKey: CVEIEBFUSJRUSP-UHFFFAOYSA-N
• SMILES: CC(=O)NC1=CC=CC(=C1)NC2=NC(=NC=C2Cl)NC3=NC=C(C=C3)C4=CSC=C4

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].
Cathepsin C-IN-5 (compound SF38) shows inhibition in THP-1 and U937 cells with IC50s of 115.4, 70.2 nM, respectively[1].
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].

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.
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