Cathepsin S inhibitor

Short Summary : Blocks MHCII antigen presentation

Category : Proteases|Cathepsin

Purity : 0.98

CAS Number : 1373215-15-6

Formula : C25H29FN4O5

Molecular Weight : 484.52

SMILE : CNC(=O)OC1COC2=C(C1NC(=O)C3=CC=C(C=C3)F)C=C(C=C2)N4CCN(CC4)C5COC5

Solubility : >24.3mg/mL in DMSO

Storage : Store at -20°C

Description : Ki: 0.185 nM Cathepsin S is a lysosomal cysteine protease, playing an important role in antigen presentation. The inhibition of Cathepsin S is expected to result in immunosuppression, which makes this enzyme an attractive target to potentially treat autoimmune and inflammatory diseases. Cathepsin S inhibitor is a novel Cathepsin S inhibitor. In vitro: Cathepsin S inhibitor was a slow, tight-binding reversible inhibitor of recombinant cathepsin S, exhibiting greater selectivity for cathepsin S compared to cathepsin B [1]. In vivo: No animal in vivo data available currently Clinical trial: Oral Cathepsin S inhibitor that blocked MHCII antigen presentation could result in a T-cell-selective immunosuppressant agent with improved safety over the current standard of care for the treatment of rheumatoid arthritis, psoriasis, multiple sclerosis and other autoimmune-based inflammatory diseases [2].References:[1] Wiener JJ, Sun S, Thurmond RL. Recent advances in the design of cathepsin S inhibitors. Curr Top Med Chem. 2010;10(7):717-32.[2] Lee-Dutra A, Wiener DK, Sun S. Cathepsin S inhibitors: 2004-2010. Expert Opin Ther Pat. 2011;21(3):311-37.

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