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Cathepsin S inhibitorBlocks MHCII antigen presentation

Cathepsin S inhibitor

Catalog No. A3284
Size Price Stock Qty
10mM (in 1mL DMSO) $250.00 In stock
5mg $212.00 In stock
10mg $275.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Steimle A, Gronbach K, et al. "Symbiotic gut commensal bacteria act as host cathepsin S activity regulators." J Autoimmun. 2016 Jul 30. PMID:27484364

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Chemical structure

Cathepsin S inhibitor

Biological Activity

A slow, tight-binding reversible inhibitor of recombinant cathepsin S (Ki = 185 pM). Exhibits about 410-fold greater selectivity for cathepsin S compared to cathepsin B (Ki = 76 nM).
Targets cathepsin S          
Ki 185pM          

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Chemical Properties

Cas No. 1373215-15-6 SDF Download SDF
Chemical Name [(3R,4S)-4-[(4-fluorobenzoyl)amino]-6-[4-(oxetan-3-yl)piperazin-1-yl]-3,4-dihydro-2H-chromen-3-yl] N-methylcarbamate
Formula C25H29FN4O5 M.Wt 484.52
Solubility >24.3mg/mL in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request


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].

[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.