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CA-074 is a potent, highly selective, and irreversible inhibitor of cathepsin B, a lysosomal cysteine protease. Originally developed by Nobuhiko Katunuma's group at Tokushima University, CA-074 is an epoxysuccinyl peptide derivative designed based on the structure of E-64. It selectively targets the active site of cathepsin B with nanomolar potency (Ki of 2–5 nM), showing several thousand-fold selectivity over other cysteine cathepsins such as cathepsin H, L, and S. CA-074 is widely utilized as a research tool to investigate the role of cathepsin B in various physiological and pathological processes, including lysosomal protein degradation, autophagy, antigen presentation, tumor invasion, metastasis, and neurodegenerative diseases like Alzheimer's disease.
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