RR-11a

RR-11a is a synthetic, cell-permeable, and irreversible aza-peptide Michael acceptor that acts as a potent and selective inhibitor of legumain (also known as asparaginyl endopeptidase, AEP, or δ-secretase). It covalently binds to the catalytic cysteine residue (Cys189) of legumain, blocking its proteolytic activity without affecting closely related proteases such as caspases. RR-11a is widely utilized as a preclinical research tool to investigate the role of legumain in various pathological conditions, including cancer, Alzheimer's disease, acute kidney injury, myocardial infarction, pulmonary fibrosis, and osteoporosis. In oncology research, RR-11a has also been employed as a targeting ligand conjugated to nanoparticles for tumor-specific drug delivery under hypoxic conditions.

Other names

2,5-dioxopyrrolidin-1-yl (E)-4-(1-(2-amino-2-oxoethyl)-2-(((benzyloxy)carbonyl)-L-alanyl-L-alanyl)hydrazineyl)-4-oxobut-2-enoateRR-11a analogRR11a analogRR 11a analogaza-peptide Michael acceptor, 7a