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PRDX1-IN-1 is a potent and selective small-molecule inhibitor of Peroxiredoxin 1 (PRDX1), an antioxidant enzyme that is frequently overexpressed in various cancers and plays a role in maintaining redox homeostasis. Derived from celastrol-ligustrazine hybrid chemistry, the compound has an IC50 of 0.164 μM against PRDX1. By inhibiting the antioxidant activity of PRDX1, PRDX1-IN-1 promotes the intracellular accumulation of reactive oxygen species (ROS), which leads to the induction of apoptosis and the inhibition of cancer cell proliferation, migration, and invasion. Preclinical research has explored its potential in models of breast, esophageal, lung, and clear cell renal cell carcinoma. It is currently utilized primarily as a research reagent to study PRDX1 biology and as a lead compound for anticancer drug development.
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