PDI-IN-1 is a cell-permeable PDI covalent inhibitor with an IC 50 of 1.7 μM against bovine PDI . PDI-IN-1 specifically modifies the Cys397 residue at the active site of human PDI , selectively labels endogenous PDI in living mammalian cancer cells, and effectively inhibits PDI-mediated insulin aggregation in vitro. PDI-IN-1 exhibits significant anti-tumor activity and inhibits the growth of various cancer cell lines.
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