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This study adds thiolactones to the collection of cascade exchangers (CAXs) and reports with dynamic covalent Michael acceptor dimers the first CAXs that rather inhibit than enable thiol‐mediated uptake. The superior performance of dimers compared to monomeric Michael acceptors as inhibitors might suggest that top inhibitors move along thiol/ate arrays without losing covalent contact, while cell penetrators...
Thiol‐mediated uptake is emerging as method of choice to penetrate cells. This study focuses on irreversible covalent inhibitors of thiol‐mediated uptake. High‐content high‐throughput screening of the so far largest collection of hypervalent iodine reagents affords inhibitors that are more than 250 times more active than Ellman’s reagent and rival the best dynamic covalent inhibitors. Comparison with...
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