KSC-34, a covalent modifier of protein disulfide isomerase A1 (PDIA1) , is also a selective and potent a-site inhibitor of PDIA1 with an IC 50 of 3.5 μM. KSC-34 displays a 30-fold selectivity for a domain over a′ domain and displays high selectivity for PDIA1 in complex proteomes with minimal engagement of other members of the PDI family. KSC-34 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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