PDI-IN-2

PDI-IN-2 (compound 22) inhibits platelet surface PDI reductase activity with an IC₅₀ of 0.62 μM, matching the potency of Juglone (HY-N6949)^[1].
PDI-IN-2 inhibits recombinant human PDI reductase activity with an IC₅₀ of 0.63 μM, outperforming the parent compound juglone^[1].
PDI-IN-2 inhibits U46619-induced human platelet aggregation with an IC₅₀ of 1.54 μM, showing greater potency than juglone^[1].
PDI-IN-2 inhibits collagen-induced human platelet aggregation with an IC₅₀ of 0.50 μM, outperforming juglone^[1].
PDI-IN-2 (1-2 μM; up to 25 min) significantly inhibits tumor cell-induced platelet aggregation by A549, MDA-MB-231, and RPMI 8226 cells at concentrations of 1 μM and 2 μM^[1].
PDI-IN-2 shows selective inhibition of recombinant human PDI over ERp57 and ERp72, with IC₅₀ values of 3.24 μM for ERp57 and 4.01 μM for ERp72, which are 5.1-fold and 6.4-fold higher than its PDI IC₅₀^[1].
PDI-IN-2 (10 μM) exhibits reduced PDI inhibitory activity in the presence of 1 mM GSH, indicating it acts as a covalent PDI inhibitor susceptible to thiol competition^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.