KEA1-97 targets lysine 72 of thioredoxin. It disrupts the interaction of thioredoxin with caspase 3, activates caspases, and induces apoptosis without affecting thioredoxin activity.

3-Methyltoxoflavin is a potent Protein disulfide isomerase (PDI) inhibitor, with an IC50 of 170 nM.

LOC14 is a high affinity protein disulfide isomerase (PDI) modulator with Kd of 62 nM.

CCF642 is a PDI-inhibiting compound with antimyeloma activity.

PX-12 is an irreversible thioredoxin-1 (Trx-1) inhibitor with antitumor activity.

TRi-1 is a potent, specific and irreversible TXNRD1 inhibitor with IC50 value of 12nM.

Aurothioglucose is a well known active-site inhibitor of TrxR1, inhibited TrxR1 activity in HeLa cell cytosol but had no effect on the viability of the cells.