Table 3.

Recently identified PDI inhibitors.

Inhibitor	Activity assay	IC50 (μM)	PDI members	In vitro	In vivo	Ref.
Aziridine-2-carboxylic acid derivatives	Insulin turbidity assay	0.6 1	PDIA1 PDIA3	HT-29 CaCo-2 cytotoxicity MCF-7 and MDA-MB-231 cell lines	In vivo in rat model of arterial thrombosis	Kurpinska et al. (2022); Zelencova-Gopejenko et al. (2023)
Piericones A Piericones B	Insulin turbidity assay	0.15 0.23	PDIA1 PDIA3 PDIA4 PDIA5	In vitro platelet aggregation and fibrin formation	In vivo thrombus formation	Zheng et al. (2023)
Galangin	Tryptophan fluorescence-based assay	5.9	PDIAl	N/A	Delayed the time of blood vessel occlusion in an electricity-induced mouse thrombosis model	Liang, et al. (2022)
Quercetin-3-rutinoside	Tryptophan displacement assay	0.43	PDIAl	Quercetin-3-rutinoside at 10μM effectively reduced chemotherapy-induced TF activity to its baseline	N/A	Beckmann et al. (2021); Liao et al. (2022)
tcyDTDO derivatives	Binding assay	N/A	PDIA1 PDIA10 PDIA17	DDAs disrupt disulfide bonding between PDIA1 and ERp44 and their client proteins	N/A	Law et al. (2022)
Origamicin	Protein disulfide isomerase activity assay	32.9	PDIA1	Induces oxidative stress response, downregulates MYC, and activates the p53 signaling pathway in neuroblastoma cells	N/A	Ozcelik and Pezacki (2019)
BAP2 derivatives	PDI reductase assay	0.12–11	PDIA1 PDIA2	Inhibit glioblastoma cell growth, induce ER stress, increase expression of G2M checkpoint proteins, and reduce expression of DNA repair proteins	N/A	Yang et al. (2019)