Table 2.

Commercially available PDI inhibitors.

Inhibitor	Chemical name	IC50 (μM)	PDI members	PDI inhibition activity	Membrane permeable reversibility	Refs.
35G8	1,3,6-Trimethylpyrimido [5,4-e] [1,2,4] triazine-5,7-dione	0.17	PDIA1	Induces Nrf2 antioxidant response, endoplasmic reticulum stress response, autophagy, and may induce cell death via ferroptosis	Cell permeable	Kyani et al. (2018)
E64FC26	(lE)-1-nonylidene-3-(trifluoromethyl) indene-5,6-diol	1.9 20.9 25.9 16.3 25.4	PDIA1 PDIA3 PDIA4, TXNDC5 PDIA6	anti-myeloma activity	Cell permeable	Robinson et al. (2019)
PACMA 31	N-(2,4-Dimethoxyphenyl)-N-(1-oxo-2-propyn-1-yl)-2-(2-thienyl) glycyl-glycine ethyl ester	10	PDIA1	Cytotoxic in ovarian cancer cells	Cell permeable irreversible	Xu et al. (2012)
Bacitracin	Commercial bacitracin is a mixture of at least 22 structurally related peptides.	150	PDIA1	Inhibits cell death through enhanced apoptosis in melanoma cells	Cell permeable reversible	Karala and Ruddock (2010)
16F16	2-(2-Cbloroacetyl)-2,3,4,9-tetrahydro-1-methyl-1H-pyrido [3,4-b] indole-1-carboxylic acid methyl ester, Methyl 2-(2-chloroacetyl)-1-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b] indole-1-carboxylate	63	PDIA1 PDIA3	Inhibits apoptosis in PC12 cell model of HD	Cell permeable irreversible	Kaplan et al. (2015)
P1	N-[(1,1-Dimethylethoxy)carbonyl]-l-phenylalanyl-O-(ethenylsulfonyl) -N-4-pentyn-1-yl-l-tyrosinamide	1.7	PDIA1	Inhibits proliferation of MCF7, MDA-MB-231, HepG2 and UACC257 and T47D	Cell permeable irreversible	Ge et al. (2013)
CCF 642	Spyietqlovdjcf-xyokqwhbsa-n	2.9	PDIA1	Induce apoptosis and cytotoxic effects in multiple myeloma cells	Cell permeable irreversible	Vatolin et al. (2016)
LOC14	2-((4-(Cyclopropanecarbonyl)piperazin-1-yl) methyl) benzo[d]isothiazol-3(2H-f)-one, 2-((4-(Cyclopropylcarb onyl)-1-piperazinyl) methyl)-1,2-benzothiazol-3 (2H)-one	0.5	PDIA3	Antiapoptotic neuroprotective	Cell permeable reversible	Kaplan, et al. (2015); O’Sullivanet al. (2022)
BAP2	(E)-3-(3-(4-Hydroxyphenyl)-3-oxoprop-1-en-1-yl)benzonitrile	0.9	PDIA1 PDIA2	Inhibits tumor growth in glioblastoma	Cell permeable	Xu et al. (2019)
KSC-34	2-Chloro-N-[2-[[4-[methyl(4-phenylbutyl)amino]-6-(prop-2-ynylamino)-l,3,5-triazin-2-yl]amino]ethyl]acetamide	3.5	PDIA1	Reduce the extracellular pathogenic load of the amyloidogenic antibody light chain	Cell Permeable	Cole et al. (2018)