Table 2.
Reagents that modulate ferroptosis
| Classification | Reagents | Targets | Impact on ferroptosis |
|---|---|---|---|
| Ferroptosis inducers | Sulphasalazine | System Xc- | Prevents cystine import, causes GSH depletion |
| Sorafenib | System Xc- | Prevents cystine import, causes GSH depletion | |
| Glutamate | System Xc- | Prevents cystine import, causes GSH depletion | |
| Erastin and its analogs | System Xc-, VDAC2/3 | Prevents cystine import, causes GSH depletion | |
| RSL3 | GPX4 | Covalent inhibitor of GPX4 that causes accumulation of lipid hydroperoxides |
|
| ML162 | GPX4 | Covalent inhibitor of GPX4 that causes accumulation of lipid hydroperoxides |
|
| FINO2 | GPX4 | Covalent inhibitor of GPX4 that causes accumulation of lipid hydroperoxides |
|
| FIN56 | CoQ10 and GPX4 | Depletes CoQ10 via SQS-mevalonate pathway and causes decrease in GPX4 protein abundance |
|
| BSO, DPI2, cisplatin | GHS | GHS deletion | |
| Statins (e.g., cerivastatin, simvastatin) | HMGCR | Blocks CoQ10 biosynthesis | |
| Trigonelline, brusatol | Nrf2 | Nrf2 inhibition | |
| Siramesine, lapatinib | Ferroportin, Transferrin | Upregulates cellular iron | |
| Brequinar | DHODH | Inhibits DHODH | |
| iFSP | FSP1 | Inhibits FSP1 | |
| BAY 87‐2243 | Mitochondrial respiratory chain | Inhibits mitochondrial respiratory chain | |
| Andrographolide | Lipid peroxidation | Promotes lipid peroxidation | |
| Toosendanin | Lipid peroxidation | Promotes lipid peroxidation | |
| Gliotoxin | ROS, lipid peroxidation | Promotes lipid peroxidation | |
| Arsenic trioxide | ACSL4 | ACSL4 activation | |
| Manganese | ROS, lipid peroxidation | Promotes lipid peroxidation | |
| Fatostatin | GPX4 | Inhibits GPX4 expression | |
| Legumain | GPX4 | Facilitates chaperone-mediated autophagy of GPX4 | |
| Dihydroartemisinin (DHA) | Ferritin, iron overload | Increases cellular iron | |
| Artemisinins | Iron overload | Increases cellular iron | |
| Ferroptosis inhibitors | Ferrostatin-1 | Lipid peroxidation | Blocks lipid peroxidation |
| Liproxstatin-1 | Lipid peroxidation | Blocks lipid peroxidation | |
| Vitamin E | Lipid peroxidation | Blocks lipid peroxidation | |
| SRS 16-86, SRS 11-92 | Lipid peroxidation | Blocks lipid peroxidation | |
| Troglitazone, Pioglitazone, Rosiglitazone | ACSL4 | ACSL4 inactivation | |
| Deuterated polyunsaturated fatty acids (D-PUFAs) | Lipid peroxidation | Blocks lipid peroxidation | |
| XJB-5-131 | Lipid peroxidation | Blocks lipid peroxidation | |
| Butylated hydroxytoluene, butylated hydroxyanisole |
Lipid peroxidation | Blocks lipid peroxidation | |
| Ferrostatins, liproxstatins | Lipid peroxidation | Blocks lipid peroxidation | |
| CDC, PD-146176, AA-861, zileuton | Lipoxygenases | Blocks lipid peroxidation | |
| Selenium | Selenoproteins | Blocks lipid peroxidation | |
| Deferoxamine, cyclipirox, deferiprone | Intracellular iron | Decreases cellular iron | |
| Vildagliptin, alogliptin, and Linagliptin | DPP4 | Blocks DPP4-mediated lipid peroxidation | |
| Irisin | GPX4 | Upregulates GPX4 | |
| Melatonin | System Xc- and GPX4 | Upregulates system Xc- and GPX4 | |
| Vitexin | System Xc- and GPX4 | Upregulates system Xc- and GPX4 | |
| Isoliquiritigenin | System Xc- and GPX4 | Upregulates system Xc- and GPX4 | |
| Vitamin A | Lipid peroxidation | Blocks lipid peroxidation | |
| Paricalcitol | GPX4 | Upregulates GPX4 | |
| Pachymic acid | Nrf2, GPX4, SCL7A11, and HO-1 | Upregulates of Nrf2, GPX4, SCL7A11 and HO-1 | |
| Rheb1 | Maintains mitochondrial homeostasis | Maintains mitochondrial homeostasis | |
| Quercetin | System Xc- and GPX4 | Upregulates system Xc- and GPX4 | |
| Artesunate | Lipoxygenases | Blocks lipid peroxidation | |
| Curcumin | Lipoxygenases | Blocks lipid peroxidation | |
| Baicalein | Lipoxygenases | Blocks lipid peroxidation | |
| Nuciferine | Lipoxygenases | Blocks lipid peroxidation | |
| Vitamin K | Lipid peroxidation | Blocks lipid peroxidation | |
| Cardamonin | Lipid peroxidation | Blocks lipid peroxidation | |
| Proanthocyanidins | Lipid peroxidation | Blocks lipid peroxidation | |
| Uridine | Lipid peroxidation | Blocks lipid peroxidation | |
| NDGA | Lipoxygenases | Blocks lipid peroxidation |