Ferroptosis

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Ferroptosis Products

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Catalog No. Product Name Information Product Use Citations Product Validations
S1077 SB202190 (FHPI) SB202190 (FHPI) is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo. SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. SB202190 significantly suppresses Erastin‐dependent ferroptosis.
Cell Res, 2022, 10.1038/s41422-022-00614-0
Nat Commun, 2022, 13(1):791
Front Immunol, 2022, 13:840510
S1443 Zileuton (A-64077) Zileuton (A-64077, Abbott 64077, ZYFLO) is an orally active inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes (LTB4, LTC4, LTD4, and LTE4) formation, used to decrease the symptoms of asthma. Zileuton induces apoptosis while inhibits ferroptosis.
J Exp Clin Cancer Res, 2021, 40(1):344
Front Microbiol, 2020, 11:845
Front Immunol, 2019, 10:1904
S1623 Acetylcysteine (N-acetylcysteine) Acetylcysteine (N-acetyl-l-cysteine, NAC) is a ROS(reactive oxygen species) inhibitor that antagonizes the activity of proteasome inhibitors. It is also a tumor necrosis factor production inhibitor. Acetylcysteine(N-acetyl-l-cysteine) suppresses TNF-induced NF-κB activation through inhibition of IκB kinases. Acetylcysteine(N-acetyl-l-cysteine) induces apoptosis via the mitochondria-dependent pathway. Acetylcysteine(N-acetyl-l-cysteine) inhibits ferroptosis and virus replication.Solutions of Acetylcysteine are best fresh-prepared.
EMBO Mol Med, 2022, 14(2):e14903
J Exp Clin Cancer Res, 2022, 41(1):41
J Nanobiotechnology, 2022, 20(1):78
S1848 Curcumin Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM)and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on.
Adv Sci (Weinh), 2021, e2103360
Front Immunol, 2021, 12:656242
Aging (Albany NY), 2021, 13(10):13968-14000
S2046 Pioglitazone HCl Pioglitazone HCl (AD-4833, U-72107E) is an inhibitor of cytochrome P450 (CYP)2C8 and CYP3A4 enzymes. Pioglitazone HCl inhibits CYP2C8, CYP3A4 and CYP2C9 with Ki of 1.7 μM, 11.8 μM and 32.1 μM, respectively. Pioglitazone HCl is also a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist with EC50 of 0.93 μM and 0.99 μM for human PPARγ and mouse PPARγ, respectively. Pioglitazone HCl inhibits mitochondrial iron uptake, lipid peroxidation, and subsequent ferroptosis.
Commun Biol, 2022, 5(1):231
J Cell Mol Med, 2022, 10.1111/jcmm.17154
J Nanobiotechnology, 2021, 19(1):150
S2505 Rosiglitazone (BRL-49653) maleate Rosiglitazone maleate (BRL 49653), a member of the thiazolidinedione class of antihyperglycaemic agents, is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ (PPAR-γ) with IC50 of 42 nM. Rosiglitazone maleate also modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.
Cell Death Dis, 2021, 12(11):972
Antioxidants (Basel), 2021, 10(2)155
Front Cardiovasc Med, 2021, 8:698056
S2556 Rosiglitazone (BRL 49653) Rosiglitazone (BRL 49653) is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action. Rosiglitazone modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.
Redox Biol, 2022, 50:102256
Toxicology, 2022, 465:153048
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S3031 Linagliptin (BI-1356) Linagliptin (BI-1356) is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM and exhibits a 10,000-fold higher selectivity for DPP-4 than for other dipeptidyl peptidases such as DPP-2, DPP-8, and DPP-9. Linagliptin activates glomerular autophagy in a model of type 2 diabetes. DPP4 mediates ferroptosis in TP53-deficient CRC cells.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
S3984 Nordihydroguaiaretic acid (NDGA) Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis. Nordihydroguaiaretic acid (NDGA) inhibits p300 and activates autophagy. Nordihydroguaiaretic acid (NDGA) protects cells from ferroptosis.
S5742 Deferoxamine mesylate (Ba 33112) Deferoxamine mesylate (Ba 33112, Desferrioxamine B, DFOM, NSC 644468) is the mesylate salt of Deferoxamine, which forms iron complexes and is used as a chelating agent. Deferoxamine is a ferroptosis inhibitor that stabilizes HIF-1α expression and improves HIF-1α transactivity in hypoxic and hyperglycemic states in vitro. Deferoxamine decreases beta-amyloid (Aβ) deposition and induces autophagy.
Nat Cell Biol, 2022, 24(1):88-98
Nat Commun, 2022, 13(1):494
Bone Res, 2022, 10(1):26
S7171 Setanaxib (GKT137831) Setanaxib (GKT137831, GKT831) is a potent, dual NADPH oxidase NOX1/NOX4 inhibitor with Ki of 110 nM and 140 nM, respectively. Treatment with GKT137831 suppresses reactive oxygen species (ROS) production. GKT137831 partly inhibits ferroptosis.
Cell Chem Biol, 2022, S2451-9456(22)00127-1
Antioxidants (Basel), 2022, 11(3)513
Food Chem Toxicol, 2022, 163:112966
S7243 Ferrostatin-1 (Fer-1) Ferrostatin-1 (Fer-1) is a potent and selective inhibitor of ferroptosis with EC50 of 60 nM.
Signal Transduct Target Ther, 2022, 7(1):59
Nat Cell Biol, 2022, 24(1):88-98
Bone Res, 2022, 10(1):26
S7699 Liproxstatin-1 Liproxstatin-1 is a potent ferroptosis inhibitor with an IC50 of 22 nM.
Signal Transduct Target Ther, 2022, 7(1):59
Mol Cell, 2022, 82(5):920-932.e7
Cell Death Differ, 2022, 10.1038/s41418-022-00957-6
S8078 Bardoxolone Methyl Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor. Bardoxolone Methyl abrogates ferroptosis. Bardoxolone methyl induces apoptosis and autophagy in cancer cells.
Drug Des Devel Ther, 2021, 15:21-35
Cancers (Basel), 2020, 12(6):E1645
Antioxidants (Basel), 2020, 9(1)
S8432 Troglitazone (CS-045) Troglitazone (Rezulin, Romglizone, Prelay, CS045, Romozin) is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR) that is a ligand activated transcription factor regulating cell differentiation and growth. Troglitazone induces autophagy, apoptosis and necroptosis in bladder cancer cells. Troglitazone prevents RSL3-induced ferroptosis and lipid peroxidation in Pfa1 cells.
Free Radic Biol Med, 2021, 163:234-242
Biomed Pharmacother, 2020, 132:110741
Nat Commun, 2019, 11;10(1):4621
S8792 UAMC-3203 UAMC-3203 is an improved ferroptosis inhibitor with an IC50 value of 10 nM in IMR-32 neuroblastoma cells.
Shock, 2022, 57(3):344-350
J Mol Cell Cardiol, 2021, 150:65-76
J Mol Cell Cardiol, 2021, 150:65-76
S9839New SRS11-92 SRS11-92 (AA9), a Ferrostatin-1 (Fer-1) analogue, is a potent inhibitor of ferroptosis. SRS11-92 inhibits ferroptotic cell death induced by Erastin in HT-1080 human fibrosarcoma cells with EC50 of 6 nM.
S9840New SRS16-86 SRS16-86, a novel third-generation ferrostatin, is an inhibitor of ferroptosis.
E0375New Ammonium ferric citrate Ammonium ferric citrate (Ferric ammonium citrate, Ammonium iron(III) citrate, Iron ammonium citrate, FerriSeltz) induces ferroptosis in non-small-cell lung carcinoma through the inhibition of GPX4-GSS/GSR-GGT axis activity.
S0788 ML 210 ML-210 (CID 49766530) is a selective covalent inhibitor of cellular glutathione peroxidase 4 (GPX4) with EC50 of 0.04 μM and induces ferroptosis. ML-210 can selectively kill cells induced to express mutant RAS. ML-210 exhibits anti-cancer activity.
Prostate, 2022, 10.1002/pros.24308
Bioengineered, 2022, 13(2):2498-2512
Cancer Res, 2021, canres.0955.2021
S1007 Roxadustat (FG-4592) Roxadustat (FG-4592) is an HIF-α prolyl hydroxylase inhibitor in a cell-free assay, stabilizes HIF-2 and induces EPO production. Roxadustat potentiates RSL3 induced ferroptosis. Phase 3.
Front Immunol, 2022, 13:726153
Acta Physiol (Oxf), 2022, e13768
Eur J Med Chem, 2022, 230:114115
S1040 Sorafenib (BAY 43-9006) tosylate Sorafenib (BAY 43-9006) tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
Cancer Cell, 2022, S1535-6108(21)00662-0
Proc Natl Acad Sci U S A, 2022, 119(10):e2107453119
Cancer Metab, 2022, 10(1):4
S1166 Cisplatin (NSC 119875) Cisplatin (NSC 119875, Cisplatinum, cis-diamminedichloroplatinum II, CDDP, cis DDP, DDP) is an inorganic platinum complex, which is able to inhibit DNA synthesis by conforming DNA adducts in tumor cells. Cisplatin activates ferroptosis and induces autophagy. Solutions are best fresh-prepared.
Nat Immunol, 2022, 23(2):287-302
J Clin Invest, 2022, e147908
J Immunother Cancer, 2022, 10(3)e004129
S1576 Sulfasalazine (NSC 667219) Sulfasalazine (NSC 667219, Azulfidine, Salazopyrin, Sulphasalazine) is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy.
Cell Mol Life Sci, 2022, 79(5):228
Front Bioeng Biotechnol, 2022, 10:855755
Cell Metab, 2021, S1550-4131(21)00233-3
S1712 Deferasirox (ICL-670) Deferasirox (ICL-670, CGP-72670) is an iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor. Deferasirox-induced iron depletion promotes BclxL downregulation and cell death.
Cancer Res, 2022, canres.0218.2021
Br J Haematol, 2021, 192(4):747-760
J Transl Med, 2021, 19(1):347
S1792 Simvastatin (MK 733) Simvastatin (MK-0733, MK 733) is a competitive inhibitor of HMG-CoA reductase with Ki of 0.1-0.2 nM in cell-free assays. Simvastatin induces ferroptosis, mitophagy, autophagy and apoptosis.
PLoS Pathog, 2022, 18(4):e1010468
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
Theranostics, 2021, 11(4):1609-1625
S2111 Lapatinib (GW-572016) Lapatinib (GW-572016, GSK572016, GW2016), used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.
Cancer Discov, 2022, 12(1):204-219
Cell Metab, 2022, 34(1):90-105.e7
Nat Chem Biol, 2022, 10.1038/s41589-022-00984-x
S4452 ML162 ML162 is a covalent inhibitor of cellular phospholipid glutathione peroxidase (GPX-4) that induces ferroptosis.
S7242 Erastin Erastin is a ferroptosis activator by acting on mitochondrial VDAC, exhibiting selectivity for tumor cells bearing oncogenic RAS. Solutions of Erastin are best fresh-prepared.
Cell Metab, 2022, 34(1):90-105.e7
Signal Transduct Target Ther, 2022, 7(1):59
Nat Cell Biol, 2022, 24(1):88-98
S7309 BAY 87-2243 BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. BAY 87-2243 inhibits mitochondrial complex I activity, thus triggering a mitophagy-dependent ROS increase leading to necroptosis and ferroptosis. BAY 87-2243 exerts antitumor activity. Phase 1.
J Immunother Cancer, 2022, 10(3)e004414
Theranostics, 2021, 11(1):209-221
Cancer Lett, 2021, 529:19-36
S7397 Sorafenib (BAY 43-9006) Sorafenib (BAY 43-9006, NSC-724772) is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
Proc Natl Acad Sci U S A, 2022, 119(10):e2107453119
Cell Mol Life Sci, 2022, 79(5):228
Int J Mol Sci, 2022, 23(8)4277
S8155 RSL3 RSL3 ((1S,3R)-RSL3) is a ferroptosis activator in a VDAC-independent manner,exhibiting selectivity for tumor cells bearing oncogenic RAS. RSL3 binds, inactivates GPX4 and thus mediates GPX4-regulated ferroptosis.
Signal Transduct Target Ther, 2022, 7(1):59
Nat Cell Biol, 2022, 24(1):88-98
Mol Cell, 2022, 82(5):920-932.e7
S8254 FIN56 FIN56 is a specific inducer of ferroptosis .
Mol Metab, 2022, 57:101436
EMBO Mol Med, 2021, e13792
Autophagy, 2021, 10.1080/15548627.2021.2008692
S8661 CA3 (CIL56) CA3 (CIL56) has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties. CA3(CIL56) induces ferroptosis and iron-dependent reactive oxygen species (ROS).
Cell Rep, 2022, 38(7):110390
Sci Rep, 2022, 12(1):45
Cancers (Basel), 2021, 13(21)5474
S9663 iFSP1 iFSP1 is a potent, selective and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1/AIFM2) with EC50 of 103 nM. iFSP1 selectively induces ferroptosis in GPX4-knockout Pfa1 and HT1080 cells that overexpresses FSP1.
S8790 ML385 ML385 is a novel and specific NRF2 inhibitor with an IC50 of 1.9 μM. It inhibits the downstream target gene expression of NRF2. NRF2 regulates the activity of several ferroptosis and lipid peroxidation-related proteins.
Oxid Med Cell Longev, 2022, 2022:2949824
Oxid Med Cell Longev, 2022, 2022:3990607
Cells, 2022, 11(7)1230
S8877 Imidazole ketone erastin (PUN30119) Imidazole ketone erastin (PUN30119, IKE) is a potent, selective, and metabolically stable system xc– inhibitor and inducer of ferroptosis.
J Exp Clin Cancer Res, 2022, 41(1):79
Free Radic Biol Med, 2022, 181:288-299
Pharmacol Res, 2022, 177:106122
E1063New Piperazine Erastin Piperazine Erastin is an analog of Erastin, which can induces ferroptosis in cancer cells, an iron-dependent form of nonapoptotic cell death.
S1077 SB202190 (FHPI) SB202190 (FHPI) is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo. SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. SB202190 significantly suppresses Erastin‐dependent ferroptosis.
Cell Res, 2022, 10.1038/s41422-022-00614-0
Nat Commun, 2022, 13(1):791
Front Immunol, 2022, 13:840510
S1443 Zileuton (A-64077) Zileuton (A-64077, Abbott 64077, ZYFLO) is an orally active inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes (LTB4, LTC4, LTD4, and LTE4) formation, used to decrease the symptoms of asthma. Zileuton induces apoptosis while inhibits ferroptosis.
J Exp Clin Cancer Res, 2021, 40(1):344
Front Microbiol, 2020, 11:845
Front Immunol, 2019, 10:1904
S1623 Acetylcysteine (N-acetylcysteine) Acetylcysteine (N-acetyl-l-cysteine, NAC) is a ROS(reactive oxygen species) inhibitor that antagonizes the activity of proteasome inhibitors. It is also a tumor necrosis factor production inhibitor. Acetylcysteine(N-acetyl-l-cysteine) suppresses TNF-induced NF-κB activation through inhibition of IκB kinases. Acetylcysteine(N-acetyl-l-cysteine) induces apoptosis via the mitochondria-dependent pathway. Acetylcysteine(N-acetyl-l-cysteine) inhibits ferroptosis and virus replication.Solutions of Acetylcysteine are best fresh-prepared.
EMBO Mol Med, 2022, 14(2):e14903
J Exp Clin Cancer Res, 2022, 41(1):41
J Nanobiotechnology, 2022, 20(1):78
S1848 Curcumin Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM)and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on.
Adv Sci (Weinh), 2021, e2103360
Front Immunol, 2021, 12:656242
Aging (Albany NY), 2021, 13(10):13968-14000
S2046 Pioglitazone HCl Pioglitazone HCl (AD-4833, U-72107E) is an inhibitor of cytochrome P450 (CYP)2C8 and CYP3A4 enzymes. Pioglitazone HCl inhibits CYP2C8, CYP3A4 and CYP2C9 with Ki of 1.7 μM, 11.8 μM and 32.1 μM, respectively. Pioglitazone HCl is also a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist with EC50 of 0.93 μM and 0.99 μM for human PPARγ and mouse PPARγ, respectively. Pioglitazone HCl inhibits mitochondrial iron uptake, lipid peroxidation, and subsequent ferroptosis.
Commun Biol, 2022, 5(1):231
J Cell Mol Med, 2022, 10.1111/jcmm.17154
J Nanobiotechnology, 2021, 19(1):150
S2505 Rosiglitazone (BRL-49653) maleate Rosiglitazone maleate (BRL 49653), a member of the thiazolidinedione class of antihyperglycaemic agents, is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ (PPAR-γ) with IC50 of 42 nM. Rosiglitazone maleate also modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.
Cell Death Dis, 2021, 12(11):972
Antioxidants (Basel), 2021, 10(2)155
Front Cardiovasc Med, 2021, 8:698056
S2556 Rosiglitazone (BRL 49653) Rosiglitazone (BRL 49653) is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action. Rosiglitazone modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.
Redox Biol, 2022, 50:102256
Toxicology, 2022, 465:153048
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S3031 Linagliptin (BI-1356) Linagliptin (BI-1356) is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM and exhibits a 10,000-fold higher selectivity for DPP-4 than for other dipeptidyl peptidases such as DPP-2, DPP-8, and DPP-9. Linagliptin activates glomerular autophagy in a model of type 2 diabetes. DPP4 mediates ferroptosis in TP53-deficient CRC cells.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
S3984 Nordihydroguaiaretic acid (NDGA) Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis. Nordihydroguaiaretic acid (NDGA) inhibits p300 and activates autophagy. Nordihydroguaiaretic acid (NDGA) protects cells from ferroptosis.
S5742 Deferoxamine mesylate (Ba 33112) Deferoxamine mesylate (Ba 33112, Desferrioxamine B, DFOM, NSC 644468) is the mesylate salt of Deferoxamine, which forms iron complexes and is used as a chelating agent. Deferoxamine is a ferroptosis inhibitor that stabilizes HIF-1α expression and improves HIF-1α transactivity in hypoxic and hyperglycemic states in vitro. Deferoxamine decreases beta-amyloid (Aβ) deposition and induces autophagy.
Nat Cell Biol, 2022, 24(1):88-98
Nat Commun, 2022, 13(1):494
Bone Res, 2022, 10(1):26
S7171 Setanaxib (GKT137831) Setanaxib (GKT137831, GKT831) is a potent, dual NADPH oxidase NOX1/NOX4 inhibitor with Ki of 110 nM and 140 nM, respectively. Treatment with GKT137831 suppresses reactive oxygen species (ROS) production. GKT137831 partly inhibits ferroptosis.
Cell Chem Biol, 2022, S2451-9456(22)00127-1
Antioxidants (Basel), 2022, 11(3)513
Food Chem Toxicol, 2022, 163:112966
S7243 Ferrostatin-1 (Fer-1) Ferrostatin-1 (Fer-1) is a potent and selective inhibitor of ferroptosis with EC50 of 60 nM.
Signal Transduct Target Ther, 2022, 7(1):59
Nat Cell Biol, 2022, 24(1):88-98
Bone Res, 2022, 10(1):26
S7699 Liproxstatin-1 Liproxstatin-1 is a potent ferroptosis inhibitor with an IC50 of 22 nM.
Signal Transduct Target Ther, 2022, 7(1):59
Mol Cell, 2022, 82(5):920-932.e7
Cell Death Differ, 2022, 10.1038/s41418-022-00957-6
S8078 Bardoxolone Methyl Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor. Bardoxolone Methyl abrogates ferroptosis. Bardoxolone methyl induces apoptosis and autophagy in cancer cells.
Drug Des Devel Ther, 2021, 15:21-35
Cancers (Basel), 2020, 12(6):E1645
Antioxidants (Basel), 2020, 9(1)
S8432 Troglitazone (CS-045) Troglitazone (Rezulin, Romglizone, Prelay, CS045, Romozin) is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR) that is a ligand activated transcription factor regulating cell differentiation and growth. Troglitazone induces autophagy, apoptosis and necroptosis in bladder cancer cells. Troglitazone prevents RSL3-induced ferroptosis and lipid peroxidation in Pfa1 cells.
Free Radic Biol Med, 2021, 163:234-242
Biomed Pharmacother, 2020, 132:110741
Nat Commun, 2019, 11;10(1):4621
S8792 UAMC-3203 UAMC-3203 is an improved ferroptosis inhibitor with an IC50 value of 10 nM in IMR-32 neuroblastoma cells.
Shock, 2022, 57(3):344-350
J Mol Cell Cardiol, 2021, 150:65-76
J Mol Cell Cardiol, 2021, 150:65-76
S9839New SRS11-92 SRS11-92 (AA9), a Ferrostatin-1 (Fer-1) analogue, is a potent inhibitor of ferroptosis. SRS11-92 inhibits ferroptotic cell death induced by Erastin in HT-1080 human fibrosarcoma cells with EC50 of 6 nM.
S9840New SRS16-86 SRS16-86, a novel third-generation ferrostatin, is an inhibitor of ferroptosis.
E0375New Ammonium ferric citrate Ammonium ferric citrate (Ferric ammonium citrate, Ammonium iron(III) citrate, Iron ammonium citrate, FerriSeltz) induces ferroptosis in non-small-cell lung carcinoma through the inhibition of GPX4-GSS/GSR-GGT axis activity.
S0788 ML 210 ML-210 (CID 49766530) is a selective covalent inhibitor of cellular glutathione peroxidase 4 (GPX4) with EC50 of 0.04 μM and induces ferroptosis. ML-210 can selectively kill cells induced to express mutant RAS. ML-210 exhibits anti-cancer activity.
Prostate, 2022, 10.1002/pros.24308
Bioengineered, 2022, 13(2):2498-2512
Cancer Res, 2021, canres.0955.2021
S1007 Roxadustat (FG-4592) Roxadustat (FG-4592) is an HIF-α prolyl hydroxylase inhibitor in a cell-free assay, stabilizes HIF-2 and induces EPO production. Roxadustat potentiates RSL3 induced ferroptosis. Phase 3.
Front Immunol, 2022, 13:726153
Acta Physiol (Oxf), 2022, e13768
Eur J Med Chem, 2022, 230:114115
S1040 Sorafenib (BAY 43-9006) tosylate Sorafenib (BAY 43-9006) tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
Cancer Cell, 2022, S1535-6108(21)00662-0
Proc Natl Acad Sci U S A, 2022, 119(10):e2107453119
Cancer Metab, 2022, 10(1):4
S1166 Cisplatin (NSC 119875) Cisplatin (NSC 119875, Cisplatinum, cis-diamminedichloroplatinum II, CDDP, cis DDP, DDP) is an inorganic platinum complex, which is able to inhibit DNA synthesis by conforming DNA adducts in tumor cells. Cisplatin activates ferroptosis and induces autophagy. Solutions are best fresh-prepared.
Nat Immunol, 2022, 23(2):287-302
J Clin Invest, 2022, e147908
J Immunother Cancer, 2022, 10(3)e004129
S1576 Sulfasalazine (NSC 667219) Sulfasalazine (NSC 667219, Azulfidine, Salazopyrin, Sulphasalazine) is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy.
Cell Mol Life Sci, 2022, 79(5):228
Front Bioeng Biotechnol, 2022, 10:855755
Cell Metab, 2021, S1550-4131(21)00233-3
S1712 Deferasirox (ICL-670) Deferasirox (ICL-670, CGP-72670) is an iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor. Deferasirox-induced iron depletion promotes BclxL downregulation and cell death.
Cancer Res, 2022, canres.0218.2021
Br J Haematol, 2021, 192(4):747-760
J Transl Med, 2021, 19(1):347
S1792 Simvastatin (MK 733) Simvastatin (MK-0733, MK 733) is a competitive inhibitor of HMG-CoA reductase with Ki of 0.1-0.2 nM in cell-free assays. Simvastatin induces ferroptosis, mitophagy, autophagy and apoptosis.
PLoS Pathog, 2022, 18(4):e1010468
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
Theranostics, 2021, 11(4):1609-1625
S2111 Lapatinib (GW-572016) Lapatinib (GW-572016, GSK572016, GW2016), used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.
Cancer Discov, 2022, 12(1):204-219
Cell Metab, 2022, 34(1):90-105.e7
Nat Chem Biol, 2022, 10.1038/s41589-022-00984-x
S4452 ML162 ML162 is a covalent inhibitor of cellular phospholipid glutathione peroxidase (GPX-4) that induces ferroptosis.
S7242 Erastin Erastin is a ferroptosis activator by acting on mitochondrial VDAC, exhibiting selectivity for tumor cells bearing oncogenic RAS. Solutions of Erastin are best fresh-prepared.
Cell Metab, 2022, 34(1):90-105.e7
Signal Transduct Target Ther, 2022, 7(1):59
Nat Cell Biol, 2022, 24(1):88-98
S7309 BAY 87-2243 BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. BAY 87-2243 inhibits mitochondrial complex I activity, thus triggering a mitophagy-dependent ROS increase leading to necroptosis and ferroptosis. BAY 87-2243 exerts antitumor activity. Phase 1.
J Immunother Cancer, 2022, 10(3)e004414
Theranostics, 2021, 11(1):209-221
Cancer Lett, 2021, 529:19-36
S7397 Sorafenib (BAY 43-9006) Sorafenib (BAY 43-9006, NSC-724772) is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
Proc Natl Acad Sci U S A, 2022, 119(10):e2107453119
Cell Mol Life Sci, 2022, 79(5):228
Int J Mol Sci, 2022, 23(8)4277
S8155 RSL3 RSL3 ((1S,3R)-RSL3) is a ferroptosis activator in a VDAC-independent manner,exhibiting selectivity for tumor cells bearing oncogenic RAS. RSL3 binds, inactivates GPX4 and thus mediates GPX4-regulated ferroptosis.
Signal Transduct Target Ther, 2022, 7(1):59
Nat Cell Biol, 2022, 24(1):88-98
Mol Cell, 2022, 82(5):920-932.e7
S8254 FIN56 FIN56 is a specific inducer of ferroptosis .
Mol Metab, 2022, 57:101436
EMBO Mol Med, 2021, e13792
Autophagy, 2021, 10.1080/15548627.2021.2008692
S8661 CA3 (CIL56) CA3 (CIL56) has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties. CA3(CIL56) induces ferroptosis and iron-dependent reactive oxygen species (ROS).
Cell Rep, 2022, 38(7):110390
Sci Rep, 2022, 12(1):45
Cancers (Basel), 2021, 13(21)5474
S9663 iFSP1 iFSP1 is a potent, selective and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1/AIFM2) with EC50 of 103 nM. iFSP1 selectively induces ferroptosis in GPX4-knockout Pfa1 and HT1080 cells that overexpresses FSP1.
S8790 ML385 ML385 is a novel and specific NRF2 inhibitor with an IC50 of 1.9 μM. It inhibits the downstream target gene expression of NRF2. NRF2 regulates the activity of several ferroptosis and lipid peroxidation-related proteins.
Oxid Med Cell Longev, 2022, 2022:2949824
Oxid Med Cell Longev, 2022, 2022:3990607
Cells, 2022, 11(7)1230
S8877 Imidazole ketone erastin (PUN30119) Imidazole ketone erastin (PUN30119, IKE) is a potent, selective, and metabolically stable system xc– inhibitor and inducer of ferroptosis.
J Exp Clin Cancer Res, 2022, 41(1):79
Free Radic Biol Med, 2022, 181:288-299
Pharmacol Res, 2022, 177:106122
S9839New SRS11-92 SRS11-92 (AA9), a Ferrostatin-1 (Fer-1) analogue, is a potent inhibitor of ferroptosis. SRS11-92 inhibits ferroptotic cell death induced by Erastin in HT-1080 human fibrosarcoma cells with EC50 of 6 nM.
S9840New SRS16-86 SRS16-86, a novel third-generation ferrostatin, is an inhibitor of ferroptosis.
E0375New Ammonium ferric citrate Ammonium ferric citrate (Ferric ammonium citrate, Ammonium iron(III) citrate, Iron ammonium citrate, FerriSeltz) induces ferroptosis in non-small-cell lung carcinoma through the inhibition of GPX4-GSS/GSR-GGT axis activity.
E1063New Piperazine Erastin Piperazine Erastin is an analog of Erastin, which can induces ferroptosis in cancer cells, an iron-dependent form of nonapoptotic cell death.