Ferroptosis

Ferroptosis Products

  • All (42)
  • Ferroptosis Inhibitors (21)
  • Ferroptosis Activators (18)
  • Ferroptosis Modulators (2)
  • New Ferroptosis Products
Catalog No. Product Name Information Product Use Citations Product Validations
S1166 Cisplatin Cisplatin 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 unstable and should be fresh-prepared.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation.
Nat Commun, 2024, 15(1):866
Clin Cancer Res, 2024, 30(1):187-197
Cancer Lett, 2024, 586:216695
S7397 Sorafenib Sorafenib 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.
Mol Cell, 2023, 83(5):803-818.e8
Adv Sci (Weinh), 2023, 10.1002/advs.202302025
Adv Sci (Weinh), 2023, 10(27):e2302025
S2111 Lapatinib Lapatinib, 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.
Nat Commun, 2023, 14(1):5035
Nat Commun, 2023, 10.1038/s41467-023-39059-3
Nat Commun, 2023, 14(1):3469
S7243 Fer-1 (Ferrostatin-1) Fer-1 (Ferrostatin-1) is a potent and selective inhibitor of ferroptosis with EC50 of 60 nM.
Nature, 2024, 626(7998):411-418.
Redox Biol, 2024, 69:103002
Cell Death Dis, 2024, 15(2):149
S7242 Erastin Erastin is a ferroptosis activator by acting on mitochondrial VDAC, exhibiting selectivity for tumor cells bearing oncogenic RAS. Solutions are unstable and should be fresh-prepared.
Nat Commun, 2024, 15(1):1429
Genome Biol, 2024, 25(1):58
Redox Biol, 2024, 69:103002
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.
Nature, 2024, 626(7998):411-418.
Nat Commun, 2024, 15(1):1429
Biomed Pharmacother, 2024, 171:116163
S1040 Sorafenib tosylate Sorafenib 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.
bioRxiv, 2024, 10.1101/2023.01.18.524628
Cell, 2023, S0092-8674(23)01032-2
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
S7699 Liproxstatin-1 Liproxstatin-1 is a potent ferroptosis inhibitor with an IC50 of 22 nM.
Nature, 2024, 626(7998):411-418.
Nat Commun, 2024, 15(1):1429
J Transl Med, 2024, 22(1):9
S1077 SB202190 SB202190 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 Rep Med, 2024, 5(2):101396
Theranostics, 2024, 14(4):1561-1582
Clin Transl Med, 2024, 14(2):e1583
S1623 Acetylcysteine (N-acetylcysteine) Acetylcysteine (N-acetyl-l-cysteine, NAC,N-acetylcysteine) 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 are unstable and should be fresh-prepared.
Cell Signal, 2024, 114:111004
Korean J Physiol Pharmacol, 2024, 28(1):21-30
Sci Adv, 2024, 10(3):eadi2012
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.
Cell Death Discov, 2024, 10(1):35
J Cell Mol Med, 2024, 28(2):e18055
Nat Commun, 2023, 14(1):6107
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.
Cell Rep, 2024, 43(1):113606.
Signal Transduct Target Ther, 2023, 10.1038/s41392-023-01578-2
Signal Transduct Target Ther, 2023, 8(1):355
S5742 Deferoxamine mesylate Deferoxamine mesylate 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.Please do not prepare stock solutions with normal saline or PBS, as precipitation may occur.
Redox Biol, 2024, 69:103008
Ecotoxicol Environ Saf, 2024, 270:115889
J Cancer, 2024, 15(3):685-698
S1792 Simvastatin Simvastatin 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.
Neuron, 2023, S0896-6273(23)00513-5
Cancer Res, 2023, 83(13):2248-2261
Cell Death Dis, 2023, 14(4):234
S2556 Rosiglitazone Rosiglitazone 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.
Nat Commun, 2024, 15(1):1429
J Hematol Oncol, 2023, 16(1):30
EBioMedicine, 2023, 10.1016/j.ebiom.2023.104865
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.
Immunity, 2024, 57(1):52-67.e10
Nat Commun, 2023, 14(1):1235
Theranostics, 2023, 13(9):2863-2878
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.
Mol Ther Nucleic Acids, 2023, 31:421-436
Mol Med, 2023, 29(1):91
Biomater Res, 2023, 27(1):11
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.
Nutrients, 2023, 15(3)740
Phytother Res, 2022, 36(3):1326-1337
Oncol Rep, 2022, 48(6)221
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).
Nat Commun, 2023, 14(1):6699
EMBO Mol Med, 2023, e17187.
Int J Nanomedicine, 2023, 18:2989-3006
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.
Nat Commun, 2023, 14(1):3648
Redox Biol, 2023, 60:102632
Cell Rep, 2023, 42(12):113431
S2505 Rosiglitazone maleate Rosiglitazone maleate, 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.
Stem Cell Reports, 2022, 17(11):2531-2547
Cell Death Dis, 2021, 12(11):972
Antioxidants (Basel), 2021, 10(2)155
S8254 FIN56 FIN56 is a specific inducer of ferroptosis .
Antioxidants (Basel), 2024, 13(1)114
J Hematol Oncol, 2023, 16(1):46
Exp Hematol Oncol, 2023, 12(1):47
S8877New IKE(Imidazole ketone erastin) IKE(Imidazole ketone erastin) is a potent, selective, and metabolically stable system xc– inhibitor and inducer of ferroptosis.
Nat Commun, 2023, 14(1):4758
Nat Commun, 2023, 14(1):4758
J Clin Invest, 2023, 133(10)e166647
S3031 Linagliptin (GSK2118436) Linagliptin (GSK2118436) 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.
Cell Death Dis, 2023, 10.1038/s41419-023-06240-x
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S1576 Sulfasalazine Sulfasalazine 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.
Adv Sci (Weinh), 2023, 10(20):e2300517
Proc Natl Acad Sci U S A, 2022, 119(36):e2117396119
Cell Mol Life Sci, 2022, 79(5):228
S1712 Deferasirox Deferasirox 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.
J Transl Med, 2023, 21(1):50
Cell Death Discov, 2023, 9(1):97
Cancer Discov, 2022, 12(9):2180-2197
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 Genet Genomics, 2022, S1673-8527(22)00133-3
J Cell Mol Med, 2022, 10.1111/jcmm.17154
S1443 Zileuton Zileuton 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.
Cancer Sci, 2023, 10.1111/cas.15994
Biomol Ther (Seoul), 2023, 10.4062/biomolther.2023.062
Redox Biol, 2022, 55:102421
S8792 UAMC-3203 UAMC-3203 is an improved ferroptosis inhibitor with an IC50 value of 10 nM in IMR-32 Neuroblastoma Cells.
Cell Death Differ, 2023, 30(8):1988-2004
Br J Cancer, 2023, 129(4):601-611
Br J Cancer, 2023, 129(4):601-611
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.
Sci Adv, 2024, 10(7):eadk1835
Redox Biol, 2023, 62:102678
Redox Biology, 2023, Volume 62
S8432 Troglitazone Troglitazone 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
S4452 ML162 ML162 is a covalent inhibitor of cellular phospholipid glutathione peroxidase (GPX-4) that induces ferroptosis.
Sci Adv, 2024, 10(7):eadk1835
Int J Mol Sci, 2023, 24(2)1667
Cell Metab, 2022, S1550-4131-2200411-9
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.Solutions are unstable and should be fresh-prepared.
bioRxiv, 2023, 10.1101/2023.04.05.535746
E0375 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.
Cell Death Discov, 2023, 10.1038/s41420-023-01712-7
S9840 SRS16-86 SRS16-86, a novel third-generation ferrostatin, is an inhibitor of ferroptosis.
Chem Biol Interact, 2022, 369:110262
S9839 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.
CNS Neurosci Ther, 2023, 10.1111/cns.14130
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.
E1063 Piperazine Erastin Piperazine Erastin is an analog of Erastin, which can induces ferroptosis in cancer cells, an iron-dependent form of nonapoptotic cell death.
E1874New Erastin2 Erastin2 is an inducer of ferroptosis. It also selectively inhibits xc(-) cystine/glutamate transporter. It induces ferroptosis in HT-1080, T98G, and A549 cells with the potential to treat neurodegenerative diseases.
E1535New icFSP1 icFSP1 is a potent, selective human ferroptosis suppressor protein-1 (hFSP1) inhibitor, promotes ferroptosis and indirectly inhibits FSP1 by inducing condensate formation.
E1574New FSEN1 FSEN1 is a potent and non-competitive FSP1 inhibitor with an IC50 value of 313 nM. It triggers iron death in cancer cells by inhibiting FSP1 and can be used in research of cancer.
E1812New N6F11 N6F11 is an inducer of ferroptosis. N6F11 is bound to the RING domain of the E3 ubiquitin ligase tripartite motif containing 25 (TRIM25) in cancer cells to trigger TRIM25-mediated K48-linked ubiquitination of glutathione peroxidase 4 (GPX4), resulting in proteasomal degradation.
S7243 Fer-1 (Ferrostatin-1) Fer-1 (Ferrostatin-1) is a potent and selective inhibitor of ferroptosis with EC50 of 60 nM.
Nature, 2024, 626(7998):411-418.
Redox Biol, 2024, 69:103002
Cell Death Dis, 2024, 15(2):149
S7699 Liproxstatin-1 Liproxstatin-1 is a potent ferroptosis inhibitor with an IC50 of 22 nM.
Nature, 2024, 626(7998):411-418.
Nat Commun, 2024, 15(1):1429
J Transl Med, 2024, 22(1):9
S1077 SB202190 SB202190 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 Rep Med, 2024, 5(2):101396
Theranostics, 2024, 14(4):1561-1582
Clin Transl Med, 2024, 14(2):e1583
S1623 Acetylcysteine (N-acetylcysteine) Acetylcysteine (N-acetyl-l-cysteine, NAC,N-acetylcysteine) 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 are unstable and should be fresh-prepared.
Cell Signal, 2024, 114:111004
Korean J Physiol Pharmacol, 2024, 28(1):21-30
Sci Adv, 2024, 10(3):eadi2012
S5742 Deferoxamine mesylate Deferoxamine mesylate 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.Please do not prepare stock solutions with normal saline or PBS, as precipitation may occur.
Redox Biol, 2024, 69:103008
Ecotoxicol Environ Saf, 2024, 270:115889
J Cancer, 2024, 15(3):685-698
S2556 Rosiglitazone Rosiglitazone 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.
Nat Commun, 2024, 15(1):1429
J Hematol Oncol, 2023, 16(1):30
EBioMedicine, 2023, 10.1016/j.ebiom.2023.104865
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.
Immunity, 2024, 57(1):52-67.e10
Nat Commun, 2023, 14(1):1235
Theranostics, 2023, 13(9):2863-2878
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.
Nutrients, 2023, 15(3)740
Phytother Res, 2022, 36(3):1326-1337
Oncol Rep, 2022, 48(6)221
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.
Nat Commun, 2023, 14(1):3648
Redox Biol, 2023, 60:102632
Cell Rep, 2023, 42(12):113431
S2505 Rosiglitazone maleate Rosiglitazone maleate, 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.
Stem Cell Reports, 2022, 17(11):2531-2547
Cell Death Dis, 2021, 12(11):972
Antioxidants (Basel), 2021, 10(2)155
S3031 Linagliptin (GSK2118436) Linagliptin (GSK2118436) 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.
Cell Death Dis, 2023, 10.1038/s41419-023-06240-x
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
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 Genet Genomics, 2022, S1673-8527(22)00133-3
J Cell Mol Med, 2022, 10.1111/jcmm.17154
S1443 Zileuton Zileuton 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.
Cancer Sci, 2023, 10.1111/cas.15994
Biomol Ther (Seoul), 2023, 10.4062/biomolther.2023.062
Redox Biol, 2022, 55:102421
S8792 UAMC-3203 UAMC-3203 is an improved ferroptosis inhibitor with an IC50 value of 10 nM in IMR-32 Neuroblastoma Cells.
Cell Death Differ, 2023, 30(8):1988-2004
Br J Cancer, 2023, 129(4):601-611
Br J Cancer, 2023, 129(4):601-611
S8432 Troglitazone Troglitazone 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
S9840 SRS16-86 SRS16-86, a novel third-generation ferrostatin, is an inhibitor of ferroptosis.
Chem Biol Interact, 2022, 369:110262
S9839 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.
CNS Neurosci Ther, 2023, 10.1111/cns.14130
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.
E1874New Erastin2 Erastin2 is an inducer of ferroptosis. It also selectively inhibits xc(-) cystine/glutamate transporter. It induces ferroptosis in HT-1080, T98G, and A549 cells with the potential to treat neurodegenerative diseases.
E1535New icFSP1 icFSP1 is a potent, selective human ferroptosis suppressor protein-1 (hFSP1) inhibitor, promotes ferroptosis and indirectly inhibits FSP1 by inducing condensate formation.
E1574New FSEN1 FSEN1 is a potent and non-competitive FSP1 inhibitor with an IC50 value of 313 nM. It triggers iron death in cancer cells by inhibiting FSP1 and can be used in research of cancer.
S1166 Cisplatin Cisplatin 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 unstable and should be fresh-prepared.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation.
Nat Commun, 2024, 15(1):866
Clin Cancer Res, 2024, 30(1):187-197
Cancer Lett, 2024, 586:216695
S7397 Sorafenib Sorafenib 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.
Mol Cell, 2023, 83(5):803-818.e8
Adv Sci (Weinh), 2023, 10.1002/advs.202302025
Adv Sci (Weinh), 2023, 10(27):e2302025
S2111 Lapatinib Lapatinib, 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.
Nat Commun, 2023, 14(1):5035
Nat Commun, 2023, 10.1038/s41467-023-39059-3
Nat Commun, 2023, 14(1):3469
S7242 Erastin Erastin is a ferroptosis activator by acting on mitochondrial VDAC, exhibiting selectivity for tumor cells bearing oncogenic RAS. Solutions are unstable and should be fresh-prepared.
Nat Commun, 2024, 15(1):1429
Genome Biol, 2024, 25(1):58
Redox Biol, 2024, 69:103002
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.
Nature, 2024, 626(7998):411-418.
Nat Commun, 2024, 15(1):1429
Biomed Pharmacother, 2024, 171:116163
S1040 Sorafenib tosylate Sorafenib 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.
bioRxiv, 2024, 10.1101/2023.01.18.524628
Cell, 2023, S0092-8674(23)01032-2
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
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.
Cell Rep, 2024, 43(1):113606.
Signal Transduct Target Ther, 2023, 10.1038/s41392-023-01578-2
Signal Transduct Target Ther, 2023, 8(1):355
S1792 Simvastatin Simvastatin 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.
Neuron, 2023, S0896-6273(23)00513-5
Cancer Res, 2023, 83(13):2248-2261
Cell Death Dis, 2023, 14(4):234
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.
Mol Ther Nucleic Acids, 2023, 31:421-436
Mol Med, 2023, 29(1):91
Biomater Res, 2023, 27(1):11
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).
Nat Commun, 2023, 14(1):6699
EMBO Mol Med, 2023, e17187.
Int J Nanomedicine, 2023, 18:2989-3006
S8254 FIN56 FIN56 is a specific inducer of ferroptosis .
Antioxidants (Basel), 2024, 13(1)114
J Hematol Oncol, 2023, 16(1):46
Exp Hematol Oncol, 2023, 12(1):47
S1576 Sulfasalazine Sulfasalazine 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.
Adv Sci (Weinh), 2023, 10(20):e2300517
Proc Natl Acad Sci U S A, 2022, 119(36):e2117396119
Cell Mol Life Sci, 2022, 79(5):228
S1712 Deferasirox Deferasirox 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.
J Transl Med, 2023, 21(1):50
Cell Death Discov, 2023, 9(1):97
Cancer Discov, 2022, 12(9):2180-2197
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.
Sci Adv, 2024, 10(7):eadk1835
Redox Biol, 2023, 62:102678
Redox Biology, 2023, Volume 62
S4452 ML162 ML162 is a covalent inhibitor of cellular phospholipid glutathione peroxidase (GPX-4) that induces ferroptosis.
Sci Adv, 2024, 10(7):eadk1835
Int J Mol Sci, 2023, 24(2)1667
Cell Metab, 2022, S1550-4131-2200411-9
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.Solutions are unstable and should be fresh-prepared.
bioRxiv, 2023, 10.1101/2023.04.05.535746
E0375 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.
Cell Death Discov, 2023, 10.1038/s41420-023-01712-7
E1812New N6F11 N6F11 is an inducer of ferroptosis. N6F11 is bound to the RING domain of the E3 ubiquitin ligase tripartite motif containing 25 (TRIM25) in cancer cells to trigger TRIM25-mediated K48-linked ubiquitination of glutathione peroxidase 4 (GPX4), resulting in proteasomal degradation.
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.
Cell Death Discov, 2024, 10(1):35
J Cell Mol Med, 2024, 28(2):e18055
Nat Commun, 2023, 14(1):6107
S8877New IKE(Imidazole ketone erastin) IKE(Imidazole ketone erastin) is a potent, selective, and metabolically stable system xc– inhibitor and inducer of ferroptosis.
Nat Commun, 2023, 14(1):4758
Nat Commun, 2023, 14(1):4758
J Clin Invest, 2023, 133(10)e166647
S8877New IKE(Imidazole ketone erastin) IKE(Imidazole ketone erastin) is a potent, selective, and metabolically stable system xc– inhibitor and inducer of ferroptosis.
Nat Commun, 2023, 14(1):4758
Nat Commun, 2023, 14(1):4758
J Clin Invest, 2023, 133(10)e166647
E1874New Erastin2 Erastin2 is an inducer of ferroptosis. It also selectively inhibits xc(-) cystine/glutamate transporter. It induces ferroptosis in HT-1080, T98G, and A549 cells with the potential to treat neurodegenerative diseases.
E1535New icFSP1 icFSP1 is a potent, selective human ferroptosis suppressor protein-1 (hFSP1) inhibitor, promotes ferroptosis and indirectly inhibits FSP1 by inducing condensate formation.
E1574New FSEN1 FSEN1 is a potent and non-competitive FSP1 inhibitor with an IC50 value of 313 nM. It triggers iron death in cancer cells by inhibiting FSP1 and can be used in research of cancer.
E1812New N6F11 N6F11 is an inducer of ferroptosis. N6F11 is bound to the RING domain of the E3 ubiquitin ligase tripartite motif containing 25 (TRIM25) in cancer cells to trigger TRIM25-mediated K48-linked ubiquitination of glutathione peroxidase 4 (GPX4), resulting in proteasomal degradation.

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