Ferroptosis

Ferroptosis製品

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  • Ferroptosis阻害剤 (22)
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S1166 Cisplatin シスプラチン (Cisplatin (NSC 119875, Cisplatinum, cis-diamminedichloroplatinum II, CDDP, cis DDP, DDP)) は無機白金錯体であり、腫瘍細胞中において DNA 付加物を形成することにより DNA 合成を阻害する能力を有します。シスプラチンはフェロトーシス (ferroptosis) を活性化し、オートファジー (autophagy) を誘導します。溶液は都度調製してください。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 Cancer, 2024, 10.1038/s43018-024-00814-0
Nat Commun, 2024, 15(1):5775
Nat Commun, 2024, 15(1):2853
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.
J Hematol Oncol, 2024, 17(1):78
Cell Rep Med, 2024, S2666-3791(24)00201-5
J Exp Clin Cancer Res, 2024, 43(1):143
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.
Drug Resist Updat, 2024, 73:101066
J Extracell Vesicles, 2024, 13(7):e12494
Cancer Lett, 2024, 593:216968
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.
Nature, 2024, 626(7998):411-418.
Signal Transduct Target Ther, 2024, 9(1):257
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.
Cell Metab, 2024, S1550-4131(24)00371-1
Nat Commun, 2024, 15(1):1429
Nat Commun, 2024, 15(1):7522
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.
Nature, 2024, 626(7998):411-418.
Cell Discov, 2024, 10(1):39
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.
Nature, 2024, 629(8013):927-936
Cell Mol Life Sci, 2024, 81(1):238
J Transl Med, 2024, 22(1):593
S7699 Liproxstatin-1 Liproxstatin-1 is a potent ferroptosis inhibitor with an IC50 of 22 nM.
Nature, 2024, 626(7998):411-418.
Nature, 2024, 626(7998):411-418.
Mol Cancer, 2024, 23(1):113
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.
Nat Commun, 2024, 15(1):4124
Nat Commun, 2024, 15(1):5874
Nat Commun, 2024, 15(1):4124
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.
Nat Commun, 2024, 15(1):4124
Nat Commun, 2024, 15(1):4124
Dev Cell, 2024, S1534-5807(24)00326-5
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.
J Adv Res, 2024, S2090-1232(24)00422-3
Int J Biol Sci, 2024, 20(6):2323-2338
Cell Death Dis, 2024, 15(2):175
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.
Nat Commun, 2024, 15(1):3533
Theranostics, 2024, 14(7):2856-2880
Theranostics, 2024, 14(7):2856-2880
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.
Cancer Commun (Lond), 2024, 10.1002/cac2.12608
Cell Rep Med, 2024, 5(3):101476
Emerg Microbes Infect, 2024, 13(1):2382235
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.
Cancer Med, 2024, 13(12):e7393
Neuron, 2023, S0896-6273(23)00513-5
Cancer Res, 2023, 83(13):2248-2261
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
Nat Commun, 2024, 15(1):7991
Research (Wash D C), 2024, 7:0400
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, 2024, 15(1):8663
MedComm (2020), 2024, 5(8):e668
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.
Cancers (Basel), 2024, 16(5)976
PLoS One, 2024, 19(2):e0299145
Mol Ther Nucleic Acids, 2023, 31:421-436
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.
Cancer Cell Int, 2024, 24(1):303
Front Pharmacol, 2024, 15:1418902
PLoS Negl Trop Dis, 2024, 18(8):e0012428
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, 2024, 43(4):114003
BMC Cancer, 2024, 24(1):587
FEBS Open Bio, 2024, 10.1002/2211-5463.13901
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, 2024, 15(1):7249
Sci Rep, 2024, 14(1):22572
Nat Commun, 2023, 14(1):3648
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
Hepatol Commun, 2024, 8(3)e0396
J Hematol Oncol, 2023, 16(1):46
S8877 IKE(Imidazole ketone erastin) IKE(Imidazole ketone erastin) is a potent, selective, and metabolically stable system xc– inhibitor and inducer of ferroptosis.
Nat Struct Mol Biol, 2024, 10.1038/s41594-024-01329-z
Nat Commun, 2024, 15(1):8971
Redox Biol, 2024, 72:103137
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.
Pharmacol Res, 2024, 207:107298
Cell Death Dis, 2023, 10.1038/s41419-023-06240-x
J Pers Med, 2022, 12(2)258
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.
Med Oncol, 2024, 41(8):188
Adv Sci (Weinh), 2023, 10(20):e2300517
Proc Natl Acad Sci U S A, 2022, 119(36):e2117396119
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.
Elife, 2023, 12RP88745
J Transl Med, 2023, 21(1):50
Cell Death Discov, 2023, 9(1):97
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.
J Transl Med, 2024, 22(1):593
Commun Biol, 2022, 5(1):231
J Genet Genomics, 2022, S1673-8527(22)00133-3
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.
Nat Commun, 2024, 15(1):8663
J Transl Med, 2023, 21(1):923
Cancer Sci, 2023, 10.1111/cas.15994
S8792 UAMC-3203 UAMC-3203 is an improved ferroptosis inhibitor with an IC50 value of 10 nM in IMR-32 Neuroblastoma Cells.
Front Immunol, 2024, 15:1384606
Cell Death Differ, 2023, 30(8):1988-2004
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.
Cell Death Dis, 2024, 15(9):695
Cell Death Discov, 2024, 10(1):108
Commun Biol, 2024, 7(1):732
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.
CNS Neurosci Ther, 2024, 30(8):e14911
Int J Mol Med, 2024, 53(4)37
Free Radic Biol Med, 2021, 163:234-242
S4452 ML162 ML162 is a covalent inhibitor of cellular phospholipid glutathione peroxidase (GPX-4) that induces ferroptosis.
Nat Cell Biol, 2024, 10.1038/s41556-024-01450-7
Theranostics, 2024, 14(10):4090-4106
Mol Oncol, 2024, 10.1002/1878-0261.13716
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.
Nat Commun, 2024, 15(1):7611
iScience, 2024, 27(5):109774
J Ethnopharmacol, 2024, 328:118080
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.

Antioxidants (Basel), 2024, 13(4)430
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.
J Oleo Sci, 2024, 73(7):991-999
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. Nordihydroguaiaretic acid (NDGA) inhibits p300 and activates autophagy. Nordihydroguaiaretic acid (NDGA) protects cells from ferroptosis.
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.
E1867New NPD4928 NPD4928 is an inhibitor of Ferroptosis Suppressor Protein 1 (FSP1) that enhances ferroptosis. It enhances the cytotoxic effects on various cell types when combined with GPX4 antagonists.
E1925New Butylhydroxyanisole Butylhydroxyanisole (Butylated hydroxyanisole, BHA, E320) is an inhibitor of ferroptosis, a food preservative and antioxidant that prevents the formation of harmful compounds, extending shelf life. However, it's associated with liver toxicity, reproductive organ development issues, learning delays, and sleep problems.
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.
Nature, 2024, 626(7998):411-418.
Signal Transduct Target Ther, 2024, 9(1):257
S7699 Liproxstatin-1 Liproxstatin-1 is a potent ferroptosis inhibitor with an IC50 of 22 nM.
Nature, 2024, 626(7998):411-418.
Nature, 2024, 626(7998):411-418.
Mol Cancer, 2024, 23(1):113
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.
Nat Commun, 2024, 15(1):4124
Nat Commun, 2024, 15(1):5874
Nat Commun, 2024, 15(1):4124
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.
Nat Commun, 2024, 15(1):4124
Nat Commun, 2024, 15(1):4124
Dev Cell, 2024, S1534-5807(24)00326-5
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.
Cancer Commun (Lond), 2024, 10.1002/cac2.12608
Cell Rep Med, 2024, 5(3):101476
Emerg Microbes Infect, 2024, 13(1):2382235
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
Nat Commun, 2024, 15(1):7991
Research (Wash D C), 2024, 7:0400
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, 2024, 15(1):8663
MedComm (2020), 2024, 5(8):e668
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.
Cancer Cell Int, 2024, 24(1):303
Front Pharmacol, 2024, 15:1418902
PLoS Negl Trop Dis, 2024, 18(8):e0012428
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, 2024, 15(1):7249
Sci Rep, 2024, 14(1):22572
Nat Commun, 2023, 14(1):3648
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.
Pharmacol Res, 2024, 207:107298
Cell Death Dis, 2023, 10.1038/s41419-023-06240-x
J Pers Med, 2022, 12(2)258
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.
J Transl Med, 2024, 22(1):593
Commun Biol, 2022, 5(1):231
J Genet Genomics, 2022, S1673-8527(22)00133-3
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.
Nat Commun, 2024, 15(1):8663
J Transl Med, 2023, 21(1):923
Cancer Sci, 2023, 10.1111/cas.15994
S8792 UAMC-3203 UAMC-3203 is an improved ferroptosis inhibitor with an IC50 value of 10 nM in IMR-32 Neuroblastoma Cells.
Front Immunol, 2024, 15:1384606
Cell Death Differ, 2023, 30(8):1988-2004
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.
CNS Neurosci Ther, 2024, 30(8):e14911
Int J Mol Med, 2024, 53(4)37
Free Radic Biol Med, 2021, 163:234-242
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.
J Oleo Sci, 2024, 73(7):991-999
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. Nordihydroguaiaretic acid (NDGA) inhibits p300 and activates autophagy. Nordihydroguaiaretic acid (NDGA) protects cells from ferroptosis.
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.
E1867New NPD4928 NPD4928 is an inhibitor of Ferroptosis Suppressor Protein 1 (FSP1) that enhances ferroptosis. It enhances the cytotoxic effects on various cell types when combined with GPX4 antagonists.
E1925New Butylhydroxyanisole Butylhydroxyanisole (Butylated hydroxyanisole, BHA, E320) is an inhibitor of ferroptosis, a food preservative and antioxidant that prevents the formation of harmful compounds, extending shelf life. However, it's associated with liver toxicity, reproductive organ development issues, learning delays, and sleep problems.
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 シスプラチン (Cisplatin (NSC 119875, Cisplatinum, cis-diamminedichloroplatinum II, CDDP, cis DDP, DDP)) は無機白金錯体であり、腫瘍細胞中において DNA 付加物を形成することにより DNA 合成を阻害する能力を有します。シスプラチンはフェロトーシス (ferroptosis) を活性化し、オートファジー (autophagy) を誘導します。溶液は都度調製してください。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 Cancer, 2024, 10.1038/s43018-024-00814-0
Nat Commun, 2024, 15(1):5775
Nat Commun, 2024, 15(1):2853
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.
J Hematol Oncol, 2024, 17(1):78
Cell Rep Med, 2024, S2666-3791(24)00201-5
J Exp Clin Cancer Res, 2024, 43(1):143
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.
Drug Resist Updat, 2024, 73:101066
J Extracell Vesicles, 2024, 13(7):e12494
Cancer Lett, 2024, 593:216968
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.
Cell Metab, 2024, S1550-4131(24)00371-1
Nat Commun, 2024, 15(1):1429
Nat Commun, 2024, 15(1):7522
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.
Nature, 2024, 626(7998):411-418.
Cell Discov, 2024, 10(1):39
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.
Nature, 2024, 629(8013):927-936
Cell Mol Life Sci, 2024, 81(1):238
J Transl Med, 2024, 22(1):593
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.
Nat Commun, 2024, 15(1):3533
Theranostics, 2024, 14(7):2856-2880
Theranostics, 2024, 14(7):2856-2880
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.
Cancer Med, 2024, 13(12):e7393
Neuron, 2023, S0896-6273(23)00513-5
Cancer Res, 2023, 83(13):2248-2261
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.
Cancers (Basel), 2024, 16(5)976
PLoS One, 2024, 19(2):e0299145
Mol Ther Nucleic Acids, 2023, 31:421-436
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, 2024, 43(4):114003
BMC Cancer, 2024, 24(1):587
FEBS Open Bio, 2024, 10.1002/2211-5463.13901
S8254 FIN56 FIN56 is a specific inducer of ferroptosis .
Antioxidants (Basel), 2024, 13(1)114
Hepatol Commun, 2024, 8(3)e0396
J Hematol Oncol, 2023, 16(1):46
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.
Med Oncol, 2024, 41(8):188
Adv Sci (Weinh), 2023, 10(20):e2300517
Proc Natl Acad Sci U S A, 2022, 119(36):e2117396119
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.
Elife, 2023, 12RP88745
J Transl Med, 2023, 21(1):50
Cell Death Discov, 2023, 9(1):97
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.
Cell Death Dis, 2024, 15(9):695
Cell Death Discov, 2024, 10(1):108
Commun Biol, 2024, 7(1):732
S4452 ML162 ML162 is a covalent inhibitor of cellular phospholipid glutathione peroxidase (GPX-4) that induces ferroptosis.
Nat Cell Biol, 2024, 10.1038/s41556-024-01450-7
Theranostics, 2024, 14(10):4090-4106
Mol Oncol, 2024, 10.1002/1878-0261.13716
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.
Nat Commun, 2024, 15(1):7611
iScience, 2024, 27(5):109774
J Ethnopharmacol, 2024, 328:118080
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.

Antioxidants (Basel), 2024, 13(4)430
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.
J Adv Res, 2024, S2090-1232(24)00422-3
Int J Biol Sci, 2024, 20(6):2323-2338
Cell Death Dis, 2024, 15(2):175
S8877 IKE(Imidazole ketone erastin) IKE(Imidazole ketone erastin) is a potent, selective, and metabolically stable system xc– inhibitor and inducer of ferroptosis.
Nat Struct Mol Biol, 2024, 10.1038/s41594-024-01329-z
Nat Commun, 2024, 15(1):8971
Redox Biol, 2024, 72:103137
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.
E1867New NPD4928 NPD4928 is an inhibitor of Ferroptosis Suppressor Protein 1 (FSP1) that enhances ferroptosis. It enhances the cytotoxic effects on various cell types when combined with GPX4 antagonists.
E1925New Butylhydroxyanisole Butylhydroxyanisole (Butylated hydroxyanisole, BHA, E320) is an inhibitor of ferroptosis, a food preservative and antioxidant that prevents the formation of harmful compounds, extending shelf life. However, it's associated with liver toxicity, reproductive organ development issues, learning delays, and sleep problems.
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.

Ferroptosis阻害剤の選択性比較

Tags: Ferroptosis inhibitor|Ferroptosis agonist|Ferroptosis activator|Ferroptosis inducer|Ferroptosis antagonist|Ferroptosis signaling pathway|Ferroptosis assay kit