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. |
-
Int J Mol Med, 2025, 55(1)17
-
Nat Cancer, 2024, 10.1038/s43018-024-00814-0
-
Nat Commun, 2024, 15(1):5775
|
|
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 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):5874
-
Nat Commun, 2024, 15(1):4124
-
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. |
-
Mol Cancer, 2024, 23(1):240
-
Nat Commun, 2024, 15(1):4124
-
Nat Commun, 2024, 15(1):4124
|
|
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
-
J Adv Res, 2024, S2090-1232(24)00491-0
-
Int J Biol Sci, 2024, 20(6):2323-2338
|
|
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. |
-
Mol Cancer, 2024, 23(1):240
-
Cancer Commun (Lond), 2024, 10.1002/cac2.12608
-
Adv Sci (Weinh), 2024, 11(40):e2402671
|
|
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. |
-
Nat Commun, 2024, 15(1):9550
-
Cell Death Dis, 2024, 15(9):695
-
Cell Death Discov, 2024, 10(1):108
|
|
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. |
-
Theranostics, 2024, 14(16):6161-6184
-
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. |
|
|
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. |
|
|
E1535 |
icFSP1
|
icFSP1 is a potent, selective human ferroptosis suppressor protein-1 (hFSP1) inhibitor, promotes ferroptosis and indirectly inhibits FSP1 by inducing condensate formation. |
|
|
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. |
|
|
E1574 |
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):5874
- Nat Commun, 2024, 15(1):4124
- 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. |
- Mol Cancer, 2024, 23(1):240
- Nat Commun, 2024, 15(1):4124
- Nat Commun, 2024, 15(1):4124
|
|
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. |
- Mol Cancer, 2024, 23(1):240
- Cancer Commun (Lond), 2024, 10.1002/cac2.12608
- Adv Sci (Weinh), 2024, 11(40):e2402671
|
|
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
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S1443 |
Zileuton
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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
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S8792 |
UAMC-3203
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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
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S8432 |
Troglitazone
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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
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S9840 |
SRS16-86
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SRS16-86, a novel third-generation ferrostatin, is an inhibitor of ferroptosis. |
- Chem Biol Interact, 2022, 369:110262
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S9839 |
SRS11-92
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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
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S3984 |
Nordihydroguaiaretic acid (NDGA)
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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. |
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E1874New |
Erastin2
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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. |
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E1867New |
NPD4928
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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. |
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E1535 |
icFSP1
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icFSP1 is a potent, selective human ferroptosis suppressor protein-1 (hFSP1) inhibitor, promotes ferroptosis and indirectly inhibits FSP1 by inducing condensate formation. |
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E1925New |
Butylhydroxyanisole
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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. |
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E1574 |
FSEN1
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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. |
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S1166 |
Cisplatin
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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. |
- Int J Mol Med, 2025, 55(1)17
- Nat Cancer, 2024, 10.1038/s43018-024-00814-0
- Nat Commun, 2024, 15(1):5775
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S7397 |
Sorafenib
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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
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S2111 |
Lapatinib
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Lapatinib 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
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S7242 |
Erastin
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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
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S8155 |
RSL3
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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
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S1040 |
Sorafenib tosylate
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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
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S1007 |
Roxadustat (FG-4592)
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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
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S1792 |
Simvastatin
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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
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S7309 |
BAY 87-2243
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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
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S8661 |
CA3 (CIL56)
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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
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S8254 |
FIN56
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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
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S1576 |
Sulfasalazine
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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
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S1712 |
Deferasirox
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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
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S0788 |
ML 210
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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. |
- Nat Commun, 2024, 15(1):9550
- Cell Death Dis, 2024, 15(9):695
- Cell Death Discov, 2024, 10(1):108
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S4452 |
ML162
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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
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S9663 |
iFSP1
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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
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E0375 |
Ammonium ferric citrate
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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. |
- Theranostics, 2024, 14(16):6161-6184
- Antioxidants (Basel), 2024, 13(4)430
- Cell Death Discov, 2023, 10.1038/s41420-023-01712-7
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E1812New |
N6F11
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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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