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
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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. Nordihydroguaiaretic acid (NDGA) inhibits p300 and activates autophagy. Nordihydroguaiaretic acid (NDGA) protects cells from ferroptosis. |
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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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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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E1574New |
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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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
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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, 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
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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. |
- Cell Death Dis, 2024, 15(9):695
- Cell Death Discov, 2024, 10(1):108
- Commun Biol, 2024, 7(1):732
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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.
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- 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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