鐵死亡 (Ferroptosis) 是由 Scott J. Dixon 與 Brent R. Stockwell 等人於 2012 年首次提出的一種新型調控性細胞死亡 (regulated cell death, RCD),其特徵為鐵離子依賴性的脂質過氧化反應 (lipid peroxidation) 造成細胞膜磷脂中的多元不飽和脂肪酸 (polyunsaturated fatty acids, PUFAs) 發生氧化,過量累積的脂質過氧化物 (lipid hydroperoxides) 導致細胞膜完整性喪失,最終造成細胞死亡。近年來,關於鐵死亡與人類疾病的研究迅速蓬勃發展,包括癌症、神經退化性疾病(如阿茲海默症與帕金森氏症)、缺血再灌注損傷、心血管疾病、腎臟疾病、肝臟疾病、自體免疫疾病及微生物感染等,皆被認為可望透過調控鐵死亡機制發展新的治療策略,是極具開發潛力的藥物研發標的 [1-4]。本篇文章特別整理出來自化合物領導品牌 Selleck Chemicals (Selleckchem) 的鐵死亡常用研究化合物,包括抑制劑 (Inhibitors)、誘導劑 (Inducers) 和活化劑 (Activators),以及適用於高通量藥物篩選的化合物庫 (Compound Library) [5-6]。點擊列表中的產品名稱即可瀏覽詳細說明,包含化學結構、純度、生物活性、研究文獻及相關技術資料等。也歡迎您與我們聯繫,索取最新產品資訊與活動訊息。
鐵死亡抑制劑 (Ferroptosis Inhibitors)
能阻斷鐵離子過載、消除脂質過氧化物或螯合不穩定鐵池 (labile iron pool, LIP) 中的游離鐵,主要用於驗證細胞是否死於鐵死亡機制。
| Cat.No. | Product Name | Information |
|---|---|---|
| S8078 | Bardoxolone Methyl (RTA 402) | 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. |
| E1925 | 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. |
| S1712 | Deferasirox (ICL670) | 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. |
| 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. |
| S7243 | Ferrostatin-1 (Fer-1) | Ferrostatin-1 (Fer-1) is a potent and selective inhibitor of ferroptosis with EC50 of 60 nM. |
| S3031 | Linagliptin | Linagliptin 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. |
| S7699 | Liproxstatin-1 | Liproxstatin-1 is a potent ferroptosis inhibitor with an IC50 of 22 nM. |
| S1623 | N-Acetylcysteine (NAC chemical, N-Acetyl-L-Cysteine) | 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. |
| 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. |
| S2046 | Pioglitazone HCl | Pioglitazone HCl (AD-4833, U-72107E) is an inhibitor of cytochrome P450 (CYP)2C8 and CYP3A4 enzymes. This compound inhibits CYP2C8, CYP3A4 and CYP2C9 with Ki of 1.7 μM, 11.8 μM and 32.1 μM, respectively. It 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. This chemical inhibits mitochondrial iron uptake, lipid peroxidation, and subsequent ferroptosis. |
| S2556 | Rosiglitazone (BRL 49653) | 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. |
| 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. This compound also modulates TRP channels and induces autophagy. It prevents ferroptosis. |
| 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. This compound inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. It significantly suppresses Erastin-dependent ferroptosis. |
| S7171 | Setanaxib (GKT137831) | Setanaxib (GKT137831, GKT831) is a potent, dual NADPH oxidase NOX1/NOX4 inhibitor with Ki of 110 nM and 140 nM, respectively. This compound suppresses reactive oxygen species (ROS) production and partly inhibits ferroptosis. |
| S9839 | SRS11-92 | SRS11-92 (AA9), a Ferrostatin-1 (Fer-1) analogue, is a potent inhibitor of ferroptosis. This compound inhibits ferroptotic cell death induced by Erastin in HT-1080 human fibrosarcoma cells with EC50 of 6 nM. |
| S9840 | SRS16-86 | SRS16-86, a novel third-generation ferrostatin, is an inhibitor of ferroptosis. |
| S8432 | Troglitazone (CS-045) | 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. |
| S8792 | UAMC-3203 | UAMC-3203 is an improved ferroptosis inhibitor with an IC50 value of 10 nM in IMR-32 Neuroblastoma Cells. |
| 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. This compound induces apoptosis while inhibits ferroptosis. |
鐵死亡誘導劑 (Ferroptosis Inducers)
藉由阻斷胱胺酸/麩胺酸反向轉運蛋白 system xc- 以耗竭穀胱甘肽 (glutathione, GSH)、直接或間接抑制穀胱甘肽過氧化物酶 4 (glutathione peroxidase 4, GPX4) 的活性,進而誘發脂質過氧化反應並導致細胞鐵死亡。
| Cat.No. | Product Name | Information |
|---|---|---|
| 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. |
| S2264 | Artemether (SM-224) | Artemether (SM-224, CGP 56696) is an antimalarial for the treatment of resistant strains of falciparum malaria. |
| S7309 | BAY 87-2243 | BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. This compound inhibits mitochondrial complex I activity, thus triggering a mitophagy-dependent ROS increase leading to necroptosis and ferroptosis. It exerts antitumor activity. Phase 1. |
| S0910 | Bufotalin | Bufotalin is a bufadienolide from Venenum bufonis that acts as a novel inhibitor of GPX4 and induces iron-dependent ferroptosis in non-small cell lung cancer (NSCLC) cells, significantly reducing proliferation by accelerating GPX4 degradation and increasing intracellular Fe2+. |
| 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). |
| 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. |
| S1848 | Curcumin (Diferuloylmethane) | 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. |
| 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. |
| E1874 | 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. |
| E4962 | Ferric citrate | Ferric citrate (Iron(III) citrate, Zerenex) is a Class 1 ferroptosis inducer and a safe, effective oral phosphate binder that increases iron stores and reduces the need for IV iron and erythropoiesis-stimulating agents while maintaining hemoglobin. It is approved for treating hyperphosphatemia in dialysis-dependent chronic kidney disease (CKD) and for iron deficiency anemia. |
| S8254 | FIN56 | FIN56 is a specific inducer of ferroptosis. |
| S8877 | Imidazole Ketone Erastin (IKE) | IKE(Imidazole ketone erastin) is a potent, selective, and metabolically stable system xc– inhibitor and inducer of ferroptosis. |
| S2111 | Lapatinib (GW572016) | 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. |
| S4452 | ML162 | ML162 is a covalent inhibitor of cellular phospholipid glutathione peroxidase (GPX-4) that induces ferroptosis. |
| S0788 | ML-210 | ML-210 (CID 49766530) is a selective covalent inhibitor of cellular glutathione peroxidase (GPX-4) 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. |
| E1812 | N6F11 | N6F11 is an inducer of ferroptosis. This compound 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. |
| 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. |
| 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. |
| S1792 | Simvastatin (MK-733) | 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. |
| S7397 | Sorafenib (BAY 43-9006) | 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. |
| S1040 | Sorafenib Tosylate (BAY 43-9006) | 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. |
| S1576 | Sulfasalazine | Sulfasalazine is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. This compound is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. It induces ferroptosis, apoptosis and autophagy. |
鐵死亡調節劑/活化劑 (Ferroptosis Modulators/Activators)
靶向鐵死亡的核心防禦路徑(如 FSP1/CoQ10 路徑、NRF2 路徑、鐵代謝或粒線體功能),用於調控細胞對鐵死亡的敏感性 (sensitivity),或與誘導劑協同放大細胞死亡反應。
| Cat.No. | Product Name | Information |
|---|---|---|
| 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. |
| E1535 | icFSP1 | icFSP1 is a potent, selective human ferroptosis suppressor protein-1 (hFSP1) inhibitor, promotes ferroptosis and indirectly inhibits FSP1 by inducing condensate formation. |
| S9663 | iFSP1 | iFSP1 is a potent, selective and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1/AIFM2) with EC50 of 103 nM. This compound selectively induces ferroptosis in GPX4-knockout Pfa1 and HT1080 cells that overexpresses FSP1. Solutions are unstable and should be fresh-prepared. |
| 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. This compound regulates the activity of several ferroptosis and lipid peroxidation-related proteins. |
| E1867 | 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. |
| 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. This compound also potentiates RSL3 induced ferroptosis. Phase 3. |
鐵死亡化合物庫 (Ferroptosis Compound Library)
完整收錄 724 種鐵死亡研究相關化合物,其中包含 FDA 核准藥物,非常適合應用於高通量篩選 (high-throughput screening, HTS) 和高內涵篩選 (high-content screening, HCS),以進行新藥開發或轉譯醫學研究。每種化合物皆提供詳盡的化學結構與生物活性資訊,並通過核磁共振 (NMR) 與高效液相層析 (HPLC) 嚴格檢驗,確保優異的高純度品質。
| Cat. No. | Product Name | Information |
|---|---|---|
| L6400 | Ferroptosis Compound Library |
|
資料來源:
- Tang B, et al. Ferroptosis as a therapeutic target in cancer: mechanisms, immune interactions, and emerging strategies. Mol Cancer. 2026 Apr 9;25(1):140. doi: 10.1186/s12943-026-02590-0
- Artusi I, et al. Ferroptosis in Human Diseases: Fundamental Roles and Emerging Therapeutic Perspectives. Antioxidants (Basel). 2025 Nov 26;14(12):1411. doi: 10.3390/antiox14121411
- Dixon SJ, et al. Ferroptosis: an iron-dependent form of nonapoptotic cell death. Cell. 2012 May 25;149(5):1060-72. doi: 10.1016/j.cell.2012.03.042
- Li G, et al. The Research Landscape of Ferroptosis in Cancer: A Bibliometric Analysis. Front Cell Dev Biol. 2022 May 25;10:841724. doi: 10.3389/fcell.2022.841724
- Ferroptosis Inhibitors/Inducers | Selleck Chemicals
- Ferroptosis Compound Library | Selleck Chemicals
