erastin / Whitehead Institute for Biomedical Research, Dana-Farber Cancer Institute, Columbia University, Prolexys - LARVOL DELTA

Strong protection by bazedoxifene against chemically-induced ferroptotic neuronal death in vitro and in vivo. (PubMed, Cell Commun Signal) - "Ferroptosis, a form of regulated cell death associated with glutathione depletion and excess lipid peroxidation, can be induced in cultured cells by chemicals (e.g., erastin and RSL3). Together, these results reveal that BAZ is a potent inhibitor of PDI and can strongly protect against chemically-induced ferroptosis in hippocampal neurons both in vitro and in vivo. This work provides evidence for an estrogen receptor-independent, PDI-mediated novel mechanism of neuroprotection by BAZ."

Journal • Preclinical

The role of ferroptosis as a novel alternative cell death model in thyrocytes from Hashimoto´s thyroiditis patients (ESPE-ESE 2025) - "Methodology: we analyzed lipid peroxidation with a sensor for lipid peroxidation (BodipyTM 581/591 C11) in a human thyroid follicular cell line stimulated with HT-associated proinflammatory cytokines (IFN-γ and TNF-α), ferroptosis inductors (RSL3 and erastin) and inhibitors (ferrostatin-1). our data indicates that ferroptosis may constitute a novel alternative cell death model in HT pathogenesis because of the proinflammatory microenvironment."

Clinical • Addiction (Opioid and Alcohol) • Endocrine Disorders • Grave’s Disease • Immunology • GPX4 • IFNG • TNFA

L-theanine prevents myocardial injury in sleep‑deprived mice by suppressing ferroptosis through SIRT1. (PubMed, Naunyn Schmiedebergs Arch Pharmacol) - "This study utilized a modified multiple-platform water environment method to establish an SD model and induce a ferroptosis model in H9c2 cells pretreated with erastin. Notably, the SIRT1 inhibitor EX-527 can counteract the protective effect of L-theanine against ferroptosis in cardiomyocytes. These findings highlight that L-theanine mitigates SD-induced cardiac injury primarily by suppressing ferroptosis through SIRT1 in cardiomyocytes."

Journal • Preclinical • Cardiovascular • SIRT1

Stress-induced sympathetic stimulation inhibits sorafenib-induced ferroptosis in renal cell carcinoma (AACR 2025) - "Isoproterenol (ISO), a non-specific β-adrenergic receptor agonist, was added into RCC cell lines ACHN and A498 before the addition of clinically-used-drugs (sorafenib, cabozantinib, lenvatinib, and rapamycin), and cell viability was analyzed by MTS assay... Stress-induced sympathetic stimulation inhibits sorafenib-induced ferroptosis in RCC."

Genito-urinary Cancer • Oncology • Renal Cell Carcinoma • Solid Tumor • ADRB2

The PPARβ/CERK/C1P signaling pathway is a potential mechanism by which antimony exposure promotes prostate cancer cell proliferation. (PubMed, Ecotoxicol Environ Saf) - "In addition, we also found that C1P can partially inhibit ferroptosis induced by erastin. These findings indicate that C1P is closely related to antimony-induced PCa proliferation and may be a potential biomarker of PCa."

Journal • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • CERK

Berberine alleviates tendinopathy by suppressing the cGAS-STING pathway and Relieving ferroptosis. (PubMed, Biochem Biophys Res Commun) - "To validate these findings further, we administered the ferroptosis inducer Imidazole Ketone Erastin (IKE) to evaluate the effects of berberine. IKE significantly diminished the therapeutic effects of berberine on tendinopathy, as indicated by the previously mentioned markers. Thus, berberine mitigated ferroptosis by inhibiting the cGAS-STING pathway, highlighting its potential in managing tendinopathy."

Journal • GPX4

MSNs-loaded HMME and Erastin-mediated ferroptosis combined with sonodynamic therapy for HCC treatment. (PubMed, J Cancer Res Ther) - "These findings indicate that the nanoplatform can effectively alleviate tumor hypoxia while inducing apoptosis and ferroptosis, laying the foundation for enhancing the efficacy of ROS-mediated HCC therapy."

Journal • Hepatocellular Cancer • Oncology • Solid Tumor

F-box only protein 10 protects against kidney tubulointerstitial fibrosis by inhibiting ACSL4-mediated lipid peroxidation and ferroptosis. (PubMed, Cell Signal) - "FBXO10 overexpression inhibited the EMT process and counteracted the typical ferroptosis features evoked by TGF-β1 or erastin in HK-2 cells...In summary, FBXO10 mitigates ferroptosis in renal tubular epithelial cells by inhibiting ACSL4-mediated lipid peroxidation, thereby hindering the progression of kidney tubulointerstitial fibrosis. FBXO10 is proposed as a promising target for treating kidney disorders related to tubulointerstitial fibrosis."

Journal • Chronic Kidney Disease • Fibrosis • Immunology • Inflammation • Nephrology • Renal Disease • Targeted Protein Degradation • ACSL4 • CCNF • TGFB1

Regulation of SLC7A11 by LncRNA GPRC5D-AS1 mediates ferroptosis in skeletal muscle: Mechanistic exploration of sarcopenia. (PubMed, Front Mol Biosci) - "A ferroptosis model was established in human skeletal muscle cells (HSKM) using the inducer erastin, and GPRC5D-AS1 overexpression plasmids were introduced to observe their effects on cell proliferation and ferroptosis indicators...Conversely, silencing SLC7A11 diminished the protective effects of GPRC5D-AS1 on cell proliferation and ferroptosis. These findings suggest that GPRC5D-AS1 overexpression increases SLC7A11 expression and reduces ferroptosis incidence in HSKM."

Journal • Sarcopenia • ACSL4 • GPRC5D • GPX4 • MT-CO2 • PACERR • PTGS2 • SLC7A11

PRDX1 knockdown promotes erastin-induced ferroptosis and impedes diffuse large B-cell lymphoma development by inhibiting the MAPK/ERK pathway. (PubMed, BMC Cancer) - "PRDX1 knockdown facilitates erastin-induced ferroptosis and obstacles DLBCL progression by inhibiting the MAPK/ERK pathway, offering a potential treatment strategy for DLBCL treatment."

Journal • B Cell Lymphoma • Diffuse Large B Cell Lymphoma • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • GPX4 • MT-CO2 • PRDX1 • SLC7A11

Targeting HCG18 counteracts ferroptosis resistance via blocking the miR-30a-5p/RRM2/GSS pathway in hepatocellular carcinoma. (PubMed, Int J Biol Sci) - "The colony formation assay demonstrated that overexpression of HCG18 inhibited erastin-induced cell death. In addition, in vivo experiments have also confirmed that HCG18 can inhibit ferroptosis by regulating the expression of RRM2, thereby promoting HCC proliferation. Our study discovered a novel lncRNA HCG18, as a "switch-like" molecule of the axis of miR-30a-5p/RRM2/GSS, confers resistance to ferroptosis and holds promise as a potential target for ferroptosis-dependent therapy."

Journal • Hepatocellular Cancer • Oncology • Solid Tumor • MIR30A • RRM2

Bergenin Alleviates Myocardial Ischemia/Reperfusion Injury via Regulating SIRT1 Through Ferroptosis. (PubMed, J Inflamm Res) - "The in vivo model of myocardial I/R injury was established by transient ligation of the left anterior descending coronary artery in Sprague-Dawley rats, which were divided into sham, I/R, I/R+bergenin, and I/R+bergenin+erastin (an agonist of ferroptosis) groups.After the model was established, the rats underwent echocardiography to assess the cardiac function...EX527, a SIRT1 inhibitor, was used to further explore the role of SIRT1 in the myocardial protection of bergenin...Moreover, Western blotting showed that bergenin activated SIRT1, and increased the phosphorylation of AMPK and the expression level of PGC-1α. Bergenin exerted a protective effect on the myocardium by modulating the ferroptosis process during myocardial I/R injury through the SIRT1/AMPK/PGC-1α pathway."

Journal • Cardiovascular • Metabolic Disorders • Myocardial Ischemia • Reperfusion Injury • SIRT1

Elevated NGF provokes decidual lipid peroxidation and promotes preterm birth in mice. (PubMed, J Transl Med) - "This study reveals the pivotal role of NGF signaling in promoting excessive lipid peroxidation to disrupt decidual homeostasis and ultimately triggering preterm labor in mice."

Journal • Preclinical • Infectious Disease • Inflammation • NGF

The Solute Carrier Family 47 Member 1, Transcriptionally Regulated by GATA Binding Protein 6, Inhibits Ferroptosis in Gastric Cancer. (PubMed, DNA Cell Biol) - "Knockdown of SLC47A1 promoted ferroptosis in GC cells, as evidenced by increased erastin-induced cytoplasmic membrane rupture, cell death, lipid peroxidation, and malondialdehyde levels...In summary, our study revealed the significant role of SLC47A1 in the development and progression of GC through regulating ferroptosis. Targeting the GATA6/SLC47A1 axis may be a promising therapeutic strategy for GC."

Journal • Gastric Cancer • Gastrointestinal Disorder • Oncology • Solid Tumor • GATA6

In Situ Investigation of Intercellular Communication in Ferroptosis Integrated Scanning Electrochemical Microscopy with Microfluidic Devices. (PubMed, ACS Sens) - "By in situ monitoring the changes of key parameters (ROS, glutathione (GSH), and cell membrane permeability) in Erastin-induced ferroptosis, it was found that TAMs partially restored the reduced GSH efflux, increased ROS release, and impaired cell membrane barrier in TNBCs, indicating that TAMs can suppress TNBC ferroptosis...After inhibition of STAT3, increased ROS release and membrane permeability as well as decreased GSH efflux of TNBCs were in situ monitored by SECM, demonstrating the intercellular communication mechanism in ferroptosis. Therefore, this work provides a potential strategy of targeting TAMs for ferroptosis-based TNBC therapy."

Journal • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer

SLC7A11 is an unconventional H+ transporter in lysosomes. (PubMed, Cell) - "A candidate screen on an orphan lysosome membrane protein (OLMP) library enabled us to discover that SLC7A11, the protein target of the ferroptosis-inducing compound erastin, mediates a slow lysosomal H+ leak through downward flux of cystine and glutamate, two H+ equivalents with uniquely large but opposite concentration gradients across lysosomal membranes...Correction of abnormal lysosomal acidity restored lysosome homeostasis and prevented ferroptosis. These studies have revealed an unconventional H+ transport conduit that is integral to lysosomal flux of protonatable metabolites to regulate lysosome function, ferroptosis, and Parkinson's disease (PD) pathology."

Journal • CNS Disorders • Movement Disorders • Parkinson's Disease • SLC7A11

Glutathione Decreases Parkinsonism-Induced Ferroptosis and Oxidative Stress Through the Inhibition of the TRPM2 Channel in Neuronal Cells. (PubMed, Pharmacol Res Perspect) - "The SH-SY5Y cells were divided into six groups: control, MPP, MPP + erastin, MPP + erastin + ferrostatin-1, MPP + erastin + glutathione (GSH), and MPP + erastin + TRPM2 blocker (ACA)...In conclusion, the increase in death and ferroptosis in parkinsonism (MPP)-induced SH-SY5Y cells was attributed to TRPM2 activation. By regulating cytosolic oxidant/antioxidant balance, GSH regulates TRPM2 channel activity and lowers neuronal death and ferroptosis."

Journal • CNS Disorders • Movement Disorders • Parkinson's Disease

Matrine Alleviates Atherosclerosis by Targeting REG1A and Activating the PI3K/AKT/mTOR Pathway to Inhibit Endothelial Cell Ferroptosis. (PubMed, Biochem Genet) - "In addition, both LY294002 (an inhibitor of the PI3K signaling) and Erastin (an inducer of ferroptosis) reversed the alleviation of matrine treatment on ferroptosis in ox-LDL treated HUVECs. The results in vivo showed that matrine treatment inhibited high-fat diet-induced aortic ferroptosis in ApoE-/- mice and alleviated arterial tissue lesions. In summary, matrine inhibits ferroptosis by targeting REG1A to activate PI3K/Akt/mTOR pathway, thereby alleviating aortic endothelial injury and lipid plaque formation in AS mice, suggesting that matrine has potential value for the treatment of AS."

Journal • Atherosclerosis • Cardiovascular • Oncology • APOE • REG1A

Dapagliflozin activates the RAP1B/NRF2/GPX4 signaling and promotes mitochondrial biogenesis to alleviate vascular endothelial ferroptosis. (PubMed, Cell Signal) - "Dapagliflozin significantly decreased the iron and malondialdehyde levels and the release of inflammatory factors in HUVECs treated with oxidized low-density lipoprotein or Erastin but increased the superoxide dismutase activity and the reduced glutathione / oxidized glutathione ratio. When mitochondrial oxidative phosphorylation was pharmacologically inhibited, ferroptosis was reactivated, promoting atherosclerotic plaque formation. In conclusion, this study demonstrated that dapagliflozin activates the RAP1B/NRF2/GPX4 signaling pathway and promotes mitochondrial biogenesis, thereby alleviating vascular endothelial ferroptosis."

Journal • Atherosclerosis • Cardiovascular • Congestive Heart Failure • Dyslipidemia • Heart Failure • Hematological Disorders • APOE • GPX4

Deubiquitinating enzyme UCHL1 stabilizes CAV1 to inhibit ferroptosis and enhance docetaxel resistance in nasopharyngeal carcinoma. (PubMed, Anticancer Drugs) - "Additionally, treatment with the ferroptosis inducer erastin could counteract the effects of CAV1 overexpression on drug resistance. UCHL1 interacted with CAV1 and inhibited its ubiquitin-mediated degradation pathway. By deubiquitinating CAV1, UCHL1 stabilizes and increases its expression, which inhibits ferroptosis and enhances the resistance of NPC cells to docetaxel."

Journal • Nasopharyngeal Carcinoma • Oncology • Solid Tumor • Targeted Protein Degradation • CAV1 • UCHL1

Inhibition of LPL suppresses the osteoclast differentiation of bone-marrow-derived macrophages by promoting the ACSL4 ubiquitination. (PubMed, Int Immunopharmacol) - "Suppression of LPL inhibits the osteoclast differentiation of BMMs in vitro. The mechanism may be related to the LPL knockdown induced USP14 meidated the ACSL4 ubiquitination. Taken together, down-regulation of LPL may be a promising method to suppress osteoclast differentiation to treat osteoporosis."

Journal • Osteoporosis • Rheumatology • Targeted Protein Degradation • ACSL4 • CSF1 • CTSK • LPL • USP14

Hsa_circ_0001944 Regulates FXR/TLR4 Pathway and Ferroptosis to Alleviate Nickel Oxide Nanoparticles-Induced Collagen Formation in LX-2 Cells. (PubMed, Toxics) - "To investigate the regulatory relationship among FXR, TLR4 and ferroptosis, we treated LX-2 cells with FXR agonist (GW4064), TLR4 inhibitor (TAK-242) and ferroptosis agonist (Erastin) combined with NiONPs. Overexpression of hsa_circ_0001944 increased FXR level, reduced TLR4 level, increased the ferroptosis features and alleviated collagen deposition in LX-2 cells. In summary, we demonstrated that hsa_circ_0001944 regulates the FXR/TLR4 pathway and ferroptosis alleviate collagen formation induced by NiONPs."

IO biomarker • Journal • Fibrosis • Hepatology • Immunology • Liver Cirrhosis

ETV4/ALYREF-mediated glycolytic metabolism through PKM2 enhances resistance to ferroptosis and promotes the development of intrahepatic cholangiocarcinoma. (PubMed, Cancer Metab) - "ETV4 promotes ICC development and ferroptosis resistance by facilitating glycolytic metabolism, and regulating PKM2 transcription by directly binding to the PKM2 promoter. Additionally, it mediates m5C-dependent PKM2 stabilization by directly binding to ALYREF. This study identified a new potential therapeutic target for ICC."

Journal • Biliary Cancer • Cholangiocarcinoma • Hepatocellular Cancer • Hepatology • Liver Cancer • Oncology • Solid Tumor • ALYREF • ETV4 • PKM

Pharmacological Inhibitors of Glutamate Transport and Metabolism Suppress Oxidative Phosphorylation in Invasive Lobular Carcinoma (ENDO 2025) - "Studies were conducted in four ILC cell lines (SUM44, LCCTam, MM134, MM134-LTED) treated with three pharmacological inhibitors: Riluzole (glutamate release inhibitor); R162 (inhibitor of glutamate dehydrogenase 1, GLUD1, which converts glutamate to aKG); and erastin (inhibitor of the glutamate:cystine antiporter xCT)...Treatment with erastin significantly increased free NADH levels in ETS cells (SUM44) and the two cell lines that are resistant to Tamoxifen (LCCTam, MM134), but not in MM134-LTED, a model of aromatase inhibitor resistance...Future studies will determine whether combination therapies of GLUD1 inhibitors with ET will have superior anti-cancer efficacy compared to ET alone.*. .*"

Breast Cancer • Estrogen Receptor Positive Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor

Inhibition of VSMC Ferroptosis Mitigates Pathological Vascular Remodeling: A Novel Therapeutic Strategy for Abdominal Aortic Aneurysm. (PubMed, J Cardiovasc Transl Res) - "Additionally, the ferroptosis inducer erastin and Ang II can both promoted pathological remodeling of abdominal aortic rings, but Fer-1 significantly suppressed these effects...Mechanistically, RNA-sequencing analysis revealed that Fer-1 regulates VSMC contractile function, suppresses inflammation, and mitigates extracellular matrix remodeling. These findings highlight the critical role of VSMC ferroptosis in AAA pathogenesis and demonstrate that ferroptosis inhibition effectively reduces pathological vascular remodeling, making it a promising therapeutic strategy for preventing AAA."

Journal • Cardiovascular • Inflammation