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Ferroptosis: A Key Regulator in Cancer Therapy and Beyond

Cell Programmed Death Cell Death & Disease

Ferroptosis, a form of regulated cell death characterized by iron dependence and lipid peroxidation, has emerged as a critical player in various physiological and pathological processes. Initially identified in the context of cancer chemotherapy resistance, its role has since expanded significantly, positioning it as a key regulator not only in cancer therapy but also in a multitude of other diseases and biological contexts [1].

The dysregulation of ferroptosis has been implicated in cancer progression, where cancer cells often develop mechanisms to evade this death pathway, contributing to tumor growth and metastasis. Conversely, inducing ferroptosis in cancer cells represents a promising therapeutic strategy to overcome resistance and enhance treatment efficacy . Small molecules that promote ferroptosis, such as erastin and RSL3, have demonstrated potent anticancer effects in preclinical models, highlighting the potential of targeting this pathway for cancer therapy [2].

Beyond oncology, ferroptosis has been linked to neurodegenerative diseases, including Alzheimer’s and Parkinson’s disease, where oxidative stress and iron accumulation contribute to neuronal damage. In cardiovascular diseases, ferroptosis has been implicated in ischemia-reperfusion injury, a major cause of complications following heart attacks and strokes. Additionally, ferroptosis plays a role in inflammatory diseases and has been associated with the pathogenesis of acute kidney injury. The broad implications of ferroptosis underscore its importance as a therapeutic target across multiple disease areas. Recent advances in understanding the molecular mechanisms underlying ferroptosis have led to the development of novel compounds that can either induce or inhibit this form of cell death, offering new avenues for drug discovery. As research continues to unravel the complexities of ferroptosis, its significance as a key regulator in cancer therapy and beyond is expected to grow, paving the way for innovative therapeutic strategies[3][4].

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Cat. No. Product Name Information Application Publication
HY-100579 Ferrostatin-1
Ferrostatin-1 (Fer-1), a potent and selective ferroptosis inhibitor, suppresses Erastin-induced ferroptosis in HT-1080 cells (EC50=60 nM). Ferrostatin-1, a synthetic antioxidant, acts via a reductive mechanism to prevent damage to membrane lipids and thereby inhibits cell death. Ferrostatin-1 exhibits antifungal activity.
Ferroptosis   Fungal  
Cancer   Fungal Infection  
1785
HY-15763 Erastin
Erastin is a ferroptosis inducer. Erastin exhibits the mechanism of ferroptosis induction related to ROS and iron-dependent signaling. Erastin inhibits voltage-dependent anion channels (VDAC2/VDAC3) and accelerates oxidation, leading to the accumulation of endogenous reactive oxygen species. Erastin also disrupts mitochondrial permeability transition pore (mPTP) with anti-tumor activity. Furthermore, Erastin can block the uptake of cystine mediated by SLC7A11 and also spares UMRC6-EV and -C91A cells from disulfidptosis under glucose starvation.
VDAC   Ferroptosis   Disulfidptosis  
Cancer  
907
HY-17394 Cisplatin
Cisplatin (CDDP) is an antineoplastic chemotherapy agent by cross-linking with DNA and causing DNA damage in cancer cells. Cisplatin activates ferroptosis and induces autophagy.
DNA Alkylator/Crosslinker   Ferroptosis   Autophagy   Pyroptosis   Lipoxygenase  
Non-Small Cell Lung Cancer   Lung Adenocarcinoma   Lung Squamous Cell Carcinoma   Large Cell Lung Carcinoma   Triple-Negative Breast Cancer   Metastatic Breast Cancer  
862
HY-16658B Z-VAD-FMK
Z-VAD-FMK is a pan-caspase inhibitor and also an ICE-like protease inhibitor, which inhibits apoptosis by preventing the processing of CPP32 to its active form. Z-VAD-FMK sensitivity varies primarily due to differential expression of receptor-interacting protein 1 (RIP1). Z-VAD-FMK limits the cryopreservation-induced apoptosis by reducing caspase-3 activity of in vitro produced bovine embryos. Z-VAD-FMK is immunosuppressive in vitro and inhibits T cell proliferation without blocking the processing of caspase-8 and caspase-3. Z-VAD-FMK leads to a decrease in intracellular glutathione (GSH) with a concomitant increase in reactive oxygen species (ROS) levels in activated T cells. Z-VAD-FMK is due to oxidative stress via the depletion of GSH. Z-VAD-FMK can be used for the study of acute pancreatitis.
Caspase   Apoptosis   RIP kinase   Glutathione Peroxidase   Reactive Oxygen Species (ROS)  
Cancer   Digestive System Disease   Pancreatitis  
853
HY-B0215 Acetylcysteine
Acetylcysteine (N-Acetylcysteine) is a mucolytic agent that can cross the blood-brain barrier, which reduces the thickness of the mucus. Acetylcysteine is a ROS inhibitor. Acetylcysteine is a cysteine precursor, prevents hemin-induced ferroptosis by neutralizing toxic lipids generated by arachidonate-dependent activity of 5-lipoxygenases. Acetylcysteine induces cell apoptosis. Acetylcysteine also has anti-influenza virus activities. In addition, Acetylcysteine ​​is the most stable form of cysteine ​​during drug delivery and can be used in disulfidptosis studies.
Reactive Oxygen Species (ROS)   Endogenous Metabolite   Apoptosis   Ferroptosis   Influenza Virus   Disulfidptosis  
Neurological, Eye or Ear Disease   Digestive System Disease   Breast Cancer   Viral Infection   Digestive System Inflammation   SARS-CoV-2 Infection   Lung Fibrosis  
767
HY-100523 ML385
ML385 is a potent and selective Nrf2 inhibitor with an IC50 of 1.9 μM. ML385 directly binds to the Neh1 domain of NRF2, interferes with the binding of the MAFG-NRF2 protein complex to the antioxidant response element (ARE) DNA sequence, thereby blocking the expression of downstream target genes of NRF2. ML385 can be used in studies related to adult T-cell leukemia, breast cancer, myocardial ischemia/reperfusion injury, non-small cell lung cancer, esophageal squamous cell carcinoma, head and neck squamous cell carcinoma, and lung squamous cell carcinoma.
Keap1-Nrf2   Ferroptosis   Apoptosis   mTOR  
Breast Cancer   Colorectal Cancer   Cardiovascular Disease   Non-Small Cell Lung Cancer   Lung Squamous Cell Carcinoma   Squamous Cell Carcinoma   Esophageal Cancer  
645
HY-12041 SP600125
SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 induces the transformation of bladder cancer cells from autophagy to apoptosis.
JNK   Autophagy   Apoptosis   Ferroptosis  
Cancer   Digestive System Disease   Depression   Pain   Digestive System Inflammation   Parkinson's Disease   Obesity   Lung Fibrosis  
628
HY-15760 Necrostatin-1
Necrostatin-1 (Nec-1) is a potent and cross the blood-brain barrier necroptosis inhibitor with an EC50 of 490 nM in Jurkat cells. Necrostatin-1 inhibits RIP1 kinase (EC50=182 nM). Necrostatin-1 is also an IDO inhibitor.
RIP kinase   Autophagy   Indoleamine 2,3-Dioxygenase (IDO)   Ferroptosis   Necroptosis  
Cancer   Neurological, Eye or Ear Disease   Digestive System Disease   Digestive System Inflammation  
576
HY-100218A RSL3
RSL3 ((1S,3R)-RSL3) is an inhibitor of glutathione peroxidase 4 (GPX4) (ferroptosis activator), reduces the expression of GPX4 protein, and induces ferroptotic death of head and neck cancer cell. RSL3 increases the expression of p62 and Nrf2 and inactivates Keap1 in HN3-rslR cells.
p62   Glutathione Peroxidase   Ferroptosis   Reactive Oxygen Species (ROS)  
Ovarian Cancer  
575
HY-10201 Sorafenib
Sorafenib (Bay 43-9006) is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib inhibits tumor growth and metastasis in mouse and rat models. Sorafenib can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.
Raf   VEGFR   FLT3   Autophagy   Apoptosis   STAT   Akt   MMP   Cadherin   p38 MAPK   ERK   MEK   PI3K   PARP   Bcl-2 Family   Ephrin Receptor   PDGFR  
Gastric Cancer   Liver Cancer   Ovarian Cancer   Digestive System Inflammation   Small Cell Lung Cancer   Non-Small Cell Lung Cancer   Metastatic Breast Cancer   Metastatic Colorectal Cancer   Metastatic Prostate Cancer   Multiple Myeloma   Metastatic Pancreatic Cancer   SARS-CoV-2 Infection   Alzheimer's Disease   Parkinson's Disease   Obesity   Lung Fibrosis  
317
HY-12726 Liproxstatin-1
Liproxstatin-1 is a potent ferroptosis inhibitor and inhibits ferroptotic cell death (IC50=22 nM).
Ferroptosis  
Cancer   Neurological, Eye or Ear Disease  
263
HY-17386 Rosiglitazone
Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM), with blood-brain barrier permeability. Rosiglitazone is an TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer.
PPAR   TRP Channel   Autophagy   Ferroptosis   Apoptosis  
Digestive System Disease   Prostate Cancer   Ovarian Cancer   Viral Infection   Depression   Pain   Digestive System Inflammation   Non-Small Cell Lung Cancer   SARS-CoV-2 Infection   Type 2 Diabetes   Obesity  
197
HY-D1301 BODIPY 581/591 C11
BODIPY 581/591 C11 is a BODIPY borofluoroprene derivative with good light stability and low fluorescence artifacts. BODIPY 581/591 C11 can be used for study lipid peroxidation and antioxidant properties in living cells, or detect ferroptosis by reaction with hydroxyl radicals. BODIPY 581/591 C11 is emitted at 591 nm (reduced prototype), or redshifted to 510 nm (oxidized type). The excitation wavelengths were 581 nm (reduced prototype) and 500 nm (oxidized type).
Fluorescent Dye   Ferroptosis  
Cancer   Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
167
HY-L051 Ferroptosis Compound Library
Ferroptosis is a novel type of cell death program that is distinct from apoptosis, necroptosis and autophagy. It is dependent on iron and reactive oxygen species (ROS) and is characterized by lipid peroxidation. As a novel type of cell death, ferroptosis has distinct properties and recognizing functions involved in physical conditions or various diseases including cancers, neurodegenerative diseases, acute renal failure, etc. MCE carefully collected a unique collection of 1,255 ferroptosis signaling pathway related compounds with ferroptosis-inducing or -inhibitory activity. MCE Ferroptosis Compound Library is a useful tool to study ferroptosis mechanism as well as related diseases.

Signaling Pathway Targeting Libraries

84
HY-L162 Cell Death Library
Cell death plays a crucial role in the development of the body and the maintenance of internal balance to prevent the development of diseases. According to the regulation of the involved processes, cell death can be defined as programmed and non-programmed death. Programmed cell death (PCD) can be divided into lytic cell death and nonlytic cell death, mainly including apoptosis, necrotic apoptosis and Pyroptosis. Non-Programmed cell death (Non-PCD) generally refers to necrosis. In stark contrast to Accidental Cell Death (ACD), Regulatory Cell Death (RCD) relies on specialized molecular mechanisms. Cell death includes internal apoptosis, external apoptosis, necrotic apoptosis, ferroptosis, pyroptosis, lysosome-dependent cell death, etc. MCE designs a unique collection of 3,860 cell death compounds, covering multiple targets, such as Apoptosis, Ferroptosis, Pyroptosis, Necroptosis, etc. It is a useful tool for screening cell death drugs.

Compound Characteristic Classified Libraries

83
HY-112654 GCN2iB
GCN2iB is an ATP-competitive, selective GCN2 inhibitor with an IC50 of 2.4 nM. GCN2iB inhibits the activation of the GCN2 pathway and upregulates GPX4. GCN2iB enhances the anticancer effect of ASNase against acute lymphoblastic leukemia. GCN2iB increases left ventricular ejection fraction, while reducing fasting blood glucose and myocardial fibrosis. GCN2iB can be used in research related to acute lymphoblastic leukemia, acute myeloid leukemia and diabetic cardiomyopathy.
Eukaryotic Initiation Factor (eIF)   Glutathione Peroxidase  
Glucose Metabolism   Acute Myeloid Leukemia   Acute Lymphoblastic Leukemia   Cardiomyopathy  
65
HY-D1913 Fe2Orange
Fe2Orange is a Fe2+ selective probe with an excitation wavelength of 543 nm and an emission wavelength of 580 nm. Fe2Orange emits fluorescence after binding to intracellular Fe2+, thereby achieving specific labeling of Fe2+. Fe2Orange is used to detect the content and distribution of Fe2+ in cells.
Fluorescent Dye  
36
HY-100003 ML-210
ML-210 is a selective and covalent glutathione peroxidase 4 (GPX4) inhibitor with an EC50 of 30 nM. ML-210 binds the GPX4 selenocysteine residue. ML-210 has anti-cancer activity.
Glutathione Peroxidase   Ferroptosis  
Ovarian Cancer  
33
HY-14909 Bardoxolone
Bardoxolone (CDDO; RTA 401) is a Nrf2 activator. Bardoxolone shows anti-SARS-CoV-2 3CLpro with IC50 of 27.99 μM. Bardoxolone activates the Nrf2 pathway and inhibits the NF-κB pathway. Bardoxolone can induce cells differentiation, apoptosis and shows antiproliferative activity against cancer cells. Bardoxolone can increase ROS and decrease intracellular GSH levels. Bardoxolone inhibits Z-VAD-FMK (HY-16658B)-induced necroptosis. Bardoxolone can be used for the research of cancer, inflammation and infection, such as SARS-CoV infection and glioblastoma.
Keap1-Nrf2   NF-κB   SARS-CoV   Apoptosis   Reactive Oxygen Species (ROS)   Glutathione Peroxidase   Necroptosis  
Inflammation or Immune System Disease   Glioblastoma   SARS-CoV-2 Infection  
25
HY-N0171A Beta-Sitosterol (purity>98%)
Beta-Sitosterol (purity>98%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc.
Bacterial   Apoptosis   Reactive Oxygen Species (ROS)   MDM-2/p53   Caspase   PARP   MMP   Bcl-2 Family   HIF/HIF Prolyl-Hydroxylase   TNF Receptor   Interleukin Related   NF-κB   mTOR   Lactate Dehydrogenase   CDK   Glutathione Peroxidase   SOD  
Lung Cancer   Breast Cancer   Prostate Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Bacterial Infection   Depression   Pain   Digestive System Inflammation   Cardiovascular Disease   Glucose Metabolism   Obesity   Lung Fibrosis   Rheumatoid Arthritis  
25
HY-100002 ML162
ML162 is a covalent glutathione peroxidase 4 (GPX4) inhibitor. ML162 has a selective lethal effect on mutant RAS oncogene-expressing cell lines
Glutathione Peroxidase   Ferroptosis  
Ovarian Cancer  
18
HY-K0320 ROS Assay Kit

MCE ROS Assay Kit utilizes the fluorescent probe DCFH-DA to detect ROS.

Cell Biology Cell Analysis Metabolism Assay Kit

15
HY-112005 DOPE
DOPE (Dioleoylphosphatidylethanolamine; 1,2-Dioleoyl-sn-glycero-3-phosphoethanolamine) is an orally active inhibitor of ferroptosis with anti-inflammatory and intestinal barrier maintenance activities. DOPE regulates the expression of ACSL4, SLC7A11 and GPX4 to restore the redox system balance, thereby reducing the levels of lipid peroxides, iron ions and intestinal inflammatory factors (IL-1β and IL-6). DOPE promotes the migration and proliferation of intestinal epithelial cells and increases the level of tight junction proteins; it also destabilizes endosomal membranes, mediates the conjugation of RVG peptides with mesenchymal stem cell-derived exosomes to enhance brain targeting. DOPE can be applied to research related to neonatal necrotizing enterocolitis and Alzheimer's disease.
Liposome   Endogenous Metabolite   ACSL Family   Amino acid Transporter   Ferroptosis   Glutathione Peroxidase  
Cancer   Inflammation or Immune System Disease  
14
HY-K0319 Lipid Peroxidation (MDA) Assay Kit

MCE Lipid Peroxidation (MDA) Assay Kit is suitable for measuring MDA levels in a variety of samples including plasma, serum, urine, tissues or cell lysates.

Cell Biology Cell Analysis Metabolism Assay Kit

10
HY-B0388 Probucol
Probucol (DH-581) is an anti-hyperlipidemic agent. Probucol activates glutathione peroxidase. Probucol promotes low density lipoprotein (LDL) catabolism, inhibits ABCA1-dependent cholesterol efflux, and decreases HDL-C levels. Probucol also has anti-inflammatory, antioxidant and neuroprotective properties. Probucol can be used for researches on bone, cardiovascular, cancer, neurological, and metabolism-related diseases.
Virus Protease   Apoptosis   Reactive Oxygen Species (ROS)   Glutathione Peroxidase   Caspase  
Cancer   Neurological, Eye or Ear Disease   Digestive System Disease   Viral Infection   Digestive System Inflammation   Glucose Metabolism  
5
HY-Y0669 Pipecolic acid
Pipecolic acid is an orally bioavailable, blood-brain barrier-permeable metabolite of lysine with antioxidant, inhibitor, and inducer activity. Pipecolic acid modulates the YAP-GPX4 signaling pathway, reduces retinal vascular tube formation, and mitigates ferroptosis. Pipecolic acid potentiates voltage-sensitive Ca2+ channel currents and induces neuronal apoptosis. Pipecolic acid can be used for the research of diabetic retinopathy.
Endogenous Metabolite   YAP   Glutathione Peroxidase   Ferroptosis  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
2
HY-151212 BCP-T.A
BCP-T.A, a tunable heterocyclic electrophile, is a potent ferroptosis inducer by binding to GPX4. BCP-T.A is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Ferroptosis   Glutathione Peroxidase  
Cancer  
/
HY-P99139 Anti-Mouse IL-1b Antibody (B122)
Anti-Mouse IL-1b Antibody (B122) is an anti-mouse IL-1b IgG monoclonal antibody. Anti-Mouse IL-1b Antibody (B122) enhances ferroptosis and increases levels of reactive oxygen species (ROS) combined with Sulfasalazine (SAS) (HY-14655). Anti-Mouse IL-1b Antibody (B122) can reduce monocyte infiltration and alleviate T cell exhaustion by blocking IL-1β signaling. Anti-Mouse IL-1b Antibody (B122) can be used for researches on cancer and cardiovascular conditions such as oral squamous cell carcinoma (OSCC), glioblastoma (GBM) and heart failure.

Species: Mouse

Interleukin Related   Reactive Oxygen Species (ROS)   Ferroptosis  
Blood or Cardio-cerebrovascular Disease   Glioma  
/