Ferrostatin-1 (Fer-1), Ferroptosis Inhibitor

Ferrostatin-1 (Fer-1) is a potent inhibitor of ferroptosis with an EC50 ~60 nM, identified by a HTS using erastin-induced ferroptosis in HT-1080 cells. Ferroptosis is a unique iron-dependent form of nonapoptotic cell death triggered by the oncogenic RAS-selective lethal small molecule erastin. Ferroptosis is dependent upon intracellular iron, but not other metals, and is morphologically, biochemically, and genetically distinct from apoptosis, necrosis, and autophagy. Ferrostatin-1 was shown to inhibit ferroptosis in cancer cells, and also glutamate-induced cell death in organotypic rat brain slices. Studies revealed that erastin blocks cystine uptake via inhibition of the cystine/glutamate antiporter, resulting in a defect in the cell’s antioxidative defenses and ultimately leading to an iron-dependent, oxidative cell death (i.e., ferroptosis). Ferrostatin-1 was characterized to prevent erastin-induced accumulation of cytosolic and lipid ROS. Ferrostatin-1 serves as a very useful tool to dissect ferroptosis in cancer and many other cell types, and may provide new opportunities to protect tissues and organs from damages resulted from ferroptosis under diseases (such as neurodegeneration).

Product information

CAS Number: 347174-05-4

Molecular Weight: 262.35

Formula: C15H22N2O2

Chemical Name: ethyl 3-amino-4-(cyclohexylamino)benzoate

Smiles: CCOC(=O)C1=CC(N)=C(C=C1)NC1CCCCC1

InChiKey: UJHBVMHOBZBWMX-UHFFFAOYSA-N

InChi: InChI=1S/C15H22N2O2/c1-2-19-15(18)11-8-9-14(13(16)10-11)17-12-6-4-3-5-7-12/h8-10,12,17H,2-7,16H2,1H3

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 52 mg/mL(198.2 mM). Water: Insoluble.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

Ferrostatin-1 (Fer-1) prevents erastin-induced accumulation of cytosolic and lipid ROS. Ferrostatin-1 prevents glutamate-induced neurotoxicity in organotypic rat brain slices. Fer-1 inhibited lipid peroxidation, but not mitochondrial reactive oxygen species formation or lysosomal membrane permeability.

In Vivo:

Ferrostatin-1 inhibits cell death in cellular models of Huntington's disease (HD), periventricular leukomalacia (PVL), and kidney dysfunction. Ferrostatin-1 (0.8 mg/kg; tail vein injection) effectively alleviated LPS-induced induced acute lung injury (ALI). Ferrostatin-1 (i.p.; 5 mg/kg; C57BL/6J mice) improves renal function in mice with rhabdomyolysis.

References:

1. Dixon SJ, et al. Ferroptosis: an iron-dependent form of nonapoptotic cell death. Cell. 2012;149(5):1060-1072.
2. Skouta R, Dixon SJ, Wang J, et al. Ferrostatins inhibit oxidative lipid damage and cell death in diverse disease models. J Am Chem Soc. 2014;136(12):4551-4556.
3. Horwath MC, et al. Antifungal Activity of the Lipophilic Antioxidant Ferrostatin-1. Chembiochem. 2017;18(20):2069-2078.
4. Liu P, Feng Y, et al. Ferrostatin-1 alleviates lipopolysaccharide-induced acute lung injury via inhibiting ferroptosis. Cell Mol Biol Lett. 2020;25:10. Published 2020 Feb 27.
5. Melania Guerrero Hue, et al. FP282 FERROPTOSIS-MEDIATED CELL DEATH IS DECREASED BY CURCUMIN IN RENAL DAMAGE ASSOCIATED TO RHABDOMYOLYSIS, Nephrology Dialysis Transplantation, Volume 34, Issue Supplement_1, June 2019, gfz106.FP282.

Products are for research use only. Not for human use.