Ferrostatin-1 is a potent ferroptosis inhibitor (EC50: 60 nM).

Ferrostatin-1 (Fer-1) is the most potent inhibitor of erastin-induced ferroptosis in HT-1080 cells (EC50=60 nM). Ferrostatin-1 did prevent erastin-induced accumulation of cytosolic and lipid ROS [1]. Ferrostatin-1 inhibited cell death in cellular models of Huntington's disease (HD), periventricular leukomalacia (PVL), and kidney dysfunction; Fer-1 inhibited lipid peroxidation, but not mitochondrial reactive oxygen species formation or lysosomal membrane permeability [2]. Fer-1 is not toxic toward the SH-SY5Y cells at concentrations up to 12.5 μM. Fer-1 compound quenched the commercially available stable radical DPPH, in non-cellular assay at 82 %. Fer-1 inhibited the ROS/RNS generated under rotenone insult in SH-SY5Y cells [3].

Cell viability was typically assessed in 384-well format by Alamar Blue fluorescence (ex/em 530/590) measured on a Victor3 plate reader. In some experiments, Trypan Blue dye exclusion counting was performed using an automated cell counter. Cell viability under test conditions is reported as a percentage relative to the negative control treatment [1].

347174-05-4

C15H22N2O2

262.353

Ferrostatin 1;Ferrostatin-1 (Fer-1);Ferrostatin-1

[1]Kabiraj P, et al. The neuroprotective role of ferrostatin-1 under rotenone-induced oxidative stress in dopaminergic neuroblastoma cells. Protein J. 2015 Oct;34(5):349-58. [2]Chen X, Gao C, Cheng Z, et al. Ruxolitinib exerts neuroprotection via repressing ferroptosis in a mouse model of traumatic brain injury[J]. Experimental Neurology. 2021: 113762. [3]Wang S, Li F, Qiao R, et al. Arginine-Rich Manganese Silicate Nanobubbles as a Ferroptosis-Inducing Agent for Tumor-Targeted Theranostics[J]. ACS nano. 2018 Dec 26;12(12):12380-12392. [4]Su G, Yang W, Wang S, et al. SIRT1-autophagy axis inhibits excess iron-induced ferroptosis of foam cells and subsequently increases IL-1Β and IL-18[J]. Biochemical and Biophysical Research Communications. 2021, 561: 33-39. [5]Dixon SJ, et al. Ferroptosis: an iron-dependent form of nonapoptotic cell death. Cell. 2012 May 25;149(5):1060-72. [6]Skouta R, et al. Ferrostatins inhibit oxidative lipid damage and cell death in diverse disease models. J Am Chem Soc. 2014 Mar 26;136(12):4551-6. [7]Yin W, Luan X, Li Z, et al. Structural basis for inhibition of the SARS-CoV-2 RNA polymerase by suramin[J]. Nature Structural & Molecular Biology. 2021: 1-7. [8]Sun Y, He L, Wang T, et al. Activation of p62-Keap1-Nrf2 Pathway Protects 6-Hydroxydopamine-Induced Ferroptosis in Dopaminergic Cells[J]. Molecular Neurobiology. 2020, 57(11): 4628-4641.

[1]Wang S, Li F, Qiao R, et al. Arginine-Rich Manganese Silicate Nanobubbles as a Ferroptosis-Inducing Agent for Tumor-Targeted Theranostics. ACS nano. 2018 Dec 26;12(12):12380-12392. [2]Luo Y, Gao X, Zou L, et al. Bavachin Induces Ferroptosis through the STAT3/P53/SLC7A11 Axis in Osteosarcoma Cells. Oxidative Medicine and Cellular Longevity. 2021 [3]Jiang H, Wang C, Zhang A, et al. ATF4 protects against sorafenib-induced cardiotoxicity by suppressing ferroptosis. Biomedicine & Pharmacotherapy. 2022, 153: 113280 [4]Yu S, Li Z, Zhang Q, et al. GPX4 degradation via chaperone-mediated autophagy contributes to antimony-triggered neuronal ferroptosis. Ecotoxicology and Environmental Safety. 2022, 234: 113413. [5]Zhou Y, Wu H, Wang F, et al. GPX7 Is Targeted by miR-29b and GPX7 Knockdown Enhances Ferroptosis Induced by Erastin in Glioma. Frontiers in oncology. 2021, 11: 802124-802124. [6]Li J, Chen S, Huang J, et al. New Target in an Old Enemy: Herbicide (R)-Dichlorprop Induces Ferroptosis-like Death in Plants. Journal of Agricultural and Food Chemistry. 2021 [7]Zhao Y, Lu J, Mao A, et al. Autophagy Inhibition Plays a Protective Role in Ferroptosis Induced by Alcohol via the p62–Keap1–Nrf2 Pathway. Journal of Agricultural and Food Chemistry. 2021 [8]Tan Q, Fang Y, Peng X, et al. A new ferroptosis inhibitor, isolated from Ajuga nipponensis, protects neuronal cells via activating NRF2-antioxidant response elements (AREs) pathway. Bioorganic Chemistry. 2021: 105177. [9]Ning X, Qi H, Yuan Y, et al. Identification of a new small molecule that initiates ferroptosis in cancer cells by inhibiting the system Xc? to deplete GSH. European Journal of Pharmacology. 2022: 175304. [10]Kong R, Wang N, Han W, et al. IFNγ‐mediated repression of system xc? drives vulnerability to induced ferroptosis in hepatocellular carcinoma cells. Journal of Leukocyte Biology. 2021, 110(2): 301-314.

Ethanol:26.2 mg/mL (100 mM)
DMSO:200 mg/mL (762.3 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years