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^[1][2][3]. IC50 & Target:EC50: 60 nM (Ferroptosis)^[1] In Vitro:Ferrostatin-1 prevents erastin-induced accumulation of cytosolic and lipid ROS. Ferrostatin-1 prevents glutamate-induced neurotoxicity in organotypic rat brain slices^[1].
Ferrostatin-1 (2 μM; 24 h) prevents Glutamate (5 mM)-induced neurotoxicity in a rat organotypic hippocampal slice culture (OHSC)^[2].
Ferrostatin-1 inhibits lipid peroxidation, but not mitochondrial reactive oxygen species formation or lysosomal membrane permeability^[2].
Ferrostatin-1 inhibits cell death in cellular models of Huntington's disease (HD), periventricular leukomalacia (PVL), and kidney dysfunction^[2].
Ferrostatin-1 (1 μM; 6 h) inhibits the oxidative destruction of unsaturated fatty acids in HT-1080 cells, thus increases the number of healthy medium spiny neurons (MSNs)^[3].


Ferroptosis-sensitive Cell Lines

Ferroptosis-sensitive Cells	Ferrostatin-1 Experimental Conditions	Ferroptosis Inducers
HT-1080[1]	0.5 μM; 24 h; EC50=60 nM	Erastin (10 nM-100 μM; 24 h)
BEAS-2B[4]	2 μM; 16 h	LPS (10 mg/L; 16 h)
PC12 (differentiated)[5]	1 μM; 12 h	Erastin (7.5 μM; 12 h)
N27 neuron[8]	0.004-0.25 μM; 24 h; EC50=0.039 μM	RSL3 (1 μM; 24 h)
BMSCs[9]	1 μM; 24 h	GSDH (10-50 μM; 24 h)
HT-22[10]	3-12 μM; 16 h	Glutamate (5 mM; 16 h)
HK‑2[11]	100 μM; 24 h	Oxalate (2 mM; 24 h)
MLE12[12]	1 and 5 μM; 24 h	8% and 20% cyclic stretching (CS)
HaCaT[13]	10 μM	UVB (20mJ/cm2)
Mouse primary astrocytes[14]	0.1-2 μM; 24 h	Angiotensin II (10 μM; 24 h)
SKOV3[15]	5 μM; 24 h	Erastin (10 μM; 24 h)
OVCA429[15]	10 μM; 24 h	Erastin (20 μM; 24 h)
HK-2 WT[16]	Pretreatment with 2 μM followed by co-treatment with inducers	RSL3 (0.01-1 μM; 8 h)
MDA-MB-468[16]	Pretreatment with 2 μM for 1 h was performed, followed by co-treatment with the inducer	RSL3 (500 nM; 2 h)
NCI-H1299[16]	Pretreatment with 2 μM followed by co-treatment with inducers	Erastin (5 μM; 18 h)
HT22 neuron[17]	Cells were pretreated with the inducer and then co-treated with 10 and 20 μM Ferrostatin-1 for 6, 12, or 24 h	Erastin (0 and 5 μM; 12 h)
HT22 neuron[18]	Pretreatment with 2 μM for 30 min was performed, followed by co-treatment with the inducer for 24 h	Erastin (1 μM; 24 h)
HT-1080[19]	0.5 μM; 12 h	Erastin (10 μM; 12 h)
H1975[20]	Pretreatment with 2 μM for 14 h followed by co-treatment with the inducer for 24 h	RSL3 (1 μM; 6 or 24 h)
A549[20]	Pretreatment with 2 μM for 14 h followed by co-treatment with the inducer for 24 h	RSL3 (1 μM; 6 or 24 h)

In Vivo:Ferrostatin-1 (5 mg/kg; ip; single dose, 30 min before glycerol injection) improves renal function in mice with rhabdomyolysis, whereas no beneficial effects were observed with the pan-caspase inhibitor zVAD or in RIPK3-deficient mice^[1].
Ferrostatin-1 (0.8 mg/kg; tail vein injection) effectively alleviates LPS-induced induced acute lung injury (ALI)^[4].
Ferrostatin-1 (i.p.; 5 mg/kg; C57BL/6J mice) improves renal function in mice with rhabdomyolysis^[5].
Ferrostatin-1 (10 mg/kg/d, i.p., 3 d) attenuates hypoxic-ischemic brain damage-, oxygen-glucose deprivation-, or Erastin (HY-15763)-induced ferroptosis in brain of neonatal rats^[6].
Ferrostatin-1 (0.655 mg/kg, i.p., 3 times a week for 6 week) exerts anti-ferroptosis effects by increasing GPX4 activity and by inhibiting lipid peroxidation in the salivary gland of ovariectomized (postmenopausal model) rats^[7].