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Ferrostatin-1 [347174-05-4]

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Cat# HY-100579-5mg

Size : 5mg

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Description

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]

Cellular Effect

Cell Line	Type	Value	Description	References
Fibroblast	EC₅₀	33 nM Compound: Fer-1	Inhibition of erastin-induced cell death in FRDA patient-derived fibroblast assessed as depletion of cellular ATP incubated for 12 hrs followed by erastin stimulation and measured after by luciferase-linked ATPase enzymatic assay Inhibition of erastin-induced cell death in FRDA patient-derived fibroblast assessed as depletion of cellular ATP incubated for 12 hrs followed by erastin stimulation and measured after by luciferase-linked ATPase enzymatic assay	[PMID: 33214825]
HT-1080	EC₅₀	0.07 μM Compound: Fer-1	Anti-ferroptotic activity against Erastin-induced ferroptosis in human HT-1080 cells assessed as cell activity measured after 24 hrs by Cell Titer-Glo luminescent assay Anti-ferroptotic activity against Erastin-induced ferroptosis in human HT-1080 cells assessed as cell activity measured after 24 hrs by Cell Titer-Glo luminescent assay	[PMID: 35300093]
HT-1080	EC₅₀	0.088 μM Compound: Fer-1	Inhibition of erastin-induced ferroptosis in human HT-1080 cells assessed as cell viability incubated for 48 hrs by MTT assay Inhibition of erastin-induced ferroptosis in human HT-1080 cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 33065375]
HT-1080	IC₅₀	95 nM Compound: 1; fer-1	Antiferroptotic activity in human HT1080 cells assessed as inhibition of erastin-induced cell death by Alamar blue assay Antiferroptotic activity in human HT1080 cells assessed as inhibition of erastin-induced cell death by Alamar blue assay	[PMID: 26696014]
HT-22	EC₅₀	81.2 nM Compound: Fer-1	Anti-ferroptotic activity against RSL3-induced ferroptosis in human HT-22 cells assessed as cell viability measured after 24 hrs by MTT assay Anti-ferroptotic activity against RSL3-induced ferroptosis in human HT-22 cells assessed as cell viability measured after 24 hrs by MTT assay	[PMID: 35796002]
IMR-32	IC₅₀	18 nM Compound: 1; fer-1	Antiferroptotic activity in human IMR32 neuroblastoma cells assessed as inhibition of erastin-induced cell death preincubated for 1 hr before erastin stimulation and measured after 13 hrs by fluorescence plate reader method Antiferroptotic activity in human IMR32 neuroblastoma cells assessed as inhibition of erastin-induced cell death preincubated for 1 hr before erastin stimulation and measured after 13 hrs by fluorescence plate reader method	[PMID: 26696014]
IMR-32	IC₅₀	33 nM Compound: 1; Fer-1	Inhibition of erastin-induced ferroptosis in human IMR32 cells preincubated for 1 hr followed by erastin stimulation and measured after 13 hrs by sytox green-based fluorescence assay Inhibition of erastin-induced ferroptosis in human IMR32 cells preincubated for 1 hr followed by erastin stimulation and measured after 13 hrs by sytox green-based fluorescence assay	[PMID: 30354101]
LLC-MK2	IC₅₀	> 240 μM Compound: AA1	Cytotoxicity against monkey LLC-MK2 cells after 96 hrs by Alamar Blue assay Cytotoxicity against monkey LLC-MK2 cells after 96 hrs by Alamar Blue assay	[PMID: 26410073]
Lymphocyte	EC₅₀	48 nM Compound: Fer-1	Anti-ferroptotic activity in FRDA patient-derived Lymphocyte assessed as reduction in RSL3-induced lipid peroxidation incubated for overnight followed by RSL3 stimulation and measured after 90 mins by FACS analysis Anti-ferroptotic activity in FRDA patient-derived Lymphocyte assessed as reduction in RSL3-induced lipid peroxidation incubated for overnight followed by RSL3 stimulation and measured after 90 mins by FACS analysis	[PMID: 33214825]
NIH3T3	IC₅₀	0.22 μM Compound: Fer-1	Inhibition of TBHP-induced ferroptosis in mouse NIH/3T3 cells after 12 hrs by WST-8 assay Inhibition of TBHP-induced ferroptosis in mouse NIH/3T3 cells after 12 hrs by WST-8 assay	[PMID: 31531196]
NIH3T3	IC₅₀	0.27 μM Compound: Fer-1	Inhibition of erastin-induced ferroptosis in mouse NIH/3T3 cells after 24 hrs by WST-8 assay Inhibition of erastin-induced ferroptosis in mouse NIH/3T3 cells after 24 hrs by WST-8 assay	[PMID: 31531196]
RAW264.7	EC₅₀	0.04 μM Compound: Fer-1	Anti-ferroptotic activity against RSL-3 induced ferroptosis in mouse RAW264.7 cells assessed as cell activity measured after 24 hrs by Cell Titer-Glo luminescent assay Anti-ferroptotic activity against RSL-3 induced ferroptosis in mouse RAW264.7 cells assessed as cell activity measured after 24 hrs by Cell Titer-Glo luminescent assay	[PMID: 35300093]

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)

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male C57BL/6 mice (LPS-induced ALI)^[4]
Dosage:	0.8 mg/kg
Administration:	Tail vein injection
Result:	Exerted therapeutic action against LPS-induced ALI.

Molecular Weight

262.35

Formula

C₁₅H₂₂N₂O₂

CAS No.

347174-05-4

Appearance

Solid

Color

Gray to gray purple

SMILES

O=C(OCC)C1=CC=C(NC2CCCCC2)C(N)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (476.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.8117 mL	19.0585 mL	38.1170 mL
5 mM	0.7623 mL	3.8117 mL	7.6234 mL
10 mM	0.3812 mL	1.9059 mL	3.8117 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (7.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (7.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (7.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 10% DMSO 90% Saline
Solubility: 0.2 mg/mL (0.76 mM); Clear solution; Need ultrasonic

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 5 mg/mL (19.06 mM); Suspended solution; Need ultrasonic

Purity & Documentation

Purity: 99.96%

Data Sheet (287 KB) SDS (393 KB)

COA (245 KB) HNMR (269 KB) LCMS (267 KB) Elemental Analysis Report (103 KB)

Handling Instructions (2659 KB)

References

[1]. Dixon SJ, et al. Ferroptosis: an iron-dependent form of nonapoptotic cell death. Cell. 2012;149(5):1060-1072. [Content Brief]

[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. [Content Brief]

[3]. Horwath MC, et al. Antifungal Activity of the Lipophilic Antioxidant Ferrostatin-1. Chembiochem. 2017;18(20):2069-2078. [Content Brief]

[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. [Content Brief]

[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.

[6]. Zhang M, et al. Ferrostatin-1 attenuates hypoxic-ischemic brain damage in neonatal rats by inhibiting ferroptosis. Transl Pediatr. 2023 Nov 28;12(11):1944-1970. [Content Brief]

[7]. Cheon YI, et al. Effect of deferoxamine and ferrostatin-1 on salivary gland dysfunction in ovariectomized rats. Aging (Albany NY). 2023 Apr 6;15(7):2418-2432. [Content Brief]

[8]. Morrow J P, et al. Poly (2-oxazoline)–Ferrostatin-1 drug conjugates inhibit ferroptotic cell death[J]. Journal of Controlled Release, 2022, 350: 193-203. [Content Brief]

[9]. Xie Q, et al. Ferrostatin-1 improves BMSC survival by inhibiting ferroptosis[J]. Archives of Biochemistry and Biophysics, 2023, 736: 109535. [Content Brief]

[10]. Chu J, et al. Ferrostatin-1 protects HT-22 cells from oxidative toxicity[J]. Neural regeneration research, 2020, 15(3): 528-536. [Content Brief]

[11]. Xie J, et al. Ferrostatin‑1 alleviates oxalate‑induced renal tubular epithelial cell injury, fibrosis and calcium oxalate stone formation by inhibiting ferroptosis[J]. Molecular Medicine Reports, 2022, 26(2): 1-12. [Content Brief]

[12]. Ling M, et al. Ferrostatin-1 alleviates ventilator-induced lung injury by inhibiting ferroptosis[J]. International Immunopharmacology, 2023, 120: 110356. [Content Brief]

[13]. Y Teng, et al. "Ferrostatin 1 ameliorates UVB‐induced damage of HaCaT cells by regulating ferroptosis." Experimental Dermatology 33.2 (2024): e15018. [Content Brief]

[14]. Li S, et al. Ferrostatin-1 alleviates angiotensin II (Ang II)-induced inflammation and ferroptosis in astrocytes[J]. International immunopharmacology, 2021, 90: 107179. [Content Brief]

[15]. Liu N, et al. Activation of the reverse transsulfuration pathway through NRF2/CBS confers erastin-induced ferroptosis resistance[J]. British journal of cancer, 2020, 122(2): 279-292. [Content Brief]

[16]. Zhang Z, et al. CGI1746 targets σ1R to modulate ferroptosis through mitochondria-associated membranes[J]. Nature Chemical Biology, 2024, 20(6): 699-709. [Content Brief]

[17]. Hanke N, et al. Inhibition of autophagy rescues HT22 hippocampal neurons from erastin-induced ferroptosis[J]. Neural regeneration research, 2023, 18(7): 1548-1552. [Content Brief]

[18]. Wang X, et al. Melatonin alleviates acute sleep deprivation-induced memory loss in mice by suppressing hippocampal ferroptosis[J]. Frontiers in pharmacology, 2021, 12: 708645. [Content Brief]

[19]. Du J, et al. Identification of Frataxin as a regulator of ferroptosis[J]. Redox biology, 2020, 32: 101483. [Content Brief]

[20]. Cheff D M, et al. The ferroptosis inducing compounds RSL3 and ML162 are not direct inhibitors of GPX4 but of TXNRD1[J]. Redox Biology, 2023, 62: 102703. [Content Brief]

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Ferrostatin-1 [347174-05-4]

Cat# HY-100579-5mg

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