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MedChemExpressModel Ferrostatin-1 -347174-05-4

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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].
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Ferrostatin-1

MCE China:Ferrostatin-1

Brand:MedChemExpress (MCE)

Cat. No.HY-100579

CAS:347174-05-4

Synonyms:Fer-1

Purity:99.71%

Storage:4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Shipping:Room temperature in continental US; may vary elsewhere.

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.

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].

IC50 & Target:EC50: 60 nM (Ferroptosis)[1] Cellular Effect Cell Line Type Value Description References

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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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