A4371-1ml | Ferrostatin-1 (Fer-1) [347174-05-4] Clinisciences

Background

Ferrostatin-1 is a selective inhibitor of ferroptosis.

Ferroptosis is a regulated, oxidative, nanapoptotic cell death, Ferrostatin-1 has been founded as a potent inhibitor of it. Fer-1 can attenuate oxidative, iron-dependent cancer cell death through blocking cystine import and glutathione production. It had been reported to prevent Huntington's disease cellular models to death by inhibiting lipid peroxidation.[1]

Reference:
1. Skouta, R., et al., Ferrostatins inhibit oxidative lipid damage and cell death in diverse disease models. J Am Chem Soc, 2014. 136(12): p. 4551-6.

Product Citation

1. Qiang Wang, et al. "Verteporfin induces lipid peroxidation and ferroptosis in pancreatic cancer cells." Free Radic Biol Med. 2024 Feb 20:212:493-504. PMID: 38184120
2. Zhijing He, He Zhou, et al. "A bimetallic dual-targeting nanoplatform for combinational ferroptosis activation/epigenetic regulation/photothermal therapy against breast cancer and tumor microenvironment remodeling." Chemical Engineering Journal Volume 479, 1 January 2024, 147466.
3. Siyu Zhang, Huihan Yu, et al. "Copper homeostasis based on Cuproptosis-related signature optimizes molecular subtyping and treatment of glioma." Research Square. 28 Dec, 2023.
4. Mingchao Mu, Qin Zhang, et al. "3-Bromopyruvate overcomes cetuximab resistance in human colorectal cancer cells by inducing autophagy-dependent ferroptosis." Cancer Gene Ther. 2023 Aug 9. PMID: 37558749
5. Yu Zhang, Xiyou Du, et al. "A Vanadium-Based Nanoplatform Synergizing Ferroptotic-like Therapy with Glucose Metabolism Intervention for Enhanced Cancer Cell Death and Antitumor Immunity." ACS Nano. 2023 Jun 5. PMID: 37272777
6. Fan Zhang, Lixiang Wu, et al. "FHOD1 is upregulated in glioma cells and attenuates ferroptosis of glioma cells by targeting HSPB1 signaling." CNS Neurosci Ther. 2023 Nov;29(11):3351-3363. PMID: 37211949
7. Shibin Ding, Jinjin Jiang, et al. "Ambient particulate matter exposure plus chronic ethanol ingestion exacerbates hepatic fibrosis by triggering the mitochondrial ROS-ferroptosis signaling pathway in mice." Ecotoxicol Environ Saf. 2023 May:256:114897. PMID: 37043943
8. Qingyu Zhang, Ning Li, et al. "ACSL1-induced ferroptosis and platinum resistance in ovarian cancer by increasing FSP1 N-myristylation and stability." Cell Death Discov. 2023 Mar 8;9(1):83. PMID: 36882396
9. Dong S, Zheng L, et al. "Loss of Lactate/Proton Monocarboxylate Transporter 4 Induces Ferroptosis via the AMPK/ACC Pathway and Inhibition of Autophagy on Human Bladder Cancer 5637 Cell Line" J Oncol 2023;2023 PMID: 36718218
10. Kempen CG, Deragon MA, et al. "Necroptosis of Lung Epithelial Cells Triggered by Ricin Toxin and Bystander Inflammation." Cell Physiol Biochem 2023 Jan 25;57(1) PMID: 36695077
11. Jiawen Cui, Qin Zhou, Chintada Nageswara Rao, et al. "4-tert-butylphenol triggers common carp hepatocytes ferroptosis via oxidative stress, iron overload, SLC7A11/GSH/GPX4 axis, and ATF4/HSPA5/GPX4 axis." Ecotoxicol Environ Saf. 2022 Sep 1;242:113944. PMID: 35926411
12. Li Cai, Xiaoqing Hu, et al. "Long non-coding RNA ADAMTS9-AS1 attenuates ferroptosis by Targeting microRNA-587/solute carrier family 7 member 11 axis in epithelial ovarian cancer." Bioengineered. 2022 Apr;13(4):8226-8239. PMID: 35311457
13. Tingting Liao, Xia Xu, et al. "DJ-1 upregulates the Nrf2/GPX4 signal pathway to inhibit trophoblast ferroptosis in the pathogenesis of preeclampsia." Sci Rep. 2022 Feb 21;12(1):2934. PMID: 35190654
14. QING SHI, RUI LIU, et al. "Ferroptosis inhibitor ferrostatin‑1 alleviates homocysteine‑induced ovarian granulosa cell injury by regulating TET activity and DNA methylation." Mol Med Rep. 2022 Apr;25(4):130. PMID: 35169856
15. Xinxin Ren, Xiang Wang, et al. "Integrative bioinformatics and experimental analysis revealed TEAD as novel prognostic target for hepatocellular carcinoma and its roles in ferroptosis regulation." Aging (Albany NY). 2022 Jan 25;14(2):961-974. PMID: 35077390
16. Amjad Ali, Jasmin Shafarin, et al. "Co-targeting BET bromodomain BRD4 and RAC1 suppresses growth, stemness and tumorigenesis by disrupting the c-MYC-G9a-FTH1axis and downregulating HDAC1 in molecular subtypes of breast cancer." Int J Biol Sci. 2021 Oct 25;17(15):4474-4492. PMID: 34803511
17. Zongbo Wei, Caili Hao, et al. "Aging lens epithelium is susceptible to ferroptosis." Free Radic Biol Med. 2021 May 1;167:94-108. PMID: 33722625
18. Junting Xiao, Shanshan Zhang, et al. "Arsenite induces ferroptosis in the neuronal cells via activation of ferritinophagy." Food Chem Toxicol. 2021 May;151:112114. PMID: 33722599
19. Yue Yang, yuanyuan Lu, et al. "Identification of A New Kind of Phenazine Compounds Attenuating The Stemness of Breast Cancer Cells Through Triggering Ferroptosis." Research Square. March 1st, 2021.
20. Binghua Liu, Weiyan Wang, et al. "Sodium iodate induces ferroptosis in human retinal pigment epithelium ARPE-19 cells." Cell Death Dis. 2021 Mar 3;12(3):230. PMID: 33658488
21. Zhuo Sun, Yidan Cao, et al. "Antiangiogenic effect of arsenic trioxide in HUVECs by FoxO3a‐regulated autophagy." J Biochem Mol Toxicol. 2021 Feb 16;e22728. PMID: 33592126
22. Xinzhi Yang, Jiangang Liu, et al. "miR-18a promotes glioblastoma development by down-regulating ALOXE3-mediated ferroptotic and anti-migration activities." Oncogenesis. 2021 Feb 12;10(2):15. PMID: 33579899
23. Ali Ghoochani, En-Chi Hsu, et al. "Ferroptosis inducers are a novel therapeutic approach for advanced prostate cancer." Cancer Res. 2021 Mar 15;81(6):1583-1594. PMID: 33483372
24. Qi Wang, Yaxun Guo, et al. "RNA binding protein DAZAP1 promotes HCC progression and regulates ferroptosis by interacting with SLC7A11 mRNA." Exp Cell Res. 2021 Feb 1;399(1):112453. PMID: 33358859
25. Xia Qin, Qianghu Tang, et al. "Zinc Oxide Nanoparticles Induce Ferroptotic Neuronal Cell Death in vitro and in vivo." Int J Nanomedicine. 2020 Jul 27;15:5299-5315. PMID: 32884256
26. Tianshu Wu, Xue Liang, et al. "Induction of ferroptosis in response to graphene quantum dots through mitochondrial oxidative stress in microglia." Particle and Fibre Toxicology volume 17, Article number: 30 (2020).11 July 2020.
27. Meng P, Zhang S, et al. "Arsenite induces testicular oxidative stress in vivo and in vitro leading to ferroptosis." Ecotoxicol Environ Saf. 2020;194:110360. PMID: 32151864
28. Hu Z, Zhang H, et al. "VDR activation attenuate cisplatin induced AKI by inhibiting ferroptosis." Cell Death Dis. 2020;11(1):73. Published 2020 Jan 29. PMID: 31996668
29. Zhou HH, Chen X, et al. "Erastin Reverses ABCB1-Mediated Docetaxel Resistance in Ovarian Cancer." Front Oncol, 9, 1398 2019 Dec PMID: 31921655
30. Xiaohong Zhang, Xueshuang Xing, et al. "Ionizing radiation induces ferroptosis in granulocyte-macrophage hematopoietic progenitor cells of murine bone marrow." Int J Radiat Biol , 1-35 2020 Jan 6. PMID: 31906761
31. Wang H, Liu C, et al. "Inhibition of LONP1 protects against erastin-induced ferroptosis in Pancreatic ductal adenocarcinoma PANC1 cells." Biochem Biophys Res Commun. 2019 Dec 7. pii: S0006-291X(19)32315-0. PMID: 31822343

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Chemical Properties

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	262.35
Cas No.	347174-05-4
Formula	C₁₅H₂₂N₂O₂
Solubility	≥149 mg/mL in DMSO; ≥99.6 mg/mL in EtOH with ultrasonic; insoluble in H2O
SDF	Download SDF
Canonical SMILES	NC1=C(NC2CCCCC2)C=CC(C(OCC)=O)=C1
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:
Cell lines	Healthy medium spiny neurons, oligodendrocytes, kidney proximal tubules cell
Preparation method	The solubility of this compound in DMSO is >9.8mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reacting condition	10 nM, 100 nM, and 1 μM
Applications	Fer-1 (10 nM, 100 nM, and 1 μM) significantly increased the number of healthy MSNs. Fer-1 (1 μM) statistically increased the number of healthy MSN. Fer-1 (100 nM) fully protected oligodendrocytes from cystine deprivation. Fer-1 (0.1-2 μM) prevented lethality induced by hydroxyquinoline and ferrous ammonium sulfate (HQ + Fe; 10 μM each).
Other notes	Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References: [1]. Skouta R, Dixon S J, Wang J, et al. Ferrostatins inhibit oxidative lipid damage and cell death in diverse disease models[J]. Journal of the American Chemical Society, 2014, 136(12): 4551-4556.

Biological Activity

Description	Ferrostatin-1 is a selective inhibitor of erastin induced ferroptosis with EC50 value of 60 nM.
Targets	erastin induced ferroptosis
IC50	60 nM (EC50)