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Ferrostatin-1 (Fer-1) Ferroptosis inhibitor

Cat.No.S7243

Ferrostatin-1 (Fer-1) is a potent and selective inhibitor of ferroptosis with EC50 of 60 nM.
Ferrostatin-1 (Fer-1) Ferroptosis inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 262.35

Quality Control

Products Often Used Together with Ferrostatin-1 (Fer-1)

RSL3

It and RSL3 combination significantly inhibit NCX4040 cytotoxicity in colorectal cancer (CRC) cells, HT-29/HCT 116.

Z-VAD-FMK

It and Z-VAD-FMK combination block the cell viability inhibited by CAY10566 in ovarian cancer cell lines OVCAR-5.

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human IMR32 neuroblastoma cells Function assay 13 h 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, IC50=0.018 μM 26696014
HT1080 cells Function assay Antiferroptotic activity in human HT1080 cells assessed as inhibition of erastin-induced cell death by Alamar blue assay, IC50=0.095 μM 26696014
HRE cells Cell viability assay 1 μM 48-72 hours Induction of cell apoptosis 30794682
U57810 and C2C12 cells Cell viability assay 10 μM 24, 48, and 72 h Administration of ferrostatin-1 almost completely prevented the ferroptotic cell death. 29971532
Leishmania major Friedlin clone V1 Antileishmanial assay 72 h LD50 = 28.75 μM 26410073
IMR32 Function assay 1 h IC50 = 0.033 μM 30354101
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 262.35 Formula

C15H22N2O2

Storage (From the date of receipt)
CAS No. 347174-05-4 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CCOC(=O)C1=CC(=C(C=C1)NC2CCCCC2)N

Solubility

In vitro
Batch:

DMSO : 55 mg/mL (209.64 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 55 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
Ferroptosis [1]
(HT-1080 cells)
60 nM(EC50)
In vitro

Ferrostatin-1 (Fer-1) (2 μM) prevents erastin-induced ferroptosis in cancer cells, as well as glutamate-induced cell death in postnatal rat brain slices. It is a lipid ROS scavenger, with the N-cyclohexyl moiety serving as a lipo-philic anchor within biological membranes. This compound does not inhibit extracellular signal -regulated kinase (ERK) phos-phorylation or arrest the proliferation of HT-1080 cells, suggesting that it does not inhibit the MEK/ERK pathway, chelate iron, or inhibit protein synthesis. It does, however, prevent erastin-induced accumulation of cytosolic and lipid ROS. Ferrostatin-1 readily oxidizes the stable radical 2,2-diphenyl-1-picrylhydrazyl (DPPH) under cell-free conditions. [1]

In vivo

Ferrostatin-1 (Fer-1), a synthetic antioxidant, is a potent and selective inhibitor of ferroptosis. It acts via a reductive mechanism to prevent damage to membrane lipids and thereby inhibits cell death.[2]

References

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