Ferrostatin-1 (Fer-1) Chemical Structure

Ferrostatin-1 (Fer-1) Chemical Structure
Molecular Weight: 262.35

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Product Information

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Product Description

Biological Activity

Description Ferrostatin-1 (Fer-1) is a potent and selective inhibitor of ferroptosis with EC50 of 60 nM.
Targets Ferroptosis [1]
IC50 60 nM(EC50)
In vitro Ferrostatin-1 (2 μM) prevents erastin-induced ferroptosis in cancer cells, as well as glutamate-induced cell death in postnatal rat brain slices. Ferrostatin-1 is a lipid ROS scavenger, with the N-cyclohexyl moiety serving as a lipo-philic anchor within biological membranes. Ferrostatin-1 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. Ferrostatin-1 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
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Dixon SJ, et al. Cell, 2012, 149(5), 1060-1072..

Chemical Information

Download Ferrostatin-1 (Fer-1) SDF
Molecular Weight (MW) 262.35
Formula

C15H22N2O2

CAS No. 347174-05-4
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 52 mg/mL (198.2 mM)
Ethanol 52 mg/mL (198.2 mM)
Water <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Benzoic acid, 3-amino-4-(cyclohexylamino)-, ethyl ester

Customer Product Validation (1)


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Source Oncogene, 2015, 10.1038/onc.2015.32. Ferrostatin-1 (Fer-1) purchased from Selleck
Method Cell Viability Assay
Cell Lines HeLa cells、U2OS cells
Concentrations 1 μM
Incubation Time 24 h
Results Treatment with deferoxamine (an iron-chelating agent) and ferrostain-1 (an inhibitor of ferroptosis) prevented erastin-induced growth inhibition in HSF1 and HSPB1 knockdown HeLa (Figure k) and U2OS (Figure l) cells. Thus, these findings indicate that the inhibition of HSF1-dependent HSPB1 expression specifically increased erastin-induced ferroptosis but not other types of cell death (for example, apoptosis, necrosis and necroptosis) in cancer cells.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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