Erastin

Catalog No.S7242 Batch:S724205

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Technical Data

Formula

C30H31ClN4O4
Molecular Weight 547.04 CAS No. 571203-78-6
Solubility (25°C)* In vitro DMSO (warmed with 50ºC water bath) 15 mg/mL (27.42 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Erastin is a ferroptosis activator by acting on mitochondrial VDAC, exhibiting selectivity for tumor cells bearing oncogenic RAS. Solutions are unstable and should be fresh-prepared.
Targets
Ferroptosis [1]
In vitro

Erastin is selectively lethal to oncogenic RAS-mutant cell lines, and triggers a unique iron-dependent form of non-apoptotic cell death called ferroptosis. [1] [2]

Erastin binds directly to VDAC2 and causes mitochondrial damage via ROS production in an NADH-dependent manner, which induces cell death in some tumor cells harbouring activating mutations in the RAS-RAF-MEK pathway. [3]

In addition, erastin, via inducing ROS-mediated CID (Caspase-independent cell death), strongly enhances the effect of cisplatin in WT EGFR cells. [4]
In vivo

Erastin is a ferroptosis activator by inhibiting voltage-dependent anion channels (VDAC2/VDAC3). It also inhibits cystine-glutamate antiporter (xCT).[5]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    BJ-TERT/LT/ST/RASV12 cells

  • Concentrations

    5 or 10 μg/mL

  • Incubation Time

    6-11 hours

  • Method

    BJ-TERT/LT/ST/RASV12 cells are seeded in 100 mm dishes and allowed to grow overnight. Cells are treated with erastin (5 or 10 μg/ml) for 6, 8, or 11 hr. A camptothecin-treated (0.4 μg/ml) control is maintained, treated at the time of seeding for 20 hours. After the treatment, cells are harvested with trypsin/EDTA and washed once with fresh medium containing serum and then twice with phosphate-buffered saline. Cells are resuspended in 1× binding buffer. 100 μL is incubated with 5 μL of Annexin V-FITC and propidium iodiode for 15 min in the dark at room temperature. Then 400 μl of the 1× binding buffer s added and the cells analyzed by flow cytometry. Data are acquired and analyzed using Cellquest software. Only viable cells that do not stain with propidium iodiode are analzyed for Annexin V-FITC staining using the FL1 channel.
Animal Study:

[5]

 
  • Animal Models

    C57BL/6 mice

  • Dosages

    10 mg/kg

  • Administration

    i.n.

Customer Product Validation

, , Cancer Res, 2017, 77(8):2064-2077

Data from [Data independently produced by , , Gastroenterology, 2017, 153(5):1429-1443]

Data from [Data independently produced by , , Gastroenterology, 2018, 154(5):1480-1493]

Data from [Data independently produced by , , Hepatology, 2016, 64(2):488-500.]

Selleck's Erastin has been cited by 369 publications

Pro-ferroptotic signaling promotes arterial aging via vascular smooth muscle cell senescence [ Nat Commun, 2024, 15(1):1429] PubMed: 38365899
HiHo-AID2: boosting homozygous knock-in efficiency enables robust generation of human auxin-inducible degron cells [ Genome Biol, 2024, 25(1):58] PubMed: 38409044
Excessive SOX8 reprograms energy and iron metabolism to prime hepatocellular carcinoma for ferroptosis [ Redox Biol, 2024, 69:103002] PubMed: 38142583
Meningioma achieves malignancy and erastin-induced ferroptosis resistance through FOXM1-AURKA-NRF2 axis [ Redox Biol, 2024, 72:103137] PubMed: 38642502
SPTBN2 suppresses ferroptosis in NSCLC cells by facilitating SLC7A11 membrane trafficking and localization [ Redox Biol, 2024, 70:103039] PubMed: 38241838
Differentiation of intestinal stem cells toward goblet cells under systemic iron overload stress are associated with inhibition of Notch signaling pathway and ferroptosis [ Redox Biol, 2024, 72:103160] PubMed: 38631120
Hspb1 protects against severe acute pancreatitis by attenuating apoptosis and ferroptosis via interacting with Anxa2 to restore the antioxidative activity of Prdx1 [ Int J Biol Sci, 2024, 20(5):1707-1728] PubMed: 38481805
Caspase-2 protects against ferroptotic cell death [ Cell Death Dis, 2024, 15(3):182] PubMed: 38429264
Neutrophil extracellular traps mediate cardiomyocyte ferroptosis via the Hippo-Yap pathway to exacerbate doxorubicin-induced cardiotoxicity [ Cell Mol Life Sci, 2024, 81(1):122] PubMed: 38456997
Salidroside pretreatment alleviates ferroptosis induced by myocardial ischemia/reperfusion through mitochondrial superoxide-dependent AMPKα2 activation [ Phytomedicine, 2024, 155365] PubMed: none

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.