1. Apoptosis Membrane Transporter/Ion Channel
  2. Ferroptosis VDAC
  3. Erastin

Erastin 

Cat. No.: HY-15763 Purity: 99.72%
COA Handling Instructions

Erastine est un inducteur de ferroptose. Erastine se lie et inhibe les canaux anioniques dépendants de la tension (VDAC2/VDAC3).

Erastin ist ein Ferroptose-Induktor. Erastin bindet und hemmt spannungsabhängige Anionenkanäle (VDAC2/VDAC3).

Erastin is a ferroptosis inducer. Erastin shows selective cytotoxicity, targeting cells expressing oncogenic mutants of RAS. Erastin exhibits the mechanism of ferroptosis induction related to ROS and iron-dependent signaling. Erastin inhibits voltage-dependent anion channels (VDAC2/VDAC3) and accelerates oxidation, leading to the accumulation of endogenous reactive oxygen species. Erastin also disrupts mitochondrial permeability transition pore (mPTP) with anti-tumor activity.

For research use only. We do not sell to patients.

Erastin Chemical Structure

Erastin Chemical Structure

CAS No. : 571203-78-6

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Customer Review

Based on 291 publication(s) in Google Scholar

Other Forms of Erastin:

Top Publications Citing Use of Products

280 Publications Citing Use of MCE Erastin

Cell Viability Assay
WB
Proliferation Assay
IF

    Erastin purchased from MedChemExpress. Usage Cited in: Gene. 2023 May 9;873:147468.  [Abstract]

    Erastin (8, 16 μM; 48 h) reduces the expression of xCT in AGS and BGC-823 cells.

    Erastin purchased from MedChemExpress. Usage Cited in: Gene. 2023 May 9;873:147468.  [Abstract]

    Erastin (8 μM; 48 h) greatly induces apoptosis and cell death in AGS and BGC-823 cells.

    Erastin purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2022 Feb;24(2):168-180.  [Abstract]

    Survival rates of MCF10A-RAS cells cultured on stiff or soft Matrigel and treated for 48 h with Erastin (10-30 μM).

    Erastin purchased from MedChemExpress. Usage Cited in: Redox Biol. 2022 Aug;54:102382.  [Abstract]

    After treatment with Ferrostatin-1 (Fer-1, 5 μM) and GW4064 (1 μM) for 2 h, HK2 cells are treated with Erastin (5 μM) for another 24 h. After treatment with Fer-1 and GW4064, the cells are incubated with C11-BODIPY 581/591 (2 μM) and Hoechst 33258 for counterstaining; the images were then immediately visualized by confocal microscopy.

    Erastin purchased from MedChemExpress. Usage Cited in: Redox Biol. 2022 Aug;54:102382.  [Abstract]

    After treatment with Ferrostatin-1 (Fer-1, 5 μM) and GW4064 (1 μM) for 2 h, HK2 cells are treated with Erastin (5 μM) for another 24 h. Protein levels of GPX4 are detected by immunoblotting.

    Erastin purchased from MedChemExpress. Usage Cited in: Clin Transl Med. 2022 Apr;12(4):e752.  [Abstract]

    Representative images of intracellular mitochondrial superoxide level in SW480 and HT29 cells subjected to the stable knockdown of LINC001606 or stably overexpressing LINC001606 after treatment of DMSO, Erastin (10 μM) and RSL3 (2 μM) for 48 h.

    Erastin purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2020 Sep;27(9):2635-2650.  [Abstract]

    H&E and Masson’s staining of lung tissues show that Erastin (10 μM; tail-injected intravenously; for 20 days) aggravated edema, atelectasis, necrosis, alveolar and interstitial inflammation, and pulmonary fibrosis in I/R mice compared with sham mice, but these effects are reversed in I/R + erastin mice treated with Liproxstatin-1.

    Erastin purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2020 Sep;27(9):2635-2650.  [Abstract]

    Erastin (10 μM; tail-injected intravenously; for 20 days) treatment of I/R mice significantly increases the protein/mRNA levels of TF and significantly decreased the percentage GSH and protein/mRNA levels of FTH1 and GPX4, but these effects are reversed by Liproxstatin-1 treatment.

    Erastin purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2021 Apr;28(4):1222-1236.  [Abstract]

    Western blot analysis of the protein expression levels of BCAT2, AMPK, and pAMPK(T172) in Aspc-1, and HepG2 cells treated with Erastin (20 or 10 μM) Vin the absence or presence of AICAR (AMPK activator, 2 mmol/L) and Compound C (AMPK inhibitor, 1 μmol/L).

    Erastin purchased from MedChemExpress. Usage Cited in: Neurotherapeutics. 2020 Oct;17(4):1796-1812.  [Abstract]

    The effect of an inducer or inhibitor of ferroptosis on PC-12 cells. PC-12 cells are treated with 40 μM 6-OHDA in combination with an inducer (1 μM Erastin) of ferroptosis for 24 h. The expression of GPX4, TH, and FTH1 is significantly reduced in cells treated with the combination of erastin and 6-OHDA compared with those treated with 6-OHDA alone.

    Erastin purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2020 Dec 5;888:173574.  [Abstract]

    With the various dosage of ferroptosis inducer Erastin treatment for 24 h, the cell viability is determined by SRB method.
    • Biological Activity

    • Purity & Documentation

    • References

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    Description

    Erastin is a ferroptosis inducer. Erastin shows selective cytotoxicity, targeting cells expressing oncogenic mutants of RAS. Erastin exhibits the mechanism of ferroptosis induction related to ROS and iron-dependent signaling. Erastin inhibits voltage-dependent anion channels (VDAC2/VDAC3) and accelerates oxidation, leading to the accumulation of endogenous reactive oxygen species. Erastin also disrupts mitochondrial permeability transition pore (mPTP) with anti-tumor activity[1][2][3].

    In Vitro

    Erastin (10 μM; 24 h) triggers ferroptosis in ectopic endometrial stromal cells (EESCs), and increases the total ROS level at 9 h[1].
    Erastin shorts mitochondria and increases membrane density in EESCs[1].
    Erastin (10 μM; 9 h) decreases the mRNA expression levels of iron-related proteins, such FPN (iron exporter) in EESCs. However, FPN overexpression significantly inhibits erastin-induced ferroptosis in EESCs[1].
    Erastin (10 μM; 24 h) induces mitochondrial permeability transition pore (mPTP) opening in HT-29 colorectal cancer cells[2].
    Erastin (30 μM; 72 h) significantly inhibits the growth of HT-29 colorectal cancer cells[2].
    The molecular mechanism by which Erastin induces ferroptosis is related to genes regulating iron or mitochondrial fatty acid metabolism. Includes ribosomal protein L8, iron response element binding protein 2 (IREB2), ATP synthase F0 complex subunit C3, citrate synthase, tetrapeptide repeat domain 35, and acyl-CoA synthetase family member 2 (ACSF2)[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Viability Assay[1]

    Cell Line: Normal endometrial stromal cells (NESCs) and endometrial stromal cells (EESCs)
    Concentration: 0, 0.5, 0.8, 1, 1.5, 2, 2.5, 5, 10 μM
    Incubation Time: 24 hours
    Result: Induced cell detachment and overt death in EESCs, but not NESCs.

    Apoptosis Analysis[1]

    Cell Line: EESCs infected with adenovirus expressing FPN cDNA (co-incubation for 24 hr)
    Concentration: 0, 0.5, 1.5, 2.5, 5 and 2.5 μM
    Incubation Time: 24 hours
    Result: Induced ferroptosis by decreasing the levels of total ROS and lipid ROS. And reversed by the overexpression of FPN in adenovirus-infected cells.
    In Vivo

    Erastin can be used in animal modeling to construct ferroptosis induction model.

    Erastin (40 mg/kg; i.p.; once every 3 days for 2 weeks) suppresses endometriotic implants in the mouse endometriosis model, indicating Erastin regresses ectopic lesions by trigging ferroptosis[1].
    Erastin (10 mg/kg, 30 mg/kg; i.p.; once daily for 4 weeks) suppresses HT-29 xenograft growth in SCID mice, with more potent efficacy under 30 mg/kg treatment[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Mouse model of endometriosis[1]
    Dosage: 40 mg/kg
    Administration: Intraperitoneal injection; once every 3 days for 2 weeks
    Result: Showed little impact on body weight of mice and hair of mice displayed neat and glossy.
    Reduced the volume of ectopic lesions.
    Molecular Weight

    547.04

    Formula

    C30H31ClN4O4

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1N(C2=CC=CC=C2OCC)C(C(N3CCN(C(COC4=CC=C(Cl)C=C4)=O)CC3)C)=NC5=C1C=CC=C5

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years

    *The compound is unstable in solutions, freshly prepared is recommended.

    Solvent & Solubility
    In Vitro: 

    DMSO : 12.5 mg/mL (22.85 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8280 mL 9.1401 mL 18.2802 mL
    5 mM 0.3656 mL 1.8280 mL 3.6560 mL
    10 mM 0.1828 mL 0.9140 mL 1.8280 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 5 mg/mL (9.14 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 1.25 mg/mL (2.29 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1 mg/mL (1.83 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.76%

    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    Erastin
    Cat. No.:
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