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

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 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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1 mg * 5 USD 115 In-stock
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Customer Review

Based on 419 publication(s) in Google Scholar

Other Forms of Erastin:

Erastin Related Antibodies

Top Publications Citing Use of Products

MedChemExpress Activity Verification

Above results were obtained through MCE biological verification.

408 Publications Citing Use of MCE Erastin

Cell Viability Assay
Proliferation Assay
WB
IF

    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: 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: 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]

    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. 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. 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

    • Customer Review

    Description

    Erastin is a ferroptosis inducer. 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].
    Note:
    1. Different cell lines may have different sensitivity to a same compound. As reported, A549, HCT116, HepG2, H1299 cells may be insensitive to Erastin[3][4][5].
    2. Erastin is unstable in solution. Freshly prepared is recommended.

    Ferroptosis-sensitive Cell Lines

    Ferroptosis-sensitive Cells Test Conditions
    SKOV3[6] 5-20 μM; 1-7 days
    OVCA429[6] 5-20 μM; 1-7 days
    MCF10A-RAS[7] 0-30 μM; 48 h
    HT-22 neuron[8] 500 nM; 16 h
    NCI-H508[9] 0.1-10 μM; 48 h
    LoVo[9] 0.1-10 μM; 48 h
    LS513[9] 0.1-10 μM; 48 h
    SW480[9] 0.1-10 μM; 48 h
    SW620[9] 0.1-10 μM; 48 h
    SW1116[9] 0.1-10 μM; 48 h
    DLD-1[9] 0.1-10 μM; 48 h
    Caco-2[9] 0.1-10 μM; 48 h
    SW837[10] 0-40 μM; 24 h
    Pfa1[11] 0.1-5 μM; 48 h
    HT-1080[12] 0.1-5 μM; 48 h
    MAD-MB-231[13] 0-100 μM; 72 h; IC50: 9.55 μM
    HCC1937[13] 0-100 μM; 72 h; IC50: 11.58 μM


    Ferroptosis-insensitive Cell Lines
    Ferroptosis-insensitive Cells Test Conditions
    HCT116[11] 0-40 μM; 24 h
    SW48[11] 0-40 μM; 24 h
    HepG2[5] 0-20 μM; 24 h
    MDA-MB-436[13] 0.1-25 μM; 24 h
    HT-29[13] 0.1-25 μM; 24 h
    U-373[13] 0.1-25 μM; 24 h

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

    Erastin Related Antibodies

    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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    Volume (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

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

      This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

    • Protocol 2

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

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

      This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

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

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
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    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.76%

    COA (250 KB) HNMR (308 KB) LCMS (267 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.8280 mL 9.1401 mL 18.2802 mL 45.7005 mL
    5 mM 0.3656 mL 1.8280 mL 3.6560 mL 9.1401 mL
    10 mM 0.1828 mL 0.9140 mL 1.8280 mL 4.5700 mL
    15 mM 0.1219 mL 0.6093 mL 1.2187 mL 3.0467 mL
    20 mM 0.0914 mL 0.4570 mL 0.9140 mL 2.2850 mL
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    Erastin Related Classifications

    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.

    Keywords:

    Erastin571203-78-6VDACFerroptosisVoltage-dependent anion channel Inhibitorinhibitorinhibit

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