1. Apoptosis
  2. Ferroptosis
  3. Imidazole ketone erastin

Imidazole ketone erastin  (Synonyms: IKE)

製品番号: HY-114481 純度: 99.77%
COA 取扱説明書 Technical Support

Imidazole ketone erastin is a potent, selective, and metabolically stable inhibitor of the cystine-glutamate antiporter, system xc- and an activator of ferroptosis. Imidazole ketone erastin has anti-tumor activity.

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CAS 番号 : 1801530-11-9

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 303 在庫あり
Solution
10 mM * 1 mL in DMSO USD 303 在庫あり
Solid
2 mg $110 在庫あり
5 mg $210 在庫あり
10 mg $280 在庫あり
25 mg $500 在庫あり
50 mg $720 在庫あり
100 mg $950 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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カスタマーレビュー

Based on 50 publication(s) in Google Scholar

Other Forms of Imidazole ketone erastin:

Top Publications Citing Use of Products

顧客検証

Cell Proliferation/Viability Assay
Histological Imaging/Staining
In Vivo Efficacy Study

    Imidazole ketone erastin purchased from MedChemExpress. Usage Cited in: Mol Cell. 2025 Aug 7;85(15):2973-2987.e6.  [Abstract]

    KU1919 cells were treated with DMSO or 5 μM tazemetostat for 24 hours, followed by 24-hour treatment with 5 μM imidazole ketone erastin.

    Imidazole ketone erastin purchased from MedChemExpress. Usage Cited in: Mol Cell. 2025 Aug 7;85(15):2973-2987.e6.  [Abstract]

    Imidazole ketone erastin (50 mg/kg, i.p. injection) was administered. Growth curves of tumors derived from KU1919 cells in xenograft mouse models were recorded.

    Imidazole ketone erastin purchased from MedChemExpress. Usage Cited in: Mol Cell. 2025 Aug 7;85(15):2973-2987.e6.  [Abstract]

    Imidazole ketone erastin (50 mg/kg, i.p. injection) was administered. Representative H&E and immunostaining images of Ki67, ACSL4, ETNK1, PTGS2, 4-HNE and SO2/3-PRDX3 were shown from sections of xenograft tumors with indicated treatment. Scale bars: 40 μm.

    Imidazole ketone erastin purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Mar 21;15(1):2531.  [Abstract]

    Cell viability of A549 sgNC re-expressed with vector, sgGAS41 cells re-expressed with vector, GAS41 WT, GAS41 W93A mutant, or GAS41 L211A mutants was treated with imidazole ketone erastin (3 μM, right panel) for 24 h.

    Imidazole ketone erastin purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2022 Apr;3(4):471-485.  [Abstract]

    Imidazole ketone erastin and PPG were used at a concentration of 45 mg/kg/d through intraperitoneal injection. Tumor weight after combination treatment with IKE and PPG was measured.
    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    Imidazole ketone erastin is a potent, selective, and metabolically stable inhibitor of the cystine-glutamate antiporter, system xc- and an activator of ferroptosis. Imidazole ketone erastin has anti-tumor activity[1].

    IC50 & Target

    System Xc-, ferroptosis[1]

    Cellular Effect
    Cell Line Type Value Description References
    CCF-STTG1 IC50
    30 nM
    Compound: IKE
    Inhibition of Xct in human CCF-STTG1 cells assessed as glutamate release after 2 hrs by fluorometry
    Inhibition of Xct in human CCF-STTG1 cells assessed as glutamate release after 2 hrs by fluorometry
    [PMID: 26231156]
    DOHH-2 IC50
    0.014 μM
    Compound: 6; IKE
    Anticancer activity against human DOHH-2 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay
    Anticancer activity against human DOHH-2 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay
    [PMID: 36332549]
    HT-1080 GI50
    314 nM
    Compound: IKE
    Growth inhibition of human HT1080 cells after 48 hrs by alamar blue assay
    Growth inhibition of human HT1080 cells after 48 hrs by alamar blue assay
    [PMID: 26231156]
    SU-DHL-16 IC50
    0.012 μM
    Compound: 6; IKE
    Anticancer activity against human SU-DHL-16 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay
    Anticancer activity against human SU-DHL-16 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay
    [PMID: 36332549]
    SU-DHL-2 IC50
    0.021 μM
    Compound: 6; IKE
    Anticancer activity against human SUDHL2 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay
    Anticancer activity against human SUDHL2 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay
    [PMID: 36332549]
    SU-DHL-5 IC50
    0.001 μM
    Compound: 6; IKE
    Anticancer activity against human SU-DHL-5 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay
    Anticancer activity against human SU-DHL-5 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay
    [PMID: 36332549]
    SU-DHL-6 IC50
    0.001 μM
    Compound: 6; IKE
    Anticancer activity against human SU-DHL-6 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay
    Anticancer activity against human SU-DHL-6 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay
    [PMID: 36332549]
    SU-DHL10 IC50
    0.004 μM
    Compound: 6; IKE
    Anticancer activity against human SU-DHL-10 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay
    Anticancer activity against human SU-DHL-10 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay
    [PMID: 36332549]
    体外実験

    Imidazole ketone erastin (IKE) (0.1 nM-100 μM; 24 h) potently reduces diffuse large B cell lymphoma (DLBCL) cell number by lipid peroxidation and ferroptosis[1].
    IKE (1-250 nM; 24 h) depletes reduced glutathione (GSH) in a dose-dependent manner with an IC50 of 34 nM in SUDHL6 cells[1].
    IKE (125-500 nM) increases lipid ROS in a dose-dependent manner in SUDHL-6 cells[1].
    IKE (500 nM; 5-360 min) increases the system xc component SLC7A11, prostaglandin-endoperoxide synthase 2 (PTGS2), and ChaC glutathione-specific gamma-glutamylcyclotransferase 1 (CHAC1) expression in SUDHL-6 cells[1].
    IKE (500 nM and 1 μM) changes the relative abundance of 62 lipid species including lysophosphatidylcholines (LPC), phosphatidylcholines (PC), phosphatidylethanolamines (PE), and triglycerides (TAGs) in SUDHL6 cells[1].
    IKE (500 nM) activates de novo lipid biosynthesis pathways, phospholipid remodeling pathways, and arachidonic acid oxidation pathways in SUDHL6 cells[1].

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

    体内実験

    IKE (23-40 mg/kg; i.p. once daily for 13 d) inhibits tumor growth in mice[1].
    IKE (50 mg/kg; a single i.p) depletes GSH significantly starting from 4 h, and increases in the relative abundance of free fatty acids, phospholipids, and diacylglycerols (DAG) in mice[1].
    IKE (50 mg/kg) exhibits half-life (1.82, 1.31, and 0.96 h) and Cmax (19515, 11384, and 5203 ng/mL) following different administration (i.p., i.v., and p.o. respectively) in mice[1].

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

    Animal Model: Male NCG mice bearing SUDHL6 subcutaneous xenografts[1]
    Dosage: 23, 40 mg/kg
    Administration: I.p. injection once daily for 13 days
    Result: Caused a significant decrease in tumor growth starting from day 9.
    Had a weight loss starting from day 9.
    Animal Model: NOD/SCID mice (12 weeks old; ~28 g weight)[1]
    Dosage: 50 mg/kg (Pharmacokinetic Analysis)
    Administration: A single i.p., i.v., and p.o. administration
    Result: I.p.: T1/2=1.82 h, Cmax=19515 ng/mL.
    I.v.: T1/2=1.31 h, Cmax=11384 ng/mL.
    P.o.: T1/2=0.96 h, Cmax=5203 ng/mL.
    臨床実験
    分子量

    655.14

    分子式

    C35H35ClN6O5

    CAS 番号
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=C1N(C2=CC(C(CN3C=CN=C3)=O)=CC=C2OC(C)C)C(CN4CCN(C(COC5=CC=C(Cl)C=C5)=O)CC4)=NC6=CC=CC=C61

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件

    4°C, sealed storage, away from moisture and light

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

    溶剤 & 溶解度
    体外: 

    DMSO : 100 mg/mL (152.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5264 mL 7.6320 mL 15.2639 mL
    5 mM 0.3053 mL 1.5264 mL 3.0528 mL
    10 mM 0.1526 mL 0.7632 mL 1.5264 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    一般には略語で表示されます:C1V1 = C2V2

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    体内:

    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (3.82 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (3.82 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    +
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    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

    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.
    純度とドキュメンテーション

    純度: 99.77%

    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.5264 mL 7.6320 mL 15.2639 mL 38.1598 mL
    5 mM 0.3053 mL 1.5264 mL 3.0528 mL 7.6320 mL
    10 mM 0.1526 mL 0.7632 mL 1.5264 mL 3.8160 mL
    15 mM 0.1018 mL 0.5088 mL 1.0176 mL 2.5440 mL
    20 mM 0.0763 mL 0.3816 mL 0.7632 mL 1.9080 mL
    25 mM 0.0611 mL 0.3053 mL 0.6106 mL 1.5264 mL
    30 mM 0.0509 mL 0.2544 mL 0.5088 mL 1.2720 mL
    40 mM 0.0382 mL 0.1908 mL 0.3816 mL 0.9540 mL
    50 mM 0.0305 mL 0.1526 mL 0.3053 mL 0.7632 mL
    60 mM 0.0254 mL 0.1272 mL 0.2544 mL 0.6360 mL
    80 mM 0.0191 mL 0.0954 mL 0.1908 mL 0.4770 mL
    100 mM 0.0153 mL 0.0763 mL 0.1526 mL 0.3816 mL
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    一般には略語で表示されます:C1V1 = C2V2

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    製品名:
    Imidazole ketone erastin
    製品番号:
    HY-114481
    数量:
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