1. Apoptosis PROTAC
  2. Ferroptosis Ligands for Target Protein for PROTAC
  3. iFSP1

iFSP1 is a potent, selective and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1) (AIFM2) with an EC50 of 103 nM. iFSP1 selectively induces ferroptosis in GPX4-knockout cells which overexpressed FSP1. iFSP1 is able to sensitize a variety of human cancer cell lines to the ferroptosis inducer, such as (1S,3R)-RSL3 (HY-100218A).

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

CAS No. : 150651-39-1

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10 mM * 1 mL in DMSO
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Based on 29 publication(s) in Google Scholar

Top Publications Citing Use of Products

29 Publications Citing Use of MCE iFSP1

Cell Proliferation/Viability Assay
In Vivo Efficacy Study
WB

    iFSP1 purchased from MedChemExpress. Usage Cited in: Nature. 2026 Jan;649(8096):477-486.  [Abstract]

    Cell viability of A-375 cells ± iFSP1 (10 μM) ± BSO (1 mM) or combinations for 48 h.

    iFSP1 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Dec;12(46):e04245.  [Abstract]

    Schematic representation of the experimental induction of trained immunity in CIA treated with iFSP1 (10.0 mg kg−1 daily), Arthritis index and paw thickness were scored and compared with CIA. the establishment of a trained immunity model (β‐glucan or PBS) was initiated on day 0, the establishment of a CIA rat model was initiated on day 7, CIA was re‐enforced on day 14, and ferroptosis induction was initiated by daily intraperitoneal injection of iFSP1 (10.0 mg/kg/ daily) on day 14, the experiment was terminated on day 35.

    iFSP1 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Dec;12(46):e04245.  [Abstract]

    Representative photographs of morphology in different groups, H&E, toluidine blue O, and safranin O staining of representative joints in different groups. the establishment of a trained immunity model (β‐glucan or PBS) was initiated on day 0, the establishment of a CIA rat model was initiated on day 7, CIA was re‐enforced on day 14, and ferroptosis induction was initiated by daily intraperitoneal injection of iFSP1 (10.0 mg/kg/ daily) on day 14, the experiment was terminated on day 35.

    iFSP1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Oct 30;14(1):6908.  [Abstract]

    Ferroptosis inhibition by FXR activation is reverted when FSP1 or PPARα are inhibited. Ferroptosis was induced by 200 nM RSL3 for 18 h, 12 µM Turofexorate was used to inhibit ferroptosis. FSP1 was inhibited by iFSP1 (0.2, 1.5, 6.3, 25 μM), PPARα was inhibited by GW6471 (PPARαi).

    iFSP1 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 May 3;8(1):40.  [Abstract]

    U2OS cells were treated with iFSP1 (10 µM; 0, 0.5, 1, 2, 4, 8 h). O-GlcNAcylation levels were detected by immunoblotting with antibodies against O-GlcNAc and β-actin, and the relative intensity (O-GlcNAc/b-actin) was quantified.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    iFSP1 is a potent, selective and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1) (AIFM2) with an EC50 of 103 nM. iFSP1 selectively induces ferroptosis in GPX4-knockout cells which overexpressed FSP1. iFSP1 is able to sensitize a variety of human cancer cell lines to the ferroptosis inducer, such as (1S,3R)-RSL3 (HY-100218A)[1].

    IC50 & Target

    FSP1

     

    In Vitro

    iFSP1 (0.001-1 μM; 24 hours) inhibits the Gpx4-knockout cell growth as a dose-dependent manner, but does not inhibit the wild type cell growth. Treatment with the ferroptosis inhibitor Lip-1 protects GPX4- knockout cells from iFSP1-induced ferroptosis[1].
    iFSP1 (0.001-1 μM; 24 hours) is less efficient than genetic deletion of FSP1, whereas iFSP1 treatment in the FSP1-knockout background had no additive effect to RSL3-induced ferroptosis[1].
    iFSP1 (3 μM; 24 hours) treatment results in an obvious toxicity of RSL3 in a panel of genetically engineered (FSP1-knockout) human cancer cell lines[1].
    AIFM2: the flavoprotein apoptosis-inducing factor mitochondria-associated 2 is a previously unrecognized anti-ferroptotic gene. AIFM2, which is renamed ferroptosis suppressor protein 1 (FSP1)[1]

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

    Cell Proliferation Assay[1]

    Cell Line: Wild-type and Gpx4-knockout Pfa1 or HT 1080 cells overexpressing FSP1–HA
    Concentration: 0.001-1 μM
    Incubation Time: 24 hours
    Result: Was toxic to cells that depend solely (no GPX4 expression detectable) on FSP1 function.

    Cell Viability Assay[1]

    Cell Line: NCl-H1437, NCl-H1437 FSP1 KO, U-373, U-373 FSP1 KO, MDA-MB-436, MDA-MB-436 FSP1 KO, SW620, SW620 FSP1 KO, MDA-MB-435S, MDA-MB-435S FSP1 KO, A549 and A549 FSP1 KO
    Concentration: 3 μM
    Incubation Time: 24 hours
    Result: Sensitized a variety of human cancer cell lines to the ferroptosis inducer (1S,3R)-RSL3.
    Molecular Weight

    323.35

    Formula

    C20H13N5

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    N#CC1=C(N)N2C3=CC=CC=C3N=C2C(C#N)=C1C4=CC=C(C)C=C4

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 11.67 mg/mL (36.09 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 3.0926 mL 15.4631 mL 30.9262 mL
    5 mM 0.6185 mL 3.0926 mL 6.1852 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • 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

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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    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2 mg/mL (6.19 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
    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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    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 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: 99.96%

    References

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.0926 mL 15.4631 mL 30.9262 mL 77.3156 mL
    5 mM 0.6185 mL 3.0926 mL 6.1852 mL 15.4631 mL
    10 mM 0.3093 mL 1.5463 mL 3.0926 mL 7.7316 mL
    15 mM 0.2062 mL 1.0309 mL 2.0617 mL 5.1544 mL
    20 mM 0.1546 mL 0.7732 mL 1.5463 mL 3.8658 mL
    25 mM 0.1237 mL 0.6185 mL 1.2370 mL 3.0926 mL
    30 mM 0.1031 mL 0.5154 mL 1.0309 mL 2.5772 mL
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      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:
    iFSP1
    Cat. No.:
    HY-136057
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