GPX4-IN-3
Based on 4 publication(s) in Google Scholar
GPX4-IN-3 (26a) is a potent glutathione peroxidase 4 (GPX4) inhibitor as a selective ferroptosis inducer. GPX4-IN-3 (26a) exhibits 71.7% inhibition for GPX4 with 1 μM.
For research use only. We do not sell to patients.
- Purity : 99.83%
- CAS No.: 2761004-85-5
- Formula: C29H24ClN3O3S
- Molecular Weight:530.04
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GPX4-IN-3
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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Bio/Physico-chemical Assay
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RT-PCR
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RT-PCR
Biological Activity
Description
IC50 & Target
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GPX4 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 4T1 | IC50 |
0.78 μM
Compound: 26a
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Cytotoxicity against human 4T1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human 4T1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 34506134] |
| 4T1 | IC50 |
0.78 μM
Compound: 26a
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Cytotoxicity against mouse 4T1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against mouse 4T1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 34506134] |
| HT-1080 | IC50 |
0.15 μM
Compound: 26a
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Cytotoxicity against human HT-1080 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human HT-1080 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 34506134] |
| HT-1080 | IC50 |
4.73 μM
Compound: 26a
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Cytotoxicity against human HT-1080 cells assessed as reduction in cell viability incubated for 48 hrs in presence of Fer-1 by MTT assay
Cytotoxicity against human HT-1080 cells assessed as reduction in cell viability incubated for 48 hrs in presence of Fer-1 by MTT assay
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[PMID: 34506134] |
| MCF7 | IC50 |
6.9 μM
Compound: 26a
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Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 34506134] |
In Vitro
GPX4-IN-3 (26a) exhibits IC50 values of 0.78 μM, 6.9 μM, 0.15 μM and 4.73 μM in 4T1, MCF-7, HT1080 and HT1080 (with Fer-1) cells, respectively[1].
GPX4-IN-3 (26a) exhibits outstanding GPX4 inhibitory activity with a percent inhibition up to 71.7% at 1.0 μM compared to 45.9% of RSL-3[1].
GPX4-IN-3 (26a) could significantly induce lipid peroxide (LPO) increase and effectively induce ferroptosis with satisfactory selectivity[1].
GPX4-IN-3 (26a) is more likely to induce ferroptosis through the accumulation of intracellular peroxides via inhibiting GPX4 activity[1].
GPX4-IN-3 (26a) significantly increased the level of ROS in 4T1 cells, which could also be reversed by Ferrostatin-1 (fer-1)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse 4T1 xenograft model[1].
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Dosage:15 and 30 mg/kg.
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Administration:Intravenous injection, every two days for a total of five times.
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Result:Significantly suppress tumor growth with a tumor growth inhibition (TGI) value of 33.2 and 55.1% at 15 and 30 mg/kg, respectively.
Chemical Information
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CAS No. 2761004-85-5
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Appearance Solid
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Molecular Weight 530.04
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Formula C29H24ClN3O3S
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Color White to off-white
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SMILES
O=C(C(C1=CSC2=CC=CC=C21)N(C3=CC=C(C=C3)C4=CN=CO4)C(CCl)=O)NCCC5=CC=CC=C5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Redox Biol
EGR1 regulates oxidative stress and aldosterone production in adrenal cells and aldosterone-producing adenomas. [Abstract]2025 Mar:80:103498. PMID: 39826326
GPX4-IN-3 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2025 Mar:80:103498. [Abstract]
GPX4-IN-3 (0, 1, 2, 4, 8 μM) caused a dose-dependent increase in ROS levels in HAC15 cells.
GPX4-IN-3 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2025 Mar:80:103498. [Abstract]
GPX4-IN-3 (2 μM; 6h) decreased the RNA expression of CYP11B2 in HAC15 cells.
GPX4-IN-3 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2025 Mar:80:103498. [Abstract]
GPX4-IN-3 (2 μM; 4h) increased the RNA expression of EGR1 in HAC15 cells.
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J Exp Clin Cancer Res
L-kynurenine induces NK cell loss in gastric cancer microenvironment via promoting ferroptosis. [Abstract]2023 Mar 1;42(1):52. PMID: 36855135
GPX4-IN-3 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2023 Mar 1;42(1):52. [Abstract]
GPX4-IN-3 (1 μM; 48 h) showed that cell death was significantly increased in SE-hNK cells with L-KYN.
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GPX4-IN-3 purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2026 Jun 26;15(7):798.
GPX4-IN-3 (0.5 μM; 24 h) induced cell death in SH-SY5Y cells.
GPX4-IN-3 purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2026 Jun 26;15(7):798.
GPX4-IN-3 (0.5 μM; 16 h) induced a marked increase in oxidized lipid levels compared to control cells in SH-SY5Y cells.
Solvent & Solubility
In Vitro:
DMSO : 67.5 mg/mL (127.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 6.75 mg/mL (12.73 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 6.75 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 (67.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocols
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Ferroptosis Solutions
Ferroptosis is an iron-dependent, non-apoptotic form of regulated cell death characterized by lethal lipid peroxidation and sensitivity to suppression by iron chelators or lipophilic radical-trapping antioxidants. The core pathway links cystine uptake through system Xc−, glutathione availability, GPX4-dependent detoxification of phospholipid hydroperoxides, iron-dependent oxidative reactions, and polyunsaturated-phospholipid metabolism into a cell-death program that is biochemically and morphologically distinct from apoptosis, necrosis, and autophagy. The ferroptosis pathway is experimentally linked to phenotype through chemical and genetic perturbation. Erastin induces ferroptosis by inhibiting cystine uptake through system Xc− and weakening antioxidant defenses, while GPX4 inhibition or depletion causes lipid peroxide accumulation and ferroptotic cancer-cell death. ACSL4 and oxidizable arachidonoyl- or adrenoyl-containing phosphatidylethanolamines shape ferroptosis sensitivity by con
Purity & Documentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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, 6 months; -20°C, 1 month. 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 |
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| DMSO | 1 mM | 1.8867 mL | 9.4333 mL | 18.8665 mL | 47.1663 mL |
| 5 mM | 0.3773 mL | 1.8867 mL | 3.7733 mL | 9.4333 mL | |
| 10 mM | 0.1887 mL | 0.9433 mL | 1.8867 mL | 4.7166 mL | |
| 15 mM | 0.1258 mL | 0.6289 mL | 1.2578 mL | 3.1444 mL | |
| 20 mM | 0.0943 mL | 0.4717 mL | 0.9433 mL | 2.3583 mL | |
| 25 mM | 0.0755 mL | 0.3773 mL | 0.7547 mL | 1.8867 mL | |
| 30 mM | 0.0629 mL | 0.3144 mL | 0.6289 mL | 1.5722 mL | |
| 40 mM | 0.0472 mL | 0.2358 mL | 0.4717 mL | 1.1792 mL | |
| 50 mM | 0.0377 mL | 0.1887 mL | 0.3773 mL | 0.9433 mL | |
| 60 mM | 0.0314 mL | 0.1572 mL | 0.3144 mL | 0.7861 mL | |
| 80 mM | 0.0236 mL | 0.1179 mL | 0.2358 mL | 0.5896 mL | |
| 100 mM | 0.0189 mL | 0.0943 mL | 0.1887 mL | 0.4717 mL |
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