GPX4-IN-4
Based on 1 Customer Validation
GPX4-IN-4 (Compound 24) is a potent GPX4 inhibitor. GPX4-IN-4 can be used for the research of cancer.
For research use only. We do not sell to patients.
- Purity: 98.94%
- CAS No.: 2920221-53-8
- Formula: C22H21ClN2O5S
- Molecular Weight:460.93
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Immunology/Inflammation Compound Library
HY-L007
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Metabolism/Protease Compound Library
HY-L012
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Anti-Cancer Compound Library
HY-L025
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Anti-Aging Compound Library
HY-L034
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Antioxidant Compound Library
HY-L037
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Oxygen Sensing Compound Library
HY-L045
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Ferroptosis Compound Library
HY-L051
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Anti-Cancer Metabolism Compound Library
HY-L083
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Metabolic Enzyme Compound Library
HY-L146
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Anti-Ovarian Cancer Compound Library
HY-L173
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Radioprotector Library
HY-L178
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
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GPX4 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-1080 | EC50 |
0.09 μM
Compound: 24
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Induction of ferroptosis in GPX4-dependent human HT-1080 cells assessed as cell viability incubated for 24 hrs by time-course cell viability assay
Induction of ferroptosis in GPX4-dependent human HT-1080 cells assessed as cell viability incubated for 24 hrs by time-course cell viability assay
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[PMID: 36877935] |
| HT-1080 | EC50 |
0.17 μM
Compound: 24
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Induction of ferroptosis in GPX4-dependent human HT-1080 cells assessed as cell viability incubated for 6 hrs by time-course cell viability assay
Induction of ferroptosis in GPX4-dependent human HT-1080 cells assessed as cell viability incubated for 6 hrs by time-course cell viability assay
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[PMID: 36877935] |
| HT-1080 | EC50 |
0.27 μM
Compound: 24
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Induction of ferroptosis in GPX4-dependent human HT-1080 cells assessed as cell viability incubated for 3 hrs by time-course cell viability assay
Induction of ferroptosis in GPX4-dependent human HT-1080 cells assessed as cell viability incubated for 3 hrs by time-course cell viability assay
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[PMID: 36877935] |
| HT-1080 | EC50 |
0.49 μM
Compound: 24
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Induction of ferroptosis in GPX4-dependent human HT-1080 cells assessed as cell viability incubated for 6 hrs in presence of 40% human plasma by time-course cell viability assay
Induction of ferroptosis in GPX4-dependent human HT-1080 cells assessed as cell viability incubated for 6 hrs in presence of 40% human plasma by time-course cell viability assay
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[PMID: 36877935] |
| HT-1080 | EC50 |
0.52 μM
Compound: 24
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Induction of ferroptosis in GPX4-dependent human HT-1080 cells assessed as cell viability incubated for 24 hrs in presence of 40% human plasma by time-course cell viability assay
Induction of ferroptosis in GPX4-dependent human HT-1080 cells assessed as cell viability incubated for 24 hrs in presence of 40% human plasma by time-course cell viability assay
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[PMID: 36877935] |
| HT-1080 | EC50 |
0.77 μM
Compound: 24
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Induction of ferroptosis in GPX4-dependent human HT-1080 cells assessed as cell viability incubated for 3 hrs in presence of 40% human plasma by time-course cell viability assay
Induction of ferroptosis in GPX4-dependent human HT-1080 cells assessed as cell viability incubated for 3 hrs in presence of 40% human plasma by time-course cell viability assay
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[PMID: 36877935] |
| HT-1080 | EC50 |
0.85 μM
Compound: 24
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Induction of ferroptosis in GPX4-dependent human HT-1080 cells assessed as cell viability incubated for 1.5 hrs by time-course cell viability assay
Induction of ferroptosis in GPX4-dependent human HT-1080 cells assessed as cell viability incubated for 1.5 hrs by time-course cell viability assay
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[PMID: 36877935] |
| HT-1080 | EC50 |
1.26 μM
Compound: 24
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Induction of ferroptosis in GPX4-dependent human HT-1080 cells assessed as cell viability incubated for 1.5 hrs in presence of 40% human plasma by time-course cell viability assay
Induction of ferroptosis in GPX4-dependent human HT-1080 cells assessed as cell viability incubated for 1.5 hrs in presence of 40% human plasma by time-course cell viability assay
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[PMID: 36877935] |
| NCI-H1703 | EC50 |
0.117 μM
Compound: 24
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Induction of ferroptosis in human NCI-H1703 cells assessed as cell viability incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay
Induction of ferroptosis in human NCI-H1703 cells assessed as cell viability incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay
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[PMID: 36877935] |
| NCI-H1703 | EC50 |
4.74 μM
Compound: 24
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Induction of ferroptosis in human NCI-H1703 cells assessed as cell viability incubated for 72 hrs in presence of ferrostatin-1 by CellTiter-Glo luminescent cell viability assay
Induction of ferroptosis in human NCI-H1703 cells assessed as cell viability incubated for 72 hrs in presence of ferrostatin-1 by CellTiter-Glo luminescent cell viability assay
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[PMID: 36877935] |
GPX4-IN-4 (Compound 24; 0-1000 nM; 0-24 h) inhibits HT1080 cell viability in a concentration-and time-dependent manner[1].
GPX4-IN-4 (0-10 μM; 72 h) inhibits NCI-H1703 cell viability with EC50s of 0.117 μM and 4.74 μM without and with Fer-1 (HY-100579), respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT1080 (GPX4 dependent) cells
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Concentration:0-1000 nM
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Incubation Time:0, 1.5, 3, 6 and 24 h
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Result:Inhibited cell viability with EC50s of 0.85, 0.27, 0.17 and 0.09 μM at 1.5, 3, 6 and 24 h, respectively.
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Cell Line:NCI-H1703
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Concentration:0-10 μM
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Incubation Time:72 h
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Result:Inhibited cell viability with EC50s of 0.117 μM and 4.74 μM without and with Fer-1, respectively.
GPX4-IN-4 (50 mg/kg; i.p.; daily for 20 days) has no effect on WSU-DLCL2 tumor growth in mice, although partial target engagement is observed in tumor homogenate[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID/Beige mice[1]
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Dosage:100 and 200 mg/kg
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Administration:IP, once
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Result:The GPX4 band was shifted. Engaged kidney GPX4 and induced PD markers.
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Animal Model:SCID/Beige mice[1]
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Dosage:30 and 100 mg/kg
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Administration:IP (Pharmacokinetic Analysis)
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Result:PK Properties of GPX4-IN-4 (Compound 24)[1]
Dose t1/2 (h) Cmax (μg/mL) AUC (μg*h/mL) 30 (IP) 0.5 0.92 (±0.24) 1.89 (±0.17) 100 (IP) 1.7 5.31 (±0.53) 16.20 (±1.70)
Chemical Information
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CAS No. 2920221-53-8
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Appearance Solid
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Molecular Weight 460.93
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Formula C22H21ClN2O5S
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Color White to off-white
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SMILES
COC([C@H]1CC2=C([C@@H](N1C(CCl)=O)C3=CC=C(C=C3)S(C)(=O)=O)NC4=CC=CC=C42)=O
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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
Solvent & Solubility
DMSO : 200 mg/mL (433.91 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)
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (10.85 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
Purity & Documentation
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Data Sheet (288 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1695 mL | 10.8476 mL | 21.6953 mL | 54.2382 mL |
| 5 mM | 0.4339 mL | 2.1695 mL | 4.3391 mL | 10.8476 mL | |
| 10 mM | 0.2170 mL | 1.0848 mL | 2.1695 mL | 5.4238 mL | |
| 15 mM | 0.1446 mL | 0.7232 mL | 1.4464 mL | 3.6159 mL | |
| 20 mM | 0.1085 mL | 0.5424 mL | 1.0848 mL | 2.7119 mL | |
| 25 mM | 0.0868 mL | 0.4339 mL | 0.8678 mL | 2.1695 mL | |
| 30 mM | 0.0723 mL | 0.3616 mL | 0.7232 mL | 1.8079 mL | |
| 40 mM | 0.0542 mL | 0.2712 mL | 0.5424 mL | 1.3560 mL | |
| 50 mM | 0.0434 mL | 0.2170 mL | 0.4339 mL | 1.0848 mL | |
| 60 mM | 0.0362 mL | 0.1808 mL | 0.3616 mL | 0.9040 mL | |
| 80 mM | 0.0271 mL | 0.1356 mL | 0.2712 mL | 0.6780 mL | |
| 100 mM | 0.0217 mL | 0.1085 mL | 0.2170 mL | 0.5424 mL |
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