GPX4 activator 1
Based on 1 Customer Validation
GPX4 activator 1 is an allosteric activator of glutathione peroxidase 4 (GPX4) with a Kd value of 5.86 μM. GPX4 activator 1 binds to a specific region of GPX4 to alter protein binding kinetics and counteract ferroptosis (EC50 = 19.19 μM). GPX4 activator 1 inhibits lipid peroxidation, rescues ferroptotic cell death and maintains cell viability. GPX4 activator 1 can be used in studies related to Doxorubicin (HY-15142A)-induced myocardial injury.
For research use only. We do not sell to patients.
- Purity: 99.02%
- CAS No.: 1030098-18-0
- Formula: C20H26N6O2S
- Molecular Weight:414.52
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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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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
GPX4 5.86 μM (Kd) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-1080 | EC50 |
19.19 μM
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Rescue of erastin-induced ferroptotic cell death in human HT-1080 fibrosarcoma cells.
Rescue of erastin-induced ferroptotic cell death in human HT-1080 fibrosarcoma cells.
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39096818 |
In Vitro
GPX4 activator 1 (Compound A9) binds directly to purified GPX4 protein, with a Kd value of 5.86 μM[1].
GPX4 activator 1 (40 μM; treated for 24 h after 1 h of pre-incubation) exerts a selective effect in HT-1080 cells by rescuing Erastin-induced cell death, without affecting cell death induced by Staurosporine (HY-15141), H2O2 or Rapamycin (HY-10219)[1].
GPX4 activator 1 (1-240 min) binds to an allosteric site and reduces deuterium uptake in a specific polypeptide region in a cell-free system[1].
GPX4 activator 1 (24 h) reverses Erastin (HY-15763)-induced ferroptosis in HT-1080 cells, with an EC50 of 19.19 μM[1].
GPX4 activator 1 acts to inhibit Erastin-induced lipid peroxide accumulation in HT-1080 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-1080 cells
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Concentration:40 μM
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Incubation Time:24 h
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Result:Selectively inhibited erastin-induced ferroptosis, but had no significant effect on cell death caused by Staurosporine, H2O2, or Rapamycin.
Chemical Information
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CAS No. 1030098-18-0
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Appearance Solid
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Molecular Weight 414.52
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Formula C20H26N6O2S
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Color Off-white to light yellow
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SMILES
CN(CC1)CCN1C2=NN=C(S2)N3C=CC=C3CNC4=CC=C(OC)C(OC)=C4
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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
In Vitro:
DMSO : 100 mg/mL (241.24 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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (12.06 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (12.06 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 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.
Purity & Documentation
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Data Sheet (275 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)
- Korean - KR (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 | 2.4124 mL | 12.0621 mL | 24.1243 mL | 60.3107 mL |
| 5 mM | 0.4825 mL | 2.4124 mL | 4.8249 mL | 12.0621 mL | |
| 10 mM | 0.2412 mL | 1.2062 mL | 2.4124 mL | 6.0311 mL | |
| 15 mM | 0.1608 mL | 0.8041 mL | 1.6083 mL | 4.0207 mL | |
| 20 mM | 0.1206 mL | 0.6031 mL | 1.2062 mL | 3.0155 mL | |
| 25 mM | 0.0965 mL | 0.4825 mL | 0.9650 mL | 2.4124 mL | |
| 30 mM | 0.0804 mL | 0.4021 mL | 0.8041 mL | 2.0104 mL | |
| 40 mM | 0.0603 mL | 0.3016 mL | 0.6031 mL | 1.5078 mL | |
| 50 mM | 0.0482 mL | 0.2412 mL | 0.4825 mL | 1.2062 mL | |
| 60 mM | 0.0402 mL | 0.2010 mL | 0.4021 mL | 1.0052 mL | |
| 80 mM | 0.0302 mL | 0.1508 mL | 0.3016 mL | 0.7539 mL | |
| 100 mM | 0.0241 mL | 0.1206 mL | 0.2412 mL | 0.6031 mL |
GPX4 activator 1 Related Classifications
HY-161928 Related Classifications
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