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GPX4-IN-19 is a highly effective small-molecule inhibitor of glutathione peroxidase 4 (GPX4) with an IC50 value of 0.311 μM, which exerts its pharmacological activity by covalently binding to the Sec46 active site of GPX4, thereby disrupting lipid peroxide detoxification, inducing intracellular Fe²⁺ accumulation, elevating lipid peroxide (LPO) and reactive oxygen species (ROS) levels, triggering ferroptosis-associated DNA damage, demonstrating strong anti-proliferative effects with high ferroptosis selectivity, and providing a robust experimental tool for mechanistic and therapeutic studies in Triple-Negative Breast Cancer (TNBC).


| Description | GPX4-IN-19 is a highly effective small-molecule inhibitor of glutathione peroxidase 4 (GPX4) with an IC50 value of 0.311 μM, which exerts its pharmacological activity by covalently binding to the Sec46 active site of GPX4, thereby disrupting lipid peroxide detoxification, inducing intracellular Fe²⁺ accumulation, elevating lipid peroxide (LPO) and reactive oxygen species (ROS) levels, triggering ferroptosis-associated DNA damage, demonstrating strong anti-proliferative effects with high ferroptosis selectivity, and providing a robust experimental tool for mechanistic and therapeutic studies in Triple-Negative Breast Cancer (TNBC). |
| Targets&IC50 | GPX4:0.311 μM |
| In vivo | Method: GPX4-IN-19 was administered intraperitoneally at 5 or 10 mg/kg every two days for 24 days in MDA-MB-231 tumor-bearing mice. Result: GPX4-IN-19 produced dose-dependent tumor growth inhibition without significant toxicity or weight loss[1]. |
| Molecular Weight | 395.81 |
| Formula | C19H19ClFNO5 |
| Cas No. | 3102894-57-2 |
| Smiles | O=C(N(C1=CC(OC)=C(F)C(OC)=C1)CC2=CC=C3OCCOC3=C2)CCl |
| Color | White |
| Appearance | Solid |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 40 mg/mL (101.06 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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