GPX4 degrader-2
GPX4 degrader-2 is a GPX4 molecular glue degrader and ferroptosis inducer. GPX4 degrader-2 suppresses GPX4 enzyme activity, promotes ubiquitination-dependent proteasomal degradation of GPX4 protein. GPX4 degrader-2 indues ferroptosis, increases lipid ROS and MDA levels, suppresses glutathione levels in cancer cells. GPX4 degrader-2 inhibits cancer cells proliferation and colony formation. GPX4 degrader-2 can be used for the research of colorectal cancer.
For research use only. We do not sell to patients.
- Formula: C30H30ClNO8
- Molecular Weight:568.01
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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GPX4 |
GPX4 degrader-2 (Compound W25) (24-72 h) potently inhibits HCT-116 colorectal cancer cell viability with time-dependent efficacy, achieving IC50 values of 4.17, 2.49 and 2.24 μM after 24. 48 and 72 h treatment[1].
GPX4 degrader-2 (2.5-10 μM; 6 h) dose-dependently suppresses long-term colony formation of HCT-116 colorectal cancer cells and inhibits DNA synthesis[1].
GPX4 degrader-2 (2.5-10 μM; 6-24 h) dose- and time-dependently accumulates lipid ROS in HCT-116 colorectal cancer cells[1].
GPX4 degrader-2 (2.5-10 μM; 24 h) dose-dependently depletes intracellular GSH levels and increases intracellular MDA levels in HCT-116 colorectal cancer cells[1].
GPX4 degrader-2 (2.5-10 μM; 6-24 h) dose-dependently downregulates GPX4 protein expression in HCT-116 colorectal cancer cells by promoting ubiquitin-proteasomal degradation[1].
GPX4 degrader-2 (10 μM; 24 h) promotes ubiquitination of GPX4 protein in HCT-116 colorectal cancer cells[1].
GPX4 degrader-2 (50-100 μM; 2 h) directly binds to GPX4 protein, protecting it from pronase E digestion in HCT-116 colorectal cancer cell lysates[1].
GPX4 degrader-2 inhibits the enzymatic activity of human recombinant GPX4[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116 colorectal cancer cells
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Concentration:2.5, 5, 10 μM
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Incubation Time:6, 12, 24 h
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Result:Reduced GPX4 protein levels.
Had its GPX4-inhibitory effect reversed by MG132 treatment.
Chemical Information
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Molecular Weight 568.01
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Formula C30H30ClNO8
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SMILES
O=C(OC1=CC=C(C[C@H]2C(OCC2CC3=CC=C(OC)C(OC)=C3)=O)C=C1OC)C4=CC=C(NC(CCl)=O)C=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- GPX4 degrader-2
- Molecular Glues
- Glutathione Peroxidase
- Ferroptosis
- Reactive Oxygen Species (ROS)
- glutathione
- ubiquitin-proteasomal degradation
- human liver microsomes
- malondialdehyde
- GPX4
- lipid reactive oxygen species
- ferroptosis
- colorectal cancer cells
- HCT-116 colorectal cancer cell
- ubiquitination-dependent proteasomal degradation
- Inhibitor
- inhibitor
- inhibit