PROTAC GPX4 degrader-3
PROTAC GPX4 degrader-3 is a glutathione peroxidase 4 (GPX4) PROTAC degrader with a DC50 of 0.019 μM in HT1080 cells. PROTAC GPX4 degrader-3 degrades GPX4 primarily via the ubiquitin-proteasome system (UPS) in a dose- and time-dependent manner. PROTAC GPX4 degrader-3 induces lipid peroxidation (LPO) and ROS accumulation, thereby triggering ferroptosis (ferroptosis). PROTAC GPX4 degrader-3 exhibits in vitro anti-tumor activity against cancer cells. PROTAC GPX4 degrader-3 can be used in the research of fibrosarcoma, triple-negative breast cancer, and renal cell carcinoma.
(Pink: GPX4 ligand (HY-135832); Blue: E3 ligase ligand; Black: linker (HY-22391)).
For research use only. We do not sell to patients.
- Formula: C41H51ClN4O5
- Molecular Weight:715.32
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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GPX4 |
PROTAC GPX4 degrader-3 (R8) (72 h) inhibits the viability of HT1080, MDA-MB-231, 786-O and OS-RC-2 cells, with IC50 values of 0.024 μM, 0.032 μM, 0.046 μM and 0.072 μM against the above cells, respectively[1].
PROTAC GPX4 degrader-3 (0.005-0.8 μM; 1-24 h) potently degrades GPX4 in HT1080 cells in a dose- and time-dependent manner, with a DC50 of 0.019 μM, achieving 47% and 78% degradation at concentrations of 0.05 μM and 0.20 μM (24 h), respectively[1].
PROTAC GPX4 degrader-3 (0.05 μM; 2-12 h) mainly induces GPX4 degradation in HT1080 cells via the ubiquitin-proteasome system (UPS) pathway; the proteasome inhibitor MG132 (HY-13259) blocks this degradation process[1].
PROTAC GPX4 degrader-3 (0.2-0.5 μM; 4 h) induces significant accumulation of lipid peroxidation and ROS in HT1080 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT1080 human fibrosarcoma cells
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Concentration:0.005, 0.01, 0.04, 0.08, 0.4, 0.8 μM (24 h); 0.05 μM (time-course)
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Incubation Time:1, 3, 5, 7, 9, 12, 20 h (0.05 μM); 24 h (0.005-0.8 μM)
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Result:Degraded 47% of GPX4 protein at 0.05 μM for 24 h.
Degraded 78% of GPX4 protein at 0.20 μM for 24 h.
Exhibited dose-dependent degradation with a DC50 of 0.019 μM.
Initiated GPX4 degradation after 7 h of treatment with 0.05 μM, achieved ~50% degradation at 12 h, and continued increasing degradation through 20 h.
Chemical Information
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Molecular Weight 715.32
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Formula C41H51ClN4O5
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SMILES
O=C(OC)[C@@H](C1)N(C(CCl)=O)[C@@H](C2=CC=C(C(NCCCCCCCNC(CC3(C[C@@H](C4)C5)C[C@@H]5C[C@@H]4C3)=O)=O)C=C2)C6=C1C7=CC=CC=C7N6
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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)
PROTAC GPX4 degrader-3 Related Classifications
HY-161930 Related Classifications
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