GPX4 degrader-1
GPX4 degrader-1 (Compound RS-1) is a hydrophobic tagging (HyT)-mediated GPX4 degrader (DC50: 8.9 nM in HT1080 cells) GPX4 degrader-1 induces GPX4 degradation. GPX4 degrader-1 induces Ferroptosis. GPX4 degrader-1 increases lipid ROS. GPX4 degrader-1 demonstrates potent antitumor efficacy in a murine mammary carcinoma model.
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- CAS. Nr.: 3057531-85-5
- Formel: C38H36ClN3O4
- Molecular Weight:634.16
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
GPX4 8.9 nM (DC50) |
In Vitro
GPX4 degrader-1 (0.3-300 nM; 2-48 h) induces dose- and time-dependent proteasome-mediated GPX4 degradation in HT1080 fibrosarcoma cells, with a DC50 of 8.9 nM[1].
GPX4 degrader-1 (48 h) induces ferroptosis-mediated antiproliferative activity in HT1080, A549 and 4T1 cancer cells, with IC50 values of 130 nM, 6.4 μM and 700 nM, respectively[1].
GPX4 degrader-1 (0.5-2.0 μM for MDA; 24-48 h) increases lipid ROS and MDA in HT1080 fibrosarcoma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 6 to 8 weeks old)[1]
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Dosage:16 μmol/kg; 33 μmol/kg; 66 μmol/kg
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Administration:i.p.; daily; 10 days
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Result:Induced dose-dependent tumor growth inhibition: 29.3% TGI at 16 μmol/kg, 54.6% TGI at 33 μmol/kg, and 80.5% TGI at 66 μmol/kg.
Demonstrated statistically significant superior antitumor activity compared to RSL3 at 66 μmol/kg (P < 0.01).
Reduced tumor weight in a dose-dependent manner.
Caused no significant changes in mouse body weight during the treatment period.
Chemical Information
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CAS. Nr. 3057531-85-5
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Molecular Weight 634.16
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Formel C38H36ClN3O4
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SMILES
O=C(OC)[C@@H](C1)N(C(CCl)=O)[C@@H](C2=CC=C(C(NCCCC(C3=CC=CC=C3)C4=CC=CC=C4)=O)C=C2)C5=C1C6=CC=CC=C6N5
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
GPX4 degrader-1 Related Classifications
HY-181598 Related Classifications
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Keywords
- GPX4 degrader-1
- 3057531-85-5
- HyT
- Glutathione Peroxidase
- Ferroptosis
- Reactive Oxygen Species (ROS)
- HT1080 fibrosarcoma cells
- ubiquitin-proteasome system
- ferroptosis
- GPX4
- reactive oxygen species
- malondialdehyde
- A549 cancer cells
- 4T1 cancer cells
- lipid peroxidation
- murine mammary carcinoma model
- Inhibitor
- inhibitor
- inhibit