GCLCi0
GCLCi0 (ONO-6428513) is a glutamate-cysteine ligase catalytic subunit (GCLC) inhibitor and ferroptosis inducer that blocks the rate-limiting step of glutathione synthesis and exerts anti-tumor activity. GCLCi0 specifically targets SMARCB1-deficient cancer cells, induces reactive oxygen species production and lipid peroxidation. In addition, GCLCi0 shows a significant synergistic effect with SLC7A11 inhibitors and Telaglenastat (HY-12248). GCLCi0 can be used in the research of smarcb1-deficient malignant rhabdoid tumors and smarcb1-deficient epithelioid sarcomas.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 2926699-71-8
- Formel: C8H15F3N2O3S
- Molecular Weight:276.28
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
GCLCi0 (72 h) potently and selectively inhibits the viability of SMARCB1-deficient rhabdoid tumor cells (JMU-RTK-2, G401, G402) with significantly lower IC50 values than in SMARCB1-proficient renal cancer cells, displaying a selective index superior to approved EZH2 inhibitors[1].
GCLCi0 (0.1-10 μM; 24-48 h) selectively depletes the GSH/GSSG ratio in SMARCB1-deficient rhabdoid tumor cells (JMU-RTK-2, G401, G402) in a concentration-dependent manner, with minimal effect on SMARCB1-proficient renal cancer cells[1].
GCLCi0 (0.1-4 μM; 72 h) selectively induces concentration-dependent lipid peroxidation in SMARCB1-deficient rhabdoid tumor cells (JMU-RTK-2, G401), an effect that is suppressed by the ferroptosis inhibitor Ferrostatin-1 (HY-100579)[1].
GCLCi0 (72 h) antiproliferative effect on SMARCB1-deficient JMU-RTK-2 rhabdoid tumor cells is rescued by the ferroptosis inhibitor ferrostatin-1 but not by the apoptosis inhibitor Z-VAD-FMK, confirming ferroptosis as the mechanism of cell death[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 2926699-71-8
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Molecular Weight 276.28
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Formel C8H15F3N2O3S
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SMILES
N[C@H](C(O)=O)CCS(=N)(CCCC(F)(F)F)=O
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Synonyms
ONO-6428513
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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)
- GCLCi0
- 2926699-71-8
- ONO-6428513
- GCLCi 0
- GCLCi-0
- ONO6428513
- ONO 6428513
- Ferroptosis
- ferroptotic cell death
- reactive oxygen species
- epithelioid sarcomas
- JMU-RTK-2
- malignant rhabdoid tumors
- glutathione synthesis
- mouse tumor xenograft models
- glutamate-cysteine ligase catalytic subunit
- lipid peroxidation
- SMARCB1-deficient cancer cells
- Inhibitor
- inhibitor
- inhibit