Ferroptosis inducer-8
Ferroptosis inducer-8 is a ferroptosis inducer with high selectivity for other cell death mechanism. Ferroptosis inducer-8 induces ferroptosis by affecting ACSL4, GPX4, and FTH1, thereby disrupting intracellular iron homeostasis and the GSH/GPX4 antioxidant defense system, ultimately leading to the accumulation of lipid peroxidation. Ferroptosis inducer-8 also induces ROS production. Ferroptosis inducer-8 inhibits tumor growth and can be used for research of triple-negative breast cancer (TNBC).
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- CAS. Nr.: 3097194-74-3
- Formel: C22H25Cl2NO7
- Molecular Weight:486.34
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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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Biologische Aktivität
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GPX4 |
ACSL4 |
Ferroptosis inducer-8 binds to GPX4 and reduces the thermal stability of GPX4[1].
Ferroptosis inducer-8 (Compound B23) (48 h) shows cytotoxicity in tumor cells with IC50s of 0.08 μM (MCF-7), 0.04 μM (MDA-MB-231), 0.04 μM (MDA-MB-468), 0.05 μM (HT29), 2.81 μM (A549), 0.06 μ(MPC-3), and 2.23 μM for normal cell (MCF-10A)[1].
Ferroptosis inducer-8 (1 μM, 48 h ) selectively induces ferroptosis of MDA-MB-231 and MDA-MB-468 cells, instead of other cell death mechanisms such as apoptosis, necrosis, or autophagy[1].
Ferroptosis inducer-8 (20-60 nM, 7 h) induces disturbances in iron metabolism, exacerbates lipid peroxidation, and induces ROS production (10 h) in MDA-MB-231 cells[1].
Ferroptosis inducer-8 (20-60 nM, 8 h) upregulates expression of ACSL4, downregulates FTH1 and GPX4 in MDA-MB-231 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 and MDA-MB-468 cells
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Concentration:1 μM, co-incubation with Z-VAD-FMK (10 μM), Necrostatin-1 (10 μM) or 3-MA (5 mM); co-incubation with the ferroptosis inhibitors Fer-1 ( 1 μM), DFO (200 μM)), GSH (5 mM) or NAC (5 mM)
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Incubation Time:Pretreated with various cell death inhibitors for 30 min, then co-incubation for 48 h
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Result:Inhibited cell viability and the effect was rescued by Fer-1 ( HY-100579), Deferoxamine (DFO) (HY-B1625)), GSH (HY-D0187) or NAC (HY-B0215).
The cytotoxicity could not rescued by Z-VAD-FMK (HY-16658B), Necrostatin-1 (HY-15760), 3-MA (HY-19312).
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Cell Line:MDA-MB-231 cells
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Concentration:20, 40, 60 nM
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Incubation Time:8 h
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Result:Upregulated expression of ACSL4, downregulates FTH1 and GPX4 in MDA-MB-231 cells, and the modulatory effects were partially restored by Fer-1 (1 μM).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MDA-MB-231 xenograft model established in BALB/C nude mice (4 weeks)[1]
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Dosage:1, 2, 4 mg/kg
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Administration:Daily tail vein injection (i.v.), at the corresponding doses for 21 days.
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Result:Inhibited tumor growth in a concentration-dependent manner, with the tumor growth inhibition (TGI) rate of 78.46% (4 mg/kg), which was significantly higher than that in the positive control group (4 mg/kg RSL3 (HY-100218A), TGI = 27.21%).
Had lower toxicity (higher body weight) than RSL3 at high doses.
Showed no apparent toxicity to the hearts, livers, spleens, lungs or kidneys (H&E staining).
Chemical Information
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CAS. Nr. 3097194-74-3
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Molecular Weight 486.34
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Formel C22H25Cl2NO7
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SMILES
O=C(OC)C1=CO[C@@H](OC)[C@]2([H])C(CN(C3=CC(OC)=C(Cl)C(OC)=C3)C(CCl)=O)=CC[C@@]21[H]
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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)
Ferroptosis inducer-8 Related Classifications
HY-174345 Related Classifications
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