Autophagy-IN/Ferroptosis inducer-modulator-1
Autophagy-IN/Ferroptosis inducer-modulator-1 is a dual-functional molecule that acts as an Autophagy inhibitor and a Ferroptosis inducer. Autophagy-IN/Ferroptosis inducer-modulator-1 downregulates GPX4 expression, elevates ROS levels and reduces mitochondrial membrane potential. Autophagy-IN/Ferroptosis inducer-modulator-1 arrests the cell cycle of non-small cell lung cancer (NSCLC) cells, induces mild apoptosis and inhibits autophagy. Autophagy inhibition induced by Autophagy-IN/Ferroptosis inducer-modulator-1 acts upstream of ferroptosis to produce a synergistic effect. Autophagy-IN/Ferroptosis inducer-modulator-1 exhibits anti-tumor activity against both human tumor cells and zebrafish xenograft models. Autophagy-IN/Ferroptosis inducer-modulator-1 can be used for research related to non-small cell lung cancer.
For research use only. We do not sell to patients.
- Formula: C31H26F3N3O5
- Molecular Weight:577.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
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GPX4 |
Akt |
EGFR |
Autophagy-IN/Ferroptosis inducer-modulator-1 (compound 4k) (1.56-100 μM; 48 h) potently and selectively inhibits the proliferation of human non-small cell lung cancer A549 cells, with an IC50 of 0.85 μM[1].
Autophagy-IN/Ferroptosis inducer-modulator-1 (0.5-1.5 μM; 48 h) inhibits the migration of human non-small cell lung cancer A549 cells in a concentration-dependent manner[1].
Autophagy-IN/Ferroptosis inducer-modulator-1 (0.5-1.5 μM; 24 h) induces S-phase arrest and only mild apoptosis in human non-small cell lung cancer A549 cells[1].
Autophagy-IN/Ferroptosis inducer-modulator-1 (1 μM; 24 h) induces ultrastructural changes consistent with autophagy inhibition and ferroptosis in human non-small cell lung cancer A549 cells following treatment with 1 μM for 24 h[1].
Autophagy inhibition induced by Autophagy-IN/Ferroptosis inducer-modulator-1 (5 μM; 24 h) acts upstream of ferroptosis and exerts a synergistic effect with it in human non-small cell lung cancer A549 cells[1].
Autophagy-IN/Ferroptosis inducer-modulator-1 (0.5-1.5 μM; 24 h) concentration-dependently increases intracellular ROS levels and induces mitochondrial membrane potential depolarization in human non-small cell lung cancer A549 cells[1].
Autophagy-IN/Ferroptosis inducer-modulator-1 (2.5-10 μM; 24 h) downregulates the protein expression of GPX4, AKT and EGFR in a concentration-dependent manner in human non-small cell lung cancer A549 cells[1].
Autophagy-IN/Ferroptosis inducer-modulator-1 (2.5-10 μM; 24 h) impairs autophagic flux in human non-small cell lung cancer A549 cells in a concentration-dependent manner, and this effect after 24 h of treatment is confirmed by increased protein levels of LC3-II and p62[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human non-small cell lung cancer A549 cells
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Concentration:0.5, 1, 1.5 μM
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Incubation Time:24, 48 h
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Result:Inhibited A549 cell migration in a concentration-dependent manner.
Decreased the cell migration rate to about 22% at 1.5 μM, compared to over 80% in the control group.
Caused a significantly increased wound width at 1.5 μM.
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Cell Line:human non-small cell lung cancer A549 cells
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Concentration:0.5, 1, 1.5 μM
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Incubation Time:24 h
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Result:Induced concentration-dependent accumulation of cells in the G0/G1 phase.
Reduced the S phase population to 24.2%, 20.7%, and 13.8% at 0.5, 1, and 1.5 μM, respectively.
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Cell Line:human non-small cell lung cancer A549 cells
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Concentration:0.5, 1, 1.5 μM
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Incubation Time:24 h
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Result:Induced modest, concentration-dependent increases in total apoptotic rates: 28.4%, 31%, and 33% at 0.5, 1, and 1.5 μM, respectively.
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Cell Line:human non-small cell lung cancer A549 cells
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Concentration:2.5, 5, 10 μM
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Incubation Time:24 h
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Result:Downregulated GPX4 expression in a concentration-dependent manner.
Exhibited superior GPX4 inhibitory activity compared to equimolar Gefitinib (HY-50895) at 10 μM.
Downregulated AKT and EGFR expression in a concentration-dependent manner.
Reduced AKT expression at 5 μM and 10 μM.
Caused significant reductions in EGFR expression.
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Cell Line:human non-small cell lung cancer A549 cells
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Concentration:2.5, 5, 10 μM
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Incubation Time:24 h
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Result:Upregulated LC3-II expression in a concentration-dependent manner, indicative of autophagosome accumulation.
Simultaneously elevated p62 levels, indicative of impaired autophagic flux.
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Cell Line:human non-small cell lung cancer A549 cells
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Concentration:5 μM
5 μM (Rapamycin (HY-10219) / Ferrostatin-1 (HY-100579)) -
Incubation Time:24 h
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Result:Downregulated GPX4 expression when used alone.
Showed partially restored GPX4 levels suppressed by Autophagy-IN/Ferroptosis inducer-modulator-1 when co-treated with either Rapamycin or Ferrostatin-1.
Caused p62 accumulation that was not altered by co-treatment with Rapamycin or Ferrostatin-1.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:AB strain (embryo stage, 2 days post-fertilization)[1]
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Dosage:2.5 μM; 5 μM; 10 μM
5 μM (combined with 10 μM Rapamycin) -
Administration:immersion; 48 hours
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Result:Eliminated nearly all tumor fluorescence, induced aberrant tumor cell morphology, suppressed tumor cell proliferation, reduced pericardial edema, improved locomotion and extended zebrafish survival at 10 μM.
Elevated tumor volume when 5 μM compound was combined with 10 μM rapamycin relative to rapamycin monotherapy.
Chemical Information
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Molecular Weight 577.55
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Formula C31H26F3N3O5
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SMILES
COC1=CC=CC(C2=CC(N(CC3=CC=C(OC)C=C3)C4=C5C(C(OCC)=O)(C(F)(F)F)C(C#N)=C(N)O4)=C5C=C2)=C1
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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)
Autophagy-IN/Ferroptosis inducer-modulator-1 Related Classifications
HY-187191 Related Classifications
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