2. Apoptosis Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  3. Glutathione Peroxidase Reactive Oxygen Species (ROS) NO Synthase Ferroptosis Apoptosis
  4. anti-NSCLC agent-2

anti-NSCLC agent-2 exhibits nanomolar anti-proliferative activity and acts on wild-type and drug-resistant non-small cell lung cancer (NSCLC) cells. anti-NSCLC agent-2 downregulates ferroptosis-related factors SLC7A11 and GPX4, disrupts cellular redox homeostasis, depletes glutathione, accumulates lipid peroxides, and simultaneously elevates mitochondrial nitric oxide and ROS levels to induce ferroptosis in tumor cells. anti-NSCLC agent-2 is applicable to research related to non-small cell lung cancer.

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anti-NSCLC agent-2

anti-NSCLC agent-2 Chemical Structure

CAS No. : 3063042-21-4

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anti-NSCLC agent-2 Related Antibodies

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GPX1 GPX4

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nNOS iNOS eNOS

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Description

anti-NSCLC agent-2 exhibits nanomolar anti-proliferative activity and acts on wild-type and drug-resistant non-small cell lung cancer (NSCLC) cells. anti-NSCLC agent-2 downregulates ferroptosis-related factors SLC7A11 and GPX4, disrupts cellular redox homeostasis, depletes glutathione, accumulates lipid peroxides, and simultaneously elevates mitochondrial nitric oxide and ROS levels to induce ferroptosis in tumor cells. anti-NSCLC agent-2 is applicable to research related to non-small cell lung cancer[1].

IC50 & Target[1]

GPX4

 

In Vitro

anti-NSCLC agent-2 (compound 6o) (10-160 nM; 48 h) potently inhibits the proliferation of non-small cell lung cancer (NSCLC) cell lines A549, H1299, H2030, H1975, A549/T and A549/CDDP, with IC50 values ranging from 1.54 nM to 11.72 nM, and shows no obvious toxicity to normal HUVECs at effective tumor-inhibiting concentrations[1].
anti-NSCLC agent-2 (100 μM; 2.5 h) releases 10.02 μM of nitric oxide in A549 cells[1].
anti-NSCLC agent-2 (50 nM; 48 h) exhibits antiproliferative activity against A549 and A549/CDDP cells, and this activity is dependent on nitric oxide, as evidenced by the concentration-dependent reversal effect induced by hemoglobin scavenging[1].
Anti-NSCLC agent-2 (100 nM; 48 h) exerts antiproliferative activity against A549 and A549/CDDP cells in a ferroptosis-dependent manner[1].
anti-NSCLC agent-2 (15-60 nM; 12 h) downregulates the protein expression of SLC7A11 and GPX4 in A549 and A549/CDDP cells in a dose-dependent manner via a ferroptosis-dependent mechanism[1].
anti-NSCLC agent-2 (20-80 nM) dose-dependently and time-dependently increases the levels of reactive oxygen species and mitochondrial nitric oxide in A549 cells and A549/CDDP cells[1].
anti-NSCLC agent-2 (40-80 nM; 12 h) dose-dependently depletes intracellular glutathione and reduces the GSH/GSSG ratio in A549 and A549/CDDP cells, thereby disrupting redox homeostasis[1].
anti-NSCLC agent-2 (at a specific concentration; 4 h) induces dose-dependent collapse of mitochondrial membrane potential in A549 and A549/CDDP cells, elevates mitochondrial reactive oxygen species (superoxide) levels, triggers lipid peroxidation, and increases ferrous ion accumulation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

anti-NSCLC agent-2 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: A549, A549/CDDP
Concentration: 50 nM (compound 6o); 0, 6.25, 12.5, 25 μM (hemoglobin pre-treatment)
Incubation Time: 4 h (hemoglobin pre-treatment); 48 h (compound 6o incubation)
Result: Decreased in antiproliferative effect with increasing hemoglobin concentration.
Dropped below 15% in inhibition rate at 25 μM hemoglobin.

Cell Proliferation Assay[1]

Cell Line: A549, A549/CDDP
Concentration: 100 nM (compound 6o); 0, 75, 150, 300 nM (Ferrostatin-1)
Incubation Time: 48 h
Result: Decreased in proliferation inhibition rate with increasing Ferrostatin-1 (HY-100579) concentration in a concentration-dependent manner.
Lost almost all inhibitory activity at 300 nM Ferrostatin-1, with cell viability >95%.

Western Blot Analysis[1]

Cell Line: A549, A549/CDDP
Concentration: 15, 30 nM (A549); 30, 60 nM (A549/CDDP); 300 nM (Fer-1 for reversal)
Incubation Time: 12 h (compound 6o treatment)
Result: Dose-dependently downregulated the expression of SLC7A11 and GPX4 in both cell lines.
Fully reversed this downregulation in the presence of 300 nM Fer-1.
In Vivo

anti-NSCLC agent-2 (compound 6o) (5-10 mg/kg; i.v.; once every 2 days; 20 days) exerts dose-dependent in vivo antiproliferative activity against cisplatin-resistant A549/CDDP xenografts, with 10 mg/kg showing superior efficacy to 10 mg/kg cisplatin (HY-17394), while maintaining a favorable safety profile with no observed organ toxicity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice (female, SPF-grade, cisplatin-resistant NSCLC xenograft model)[1]
Dosage: 5 mg/kg; 10 mg/kg
Administration: i.v. (tail vein); once every 2 days; 20 days
Result: Significantly reduced tumor volume compared to vehicle control at 5 mg/kg.
Reduced final tumor weight compared to both vehicle control and 10 mg/kg cisplatin group at 5 mg/kg.
Achieved the greatest tumor volume reduction among all treatment groups at 10 mg/kg.
Reduced final tumor weight significantly lower than vehicle control and 10 mg/kg cisplatin group at 10 mg/kg.
Showed no significant body weight loss or behavioral abnormalities in either dose group.
Caused no treatment-related histopathological damage to heart, liver, spleen, lung, and kidney as observed via H&E staining.
Molecular Weight

603.43

Formula

C27H20Cl2N2O8S
CAS No.
SMILES

O=S(C1=[N+]([O-])ON=C1OCCOC2=CC(O3)=C(C=C2)C(C)=C(CC4=CC(Cl)=CC(Cl)=C4)C3=O)(C5=CC=CC=C5)=O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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anti-NSCLC agent-2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

anti-NSCLC agent-23063042-21-4Glutathione PeroxidaseReactive Oxygen Species (ROS)NO SynthaseFerroptosisApoptosisNitric oxide synthasesNOSH1975GPX4H2030HUVECsSLC7A11ferroptosisA549H1299hERG channelnonsmall cell lung cancer cellsInhibitorinhibitorinhibit

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