ArticleBiochemical pharmacology2012
Antitumor activity of a novel STAT3 inhibitor and redox modulator in non-small cell lung cancer cells.
Article in Biochemical pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 31 citations in OpenAlex.
- Nrf2 and STAT3 Pathways in Protecting Against Methylmercury-Induced Oxidative Stress in Hypothalamic Neuronal GT1-7 Cells.Neurochemical research · 2026Article
- Unraveling the Clinical Landscape of RNA Modification Regulators with Multi-Omics Insights in Pan-Cancer.Cancers · 2025Article
- Cell Death by Gallotannin Is Associated with Inhibition of the JAK/STAT Pathway in Human Colon Cancer Cells.Current therapeutic research, clinical and experimental · 2020Article
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- Auranofin-mediated inhibition of PI3K/AKT/mTOR axis and anticancer activity in non-small cell lung cancer cells.Oncotarget · 2016Article
- RAS signaling and anti-RAS therapy: lessons learned from genetically engineered mouse models, human cancer cells, and patient-related studies.Acta biochimica et biophysica Sinica · 2016Review
- Small-molecule targeting of signal transducer and activator of transcription (STAT) 3 to treat non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands) · 2015Article
- Novel 2-Carbonylbenzo[b]thiophene 1,1-Dioxide Derivatives as Potent Inhibitors of STAT3 Signaling Pathway.ACS medicinal chemistry letters · 2015Article
- A Resveratrol Analogue Promotes ERKMAPK-Dependent Stat3 Serine and Tyrosine Phosphorylation Alterations and Antitumor Effects In Vitro against Human Tumor Cells.Molecular pharmacology · 2015Article
- Predictive biomarkers in precision medicine and drug development against lung cancer.Chinese journal of cancer · 2015Review
- Expression of sulfotransferase SULT1A1 in cancer cells predicts susceptibility to the novel anticancer agent NSC-743380.Oncotarget · 2015Article
- Characterization of acute biliary hyperplasia in Fisher 344 rats administered the indole-3-carbinol analog, NSC-743380.Toxicology and applied pharmacology · 2014Article
- Development of synthetic lethality anticancer therapeutics.Journal of medicinal chemistry · 2014Review
- Prodrug oncrasin-266 improves the stability, pharmacokinetics, and safety of NSC-743380.Bioorganic & medicinal chemistry · 2014Article
- Selective antitumor activity of ibrutinib in EGFR-mutant non-small cell lung cancer cells.Journal of the National Cancer Institute · 2014Article
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- IGFBP2/FAK pathway is causally associated with dasatinib resistance in non-small cell lung cancer cells.Molecular cancer therapeutics · 2013Article
- Oxidative metabolism in cancer: A STAT affair?JAK-STAT · 2013Review
- Rebuilding pluripotency from primordial germ cells.Stem cell reports · 2013Article
Corrections and comments
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Authors and funding
14 authors at 3 institutions in 1 country.
Funding
Abstract
NSC-743380 is a novel STAT3 inhibitor that suppresses the growth of several NCI-60 cancer cell lines derived from different tissues and induces regression of xenograft tumors in vivo at various doses. To evaluate the antitumor activity of NSC-743380 in lung cancer cells, we analyzed the susceptibility of 50 NSCLC cell lines to this compound using cell viability assay. About 32% (16 of 50) of these cell lines were highly susceptible to this compound, with a 50% inhibitory concentration (IC₅₀) of < 1 μM. In mechanistic studies, the increased numbers of apoptotic cells as well as increased PARP cleavage showed that cytotoxic effects correlate with apoptosis induction. Treatment with NSC-743380 inhibited transcription factor STAT3 activation and induced ROS production in sensitive human lung cancer cell lines but not in resistant cells. Blocking ROS generation with the antioxidant NDGA dramatically abolished NSC-743380-induced growth suppression and apoptosis, but had minimal effect on NSC-743380-induced STAT3 inhibition, suggesting that STAT3 inhibition is not caused by ROS production. Interestingly, knockdown of STAT3 with use of shSTAT3 induced ROS generation and suppressed tumor cell growth. Moreover, scavenging ROS induced by STAT3 inhibition also diminished antitumor activity of STAT3 inhibition. In vivo administration of NSC-743380 suppressed tumor growth and p-STAT3 in lung tumors. Our results indicate that NSC-743380 is a potent anticancer agent for lung cancer and that its apoptotic effects in lung cancer cells are mediated by induction of ROS through STAT3 inhibition.
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