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S3I-210 (also known as NSC 151459) is a small molecule inhibitor that specifically targets the Signal Transducer and Activator of Transcription 3 (STAT3). It acts by binding to the STAT3 SH2 domain, which prevents the dimerization of STAT3 monomers, a critical step for its translocation to the nucleus and subsequent transcriptional activity. In research settings, S3I-210 has been shown to inhibit the growth and survival of various cancer cells, including leukemia stem cells, by suppressing the IL-6/JAK/STAT3 signaling pathway. It is widely used as a chemical probe to study STAT3-dependent biological processes and as a lead compound for developing more potent STAT3-targeted therapies. Additionally, it has been observed to influence mitochondrial homeostasis and downregulate the expression of FOXM1 and its downstream antioxidant targets.
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