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PBIT (S,S'-1,4-phenylenebis(1,2-ethanediyl)bis-isothiourea) is a potent and selective small molecule inhibitor of inducible nitric oxide synthase (iNOS). It is primarily utilized as a research tool in preclinical oncology to investigate the role of nitric oxide in tumor development and progression. In rodent models, PBIT has demonstrated significant chemopreventive activity against N-nitrosomethylbenzylamine (NMBA)-induced esophageal squamous cell carcinoma, both as a single agent and in combination with cyclooxygenase-2 (COX-2) inhibitors like celecoxib. By selectively targeting iNOS, PBIT reduces the inflammatory and pro-tumorigenic effects of excessive nitric oxide production without significantly affecting other nitric oxide synthase isoforms. While it has shown efficacy in reducing tumor incidence and multiplicity in animal models, it remains a research-stage compound and has not transitioned into clinical development.
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