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Beschreibung

A cell-permeable diarylsulfonamide (DASA) compound that acts as a potent and selective activator of tumor-specific M2 isozyme of pyruvate kinase (PKM2, AC50 = 65 nM). Pretreatment of A549 (adenocarcinomic human alveolar basal epithelial cells) with DASA-10 (~10 µ,M) prevents hydrogen peroxide, diamide, and hypoxia-induced inactivation of PKM2. DASA treatment is shown to cause a diminution in cellular glutathione levels, and higher oxidative stress-induced cell death.