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Beschreibung

A cell-permeable tetrahydroisoquinoline derivative that acts as a direct, non-covalent inhibitor of Keap1 - Nrf2 (Kelch-like ECH-associated protein 1 - nuclear factor erythroid 2-related factor 2) protein - protein interaction (Kd = 1 µ,M) that causes the dissociation of Nrf2 from keap1 in the cytosol. Exhibits ARE-inducing activity (EC50 = 18 µ,M in U2OS Keap1-Nrf2 functional assay) and promotes Nrf2 translocation to the nucleus (EC50 = 12 µ,M). Has good solubility in aqueous buffers (>100 µ,M in phosphate buffered saline)., A cell-permeable tetrahydroisoquinoline derivative that acts as a direct, non-covalent inhibitor of Keap1 - Nrf2 (Kelch-like ECH-associated protein 1 - nuclear factor erythroid 2-related factor 2) protein - protein interaction (Kd = 1 µ,M) that causes the dissociation of Nrf2 from keap1 in the cytosol. Exhibits ARE-inducing activity (EC50 = 18 µ,M in U2OS Keap1-Nrf2 functional assay) and promotes Nrf2 translocation to the nucleus (EC50 = 12 µ,M). Has good solubility in aqueous buffers (>100 µ,M in phosphate buffered saline).Please note that the molecular weight for this compound is batch-specific due to variable water content.