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Description

A cell-permeable, selenium-to-sulfur substituted Ebselen (Cat. No. 324483) derivative that exhibits similar NOX2 inhibitory activity as Ebselen by blocking p22phox c-terminal PRD (proline-rich domain) and p47phoxbis-SH3 interaction. Although less potent than Ebselen in cell-free p22phox PRD-p47phoxbis-SH3 binding (IC50 = 4 vs. 0.3 µ,M) and NOX2 activity (IC50 = 4 vs. 0.6 µ,M) assays, Thr101 is more potent and NOX2-selective than Ebselen in cell-based assays (Thr101 IC50 /Ebselen IC50 = 0.3/0.5, 3/0.15, 8/no inhibition, 8/0.7 µ,M, respectively, against NOX2, NOX1, NOX4, and NOX5) and exhibits no glutathione peroxidase activity.Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water., A cell-permeable, selenium-to-sulfur substituted Ebselen (Cat. No. 324483) derivative that exhibits similar NOX2 inhibitory activity as Ebselen by blocking p22phox c-terminal PRD (proline-rich domain) and p47phoxbis-SH3 interaction. Although less potent than Ebselen in cell-free p22phox PRD-p47phoxbis-SH3 binding (IC50 = 4 vs. 0.3 µ,M) and NOX2 activity (IC50 = 4 vs. 0.6 µ,M) assays, Thr101 is more potent and NOX2-selective than Ebselen in cell-based assays (Thr101 IC50 /Ebselen IC50 = 0.3/0.5, 3/0.15, 8/no inhibition, 8/0.7 µ,M, respectively, against NOX2, NOX1, NOX4, and NOX5) and exhibits no glutathione peroxidase activity.