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Description

A cell-permeable cross-conjugated alpha,beta-unsaturated dienone compound that induces caspase activation and apoptosis (IC50 = 1.76 and 1.6 µ,M in E1A and E1A/C9DN cells, respectively) via the apoptosome-independent mitochondrial pathway by selectively inhibiting ubiquitin isopeptidase activity (IC50 ~30 µ,M). The cellular expression of Bax and Bak is essential for G5-activated apoptosis, while Bcl-2 appears to protect cells against the effect of G5. G5 is more potent than, but otherwise exhibits similar pharmacological effects as, Ubiquitin Isopeptidase Inhibitor II, F6 (Cat. No. 662126). At higher concentrations (5-10 µ,M), shown to induce necrosis in apoptosis-resistant MEFs-DKO., A cell-permeable cross-conjugated alpha,beta-unsaturated dienone compound that induces caspase activation and apoptosis (IC50 = 1.76 and 1.6 µ,M in E1A and E1A/C9DN cells, respectively) via the apoptosome-independent mitochondrial pathway by selectively inhibiting ubiquitin isopeptidase activity (IC50 = ~ 30 µ,M). The cellular expression of Bax and Bak is essential for G5-activated apoptosis, while Bcl-2 appears to protect cells against the effect of G5. G5 is more potent than, but otherwise exhibits similar pharmacological effects as, Ubiquitin Isopeptidase Inhibitor II, F6 (Cat. No. 662126). At higher concentrations (5-10 µ,M), shown to induce necrosis in apoptosis-resistant MEFs-DKO.