Ubiquitin Isopeptidase Inhibitor I, G5

A cell-permeable cross-conjugated α,β-unsaturated dienone compound that induces caspase activation and apoptosis (IC₅₀ = 1.76 and 1.6 µM in E1A and E1A/C9DN cells, respectively) via the apoptosome-independent mitochondrial pathway by selectively inhibiting ubiquitin isopeptidase activity (IC₅₀ = ~ 30 µM). 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 µM), shown to induce necrosis in apoptosis-resistant MEFs-DKO.

A cell-permeable cross-conjugated α,β-unsaturated dienone compound that induces caspase activation and apoptosis (IC₅₀ = 1.76 and 1.6 µM in E1A and E1A/C9DN cells, respectively) via the apoptosome-independent mitochondrial pathway by selectively inhibiting ubiquitin isopeptidase activity (IC₅₀ ~30 µM). 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 µM), shown to induce necrosis in apoptosis-resistant MEFs-DKO.

Cell permeable: yes

Primary Target
Ubiquitin isopeptidase activity

Product does not compete with ATP.

Reversible: no

Target IC₅₀: ~ 30 µM against ubiquitin isopeptidase activity; 1.76 and 1.6 µM for the induction of caspase activation and apoptosis in E1A and E1A/C9DN cells, respectively

Packaged under inert gas

Toxicity: Irritant (B)

Unstable in DMSO; reconstitute just prior to use.

Fontanini, A., et al. 2009. J. Biol. Chem.284, 8369.
Aleo, E., et al. 2006. Cancer Res.66, 9235.

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