662125

Ubiquitin Isopeptidase Inhibitor I, G5

The Ubiquitin Isopeptidase Inhibitor I, G5, also referenced under CAS 108477-18-5, controls the biological activity of Ubiquitin Isopeptidase. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

• Synonym(s): Ubiquitin Isopeptidase Inhibitor I, G5, 3,5-bis((4-Nitrophenyl)methylene)-1,1-dioxide, tetrahydro-4H-thiopyran-4-one, NSC-144303
• Empirical Formula (Hill Notation): C₁₉H₁₄N₂O₇S
• CAS Number: 108477-18-5
• Molecular Weight: 414.39
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: yellow
• solubility: DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Description

General description

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.

Biochem/physiol Actions

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

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

Reconstitution

Unstable in DMSO; reconstitute just prior to use.

Other Notes

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

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable