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.

• Sinônimo(s): Ubiquitin Isopeptidase Inhibitor I, G5, 3,5-bis((4-Nitrophenyl)methylene)-1,1-dioxide, tetrahydro-4H-thiopyran-4-one, NSC-144303
• Fórmula empírica (Notação de Hill): C₁₉H₁₄N₂O₇S
• Número CAS: 108477-18-5
• Peso molecular: 414.39
• Código UNSPSC: 12352200
• NACRES: NA.54

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥97% (HPLC)
• forma: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: yellow
• solubilidade: DMSO: 10 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: 2-8°C

Descrição

Descrição geral

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.

Ações bioquímicas/fisiológicas

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

Embalagem

Packaged under inert gas

Advertência

Toxicity: Irritant (B)

Reconstituição

Unstable in DMSO; reconstitute just prior to use.

Outras notas

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

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 2
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable