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.

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

Propiedades

• Nivel de calidad: 100
• Análisis: ≥97% (HPLC)
• formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: yellow
• solubilidad: DMSO: 10 mg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: 2-8°C

Descripción

Descripción general

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.

Acciones bioquímicas o 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

Envase

Packaged under inert gas

Advertencia

Toxicity: Irritant (B)

Reconstitución

Unstable in DMSO; reconstitute just prior to use.

Otras notas

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

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 2
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable