557550

Ro106-9920

A cell-permeable tetrazolopyridazine-phenylsulfoxide compound that displays anti-inflammatory properties.

• Sinónimos: Ro106-9920
• Fórmula empírica (notación de Hill): C₁₀H₇N₅OS
• Número de CAS: 62645-28-7
• Peso molecular: 245.26
• Código UNSPSC: 51111800
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Análisis: ≥95% (HPLC)
• formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; desiccated; protect from light
• color: white
• solubilidad: ethanol: 1 mg/mL; DMSO: 25 mg/mL
• Condiciones de envío: wet ice
• temp. de almacenamiento: −70°C
• InChI: 1S/C10H7N5OS/c16-17(8-4-2-1-3-5-8)10-7-6-9-11-13-14-15(9)12-10/h1-7H
• Clave InChI: JFSXSNSCPNFCDM-UHFFFAOYSA-N

Descripción

Descripción general

A cell-permeable tetrazolopyridazine-phenylsulfoxide compound that displays anti-inflammatory properties. Acts as a highly selective, irreversible inhibitor of IκBαee ubiquitination (IC₅₀ = 2.3 µM). Also reported to prevent degradation of IκBαee in MM6 cells (complete inhibition at ~3-5 µM). Shown to block NF-κB-dependent cytokine expression in human peripheral blood mononuclear cells (PBMN) (IC₅₀ = 600-700 nM for TNF-α, IL-1β, and IL-6 inhibition). Also shown to lower circulating levels of TNFα in LPS-treated rats. Also shown to inhibit 5-lipoxygenase (89% inhibition) and EGFR kinase (63% inhibition) at higher concentrations (10 µM).

A cell-permeable tetrazolopyridazine-phenylsulfoxide compound that displays anti-inflammatory properties. Acts as a highly selective, irreversible inhibitor of IκBαee ubiquitination (IC₅₀ = 2.3 µM). Blocks NF-κB-dependent cytokine expression in human PBMNs (IC₅₀’s = ~ 700 nM for TNF-α, IL-1β, and IL-6 inhibition) and rats. Does not inhibit SCF^βTRCP(IκBα ubiquitin ligase)-mediated β-catenin ubiquitination in Jurkat cells. At 10 µM concentrations, also inhibits the activities of 5-lipoxygenase (by 89%) and EGFR kinase (by 63%).

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Primary Target
IκBαee ubiquitination

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 2.3 µM against IκBαee ubiquitination

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 3 months at -70°C.

Otras notas

Swinney, D.C., et al. 2002. J. Biol. Chem.277, 23573.

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 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable