557550

Ro106-9920

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

• Synonyme(s) : Ro106-9920
• Formule empirique (notation de Hill): C₁₀H₇N₅OS
• Numéro CAS: 62645-28-7
• Poids moléculaire : 245.26
• Code UNSPSC : 51111800
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; desiccated; protect from light
• Couleur: white
• Solubilité: ethanol: 1 mg/mL; DMSO: 25 mg/mL
• Conditions d'expédition: wet ice
• Température de stockage: −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
• Clé InChI: JFSXSNSCPNFCDM-UHFFFAOYSA-N

Description

Description générale

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%).

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
IκBαee ubiquitination

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 2.3 µM against IκBαee ubiquitination

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable