539649

PKCθ/δ Inhibitor

• Synonyme(s) : PKCθ/δ Inhibitor, 5-(3,4-Dimethoxyphenyl)-4-(1H-indol-5-ylamino)-3-pyridinecarbonitrile
• Formule empirique (notation de Hill): C₂₂H₁₈N₄O₂
• Poids moléculaire : 370.40
• Code UNSPSC : 12352200

Propriétés

• Pureté: ≥95% (HPLC)
• Niveau de qualité: 100
• Forme: powder
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: light yellow
• Solubilité: ethanol: 1 mg/mL; DMSO: 100 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C

Description

Description générale

A cell-permeable pyridinecarbonitrile compound that acts as a potent, ATP-competitive (K_i = 79 nM, using PKCθ KD in coupled PK/LDH assays), and isozyme-selective PKCθ inhibitor (IC₅₀ = 70 nM) with much reduced potency against other novel PKCs (IC₅₀ = 0.35, 2.33, and 16.35 µM against δ, ε, and η isoforms, respectively) and little or no activity against the conventional PKCβ and atypical PKCζ (IC₅₀ >50 µM) as well as a panel of 18 other commonly studied cellular kinases (IC₅₀ >10 µM). Shown to preferentially inhibit IL-2 production from anti-CD3- and anti-CD28-activated T cells derived from wild-type over PKCθ-knockout mice (IC₅₀ = 58 and 231 nM, respectively).

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Autres remarques

Cole, D.C., et al. 2008. J. Med. Chem.51, 5958.

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 2
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable