539649

PKCθ/δ Inhibitor

• Synonym(e): PKCθ/δ Inhibitor, 5-(3,4-Dimethoxyphenyl)-4-(1H-indol-5-ylamino)-3-pyridinecarbonitrile
• Empirische Formel (Hill-System): C₂₂H₁₈N₄O₂
• Molekulargewicht: 370.40
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥95% (HPLC)
• Qualitätsniveau: 100
• Form: powder
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: light yellow
• Löslichkeit: ethanol: 1 mg/mL; DMSO: 100 mg/mL
• Versandbedingung: ambient
• Lagertemp.: 2-8°C

Beschreibung

Allgemeine Beschreibung

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).

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 2
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable