539649

PKCθ/δ Inhibitor

• Synonym(s): PKCθ/δ Inhibitor, 5-(3,4-Dimethoxyphenyl)-4-(1H-indol-5-ylamino)-3-pyridinecarbonitrile
• Empirical Formula (Hill Notation): C₂₂H₁₈N₄O₂
• Molecular Weight: 370.40
• UNSPSC Code: 12352200

Properties

• Assay: ≥95% (HPLC)
• Quality Level: 100
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: light yellow
• solubility: ethanol: 1 mg/mL; DMSO: 100 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Description

General description

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).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

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

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable