5.31237

IRAK4 Inhibitor, Compound 26

• Sinónimos: IRAK4 Inhibitor, Compound 26, Interleukin-1 Receptor Associated Kinase 4 Inhibitor
• Fórmula empírica (notación de Hill): C₂₅H₂₇N₅O₂
• Número de CAS: 1604034-71-0
• Peso molecular: 429.51
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Análisis: ≥98% (HPLC)
• Nivel de calidad: 100
• formulario: powder
• potencia: 94 pM IC₅₀
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: pale yellow
• solubilidad: DMSO: 50 mg/mL
• temp. de almacenamiento: 2-8°C

Descripción

Descripción general

A cell permeable indolo[2,3-c]quinoline derivatived compound that acts as a selective and highly potent inhibitor of interleukin-1 receptor associated kinase (IRAK4; IC₅₀ = 94 pM). Displays much reduced potency against IRAK1 (IC₅₀ = 65 nM) and displays high selectivity over a panel of other 27 kinases, including several involved in TLR-mediated signaling. Blocks R848-induced TNF-α and IL-6 production in primary human monocytes and inhibits LPS-induced TNF-α production in mice (100 mpk). Shows minimal inhibition of Cyp2C9, 2D6, and 3A4 and has excellent microsomal stability and desirable aqueous solubility (100 μg/ml at pH 7.4).

A cell permeable indolo[2,3-c]quinoline derivatived compound that acts as a selective and highly potent inhibitor of interleukin-1 receptor associated kinase (IRAK4; IC₅₀ = 94 pM). Displays much reduced potency against IRAK1 (IC₅₀ = 65 nM) and displays high selectivity over a panel of other 27 kinases, including several involved in TLR-mediated signaling. Blocks R848-induced TNF-α and IL-6 production in primary human monocytes and inhibits LPS-induced TNF-α production in mice (100 mpk). Shows minimal inhibition of Cyp2C9, 2D6, and 3A4 and has excellent microsomal stability and desirable aqueous solubility (100 μg/ml at pH 7.4).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Primary Target
IRAK4

Reversible: yes

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Otras notas

Tumey, L.N., et al. 2014 Bioorg. Med. Chem. Lett. 24, 2066.

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