5.31237

IRAK4 Inhibitor, Compound 26

• Synonym(e): IRAK4 Inhibitor, Compound 26, Interleukin-1 Receptor Associated Kinase 4 Inhibitor
• Empirische Formel (Hill-System): C₂₅H₂₇N₅O₂
• CAS-Nummer: 1604034-71-0
• Molekulargewicht: 429.51
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Qualitätsniveau: 100
• Form: powder
• Wirksamkeit: 94 pM IC₅₀
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: pale yellow
• Löslichkeit: DMSO: 50 mg/mL
• Lagertemp.: 2-8°C

Beschreibung

Allgemeine Beschreibung

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.

Biochem./physiol. Wirkung

Cell permeable: yes

Primary Target
IRAK4

Reversible: yes

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable