5.31237

IRAK4 Inhibitor, Compound 26

• Synonyme(s) : IRAK4 Inhibitor, Compound 26, Interleukin-1 Receptor Associated Kinase 4 Inhibitor
• Formule empirique (notation de Hill): C₂₅H₂₇N₅O₂
• Numéro CAS: 1604034-71-0
• Poids moléculaire : 429.51
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: ≥98% (HPLC)
• Niveau de qualité: 100
• Forme: powder
• Puissance: 94 pM IC₅₀
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: pale yellow
• Solubilité: DMSO: 50 mg/mL
• Température de stockage: 2-8°C

Description

Description générale

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.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
IRAK4

Reversible: yes

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

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

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 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable