Biochem/physiol Actions

Reversible: yes

Cell permeable: yes

Primary TargetIRAK4

General description

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.

Legal Information

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

Other Notes

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

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Standard Handling (A)