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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-alpha and IL-6 production in primary human monocytes and inhibits LPS-induced TNF-alpha production in mice (100 mpk). Shows minimal inhibition of Cyp2C9, 2D6, and 3A4 and has excellent microsomal stability and desirable aqueous solubility (100 mug/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-alpha and IL-6 production in primary human monocytes and inhibits LPS-induced TNF-alpha production in mice (100 mpk). Shows minimal inhibition of Cyp2C9, 2D6, and 3A4 and has excellent microsomal stability and desirable aqueous solubility (100 mug/ml at pH 7.4).Please note that the molecular weight for this compound is batch-specific due to variable water content.