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IRAK4 inhibitor 28 is an inhibitor of IL-1 receptor-associated kinase 4 (IRAK4; IC50 = 0.005 µM).1 It is selective for IRAK4 over IRAK1, CDC-like kinase 1 (Clk1), and Clk3 (IC50s = 0.023, 0.05, and >1 µM, respectively) but does inhibit Clk2, Clk4, and haspin (IC50s = 0.005, 0.008, and 0.004 µM, respectively). IRAK4 inhibitor 28 (0.12-3.3 µM) inhibits IκBα phosphorylation in OCI-LY10 diffuse large B cell lymphoma (DLBCL) cells. In vivo, IRAK4 inhibitor 28 (12.5 mg/kg) reduces tumor volume in an OCI-LY10 mouse xenograft model.
WARNING This product is not for human or veterinary use.
1. Discovery and optimization of pyrrolopyrimidine inhibitors of interleukin-