Biochem/physiol Actions

IKK-16 is a selective inhibitor of I K B kinase (IKK), part of the upstream NF- K B signal transduction cascade involved in the cellular response to inflammation. IKK-16 has IC₅₀ values of 40, 70 and 200 nM for IKKβ (IKK-2), IKK complex and IKKα (IKK-1) respectively. In a mouse sepsis model, IKK-16 reduced the multiple organ dysfunction, showing an antiinflammatory and endothelial protective effect likely mediated by inhibition of inflammation through NF- K B. IKK-16 has also been found to have some activity as an inhibitor of protein kinase D (PKD) and of multidrug resistance protein 1 (MDR1, ABCB1).