[HTML][HTML] A selective IKK-2 inhibitor blocks NF-κB-dependent gene expression in interleukin-1β-stimulated synovial fibroblasts
N Kishore, C Sommers, S Mathialagan… - Journal of Biological …, 2003 - ASBMB
NF-κB-induced gene expression contributes significantly to the pathogenesis of
inflammatory diseases such as arthritis. IκB kinase (IKK) is the converging point for the
activation of NF-κB by a broad spectrum of inflammatory agonists and is thus a novel target
for therapeutic intervention. We describe a small molecule, selective inhibitor of IKK-2, SC-
514, which does not inhibit other IKK isoforms or other serine-threonine and tyrosine
kinases. SC-514 inhibits the native IKK complex or recombinant human IKK-1/IKK-2 …
inflammatory diseases such as arthritis. IκB kinase (IKK) is the converging point for the
activation of NF-κB by a broad spectrum of inflammatory agonists and is thus a novel target
for therapeutic intervention. We describe a small molecule, selective inhibitor of IKK-2, SC-
514, which does not inhibit other IKK isoforms or other serine-threonine and tyrosine
kinases. SC-514 inhibits the native IKK complex or recombinant human IKK-1/IKK-2 …