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Description

A cell-permeable, potent, reversible, ATP-competitive and highly selective inhibitor of IKK-2 (IC50 ~3-12 µ,M for IKK-2 homodimer, IKK-1/IKK-2 heterodimer, and IKK-2) that also displays anti-inflammatory properties. Specificity has been reported using a panel of 31 additional kinases, including IKK isoforms IKK-1, IKK-i, and TBK-1 (IC50 >200 µ,M). Shown to specifically block NF-kappaB-dependent gene expression, but not MAP kinase pathways, in stimulated RASF synovial fibroblast cells. Does not inhibit the phosphorylation and activation of the IKK complex.