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BMS 345541 is a cell permeable inhibitor of the IκB kinases IKKα and IKKβ (IC50s = 4 and 0.3 μM). It is without effect against a panel of other serine/threonine and tyrosine kinases at 100 μM. BMS 345541 inhibits signaling through nuclear factor-κB (NF-κB) both in cells and in vivo, showing excellent pharmacokinetics in mice. It blocks joint inflammation and damage in collagen-induced arthritis in mice and induces apoptosis in melanoma cells both in vitro and in vivo. BMS 345541 is used to explore novel roles for IKK phosphorylation and NF-κB signaling.

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