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LY2409881 is a potent and selective small molecule inhibitor of IκB kinase beta (IKKβ, also known as IKK2), with an IC50 of 30 nM and greater than 10-fold selectivity over IKK1 and other common kinases[1][9]. It inhibits the NF-κB signaling pathway by blocking IKK2 activity, leading to concentration- and time-dependent growth inhibition and apoptosis in various cancer cell lines, particularly those with constitutively activated NF-κB, such as certain lymphomas[1][3][7]. In preclinical models, LY2409881 demonstrated significant antitumor activity, especially when combined with histone deacetylase inhibitors, suggesting potential as part of combination regimens for hematologic malignancies[3][10]. LY2409881 was originally developed by Eli Lilly[5].
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