Nuclear factor-κB (NF-κB) is a protein complex which modulates gene transcription relevant to cellular responses to inflammation, stress, infection, and other factors. The inhibitor of NF-κB kinase β (IKKβ), in complex with IKKα and IKKγ, phosphorylates inhibitor of NF-κB A and B (IκA and IκB) and other proteins involved in NF-κB signaling, and thus plays a central regulatory role. PS-1145 is a potent inhibitor of IKKβ (IC50 = 88-100 nM). Through this action, it is used to elucidate roles for NF-κB both in cells and in vivo.