IKKΒ-IN-5 is an orally active and selective inhibitor of IKKβ, with an IC50 value of 7.5 nM. It directly suppresses IKKβ phosphorylation, thereby mitigating NF-κB-mediated inflammation and survival signaling while enhancing autophagy (autophagy) flux. IKKΒ-IN-5 demonstrates a sixfold selectivity for IKKβ over the homologous kinase IKKα. This compound exhibits potent antiproliferative effects through a dual mechanism of inducing G₂/M cell cycle arrest and activating autophagy (autophagy), even under in vitro inflammatory stimulus conditions. IKKΒ-IN-5 shows favorable pharmacokinetic properties in vivo and inhibits tumor growth. It is applicable in research related to colorectal cancer and other potentially inflammation-driven malignancies.

IKKβ:7.5 nM