IKKα, a member of the IKK family, possesses two kinase domains responsible for regulating the phosphorylation and degradation of IκB proteins. It specifically phosphorylates certain residues of IκB proteins (such as Ser32 and Ser36), leading to the degradation of IκB and subsequent activation of the NF-κB signaling pathway. IKKα plays a significant role in the immune system, particularly in regulating T-cell functions. It controls T-cell metabolism and proliferation, thereby influencing immune responses. Additionally, IKKα modulates the synthesis of cytokines, regulating interactions among immune cells. Studies have indicated abnormal expression or activity of IKKα in various cancers. Targeting IKKα represents a potential new strategy for cancer therapy. IKKα is also involved in the pathogenesis of multiple inflammatory diseases. Inhibitors of IKKα can alleviate inflammatory reactions, offering new avenues for treating these conditions.