BAY 65-1942

BAY 65-1942 is a selective, ATP-competitive small molecule inhibitor of IκB kinase β (IKKβ), originally developed by Bayer. It possesses high potency with a Ki value of 2 nM and exhibits greater than 50-fold selectivity for IKKβ over its isoform IKKα. The compound functions by blocking the IKKβ/NF-κB signaling pathway, which is a key regulator of inflammatory responses and cancer cell survival mechanisms. In the context of head and neck squamous cell carcinoma (HNSCC), BAY 65-1942 has been studied as a sensitizing agent to overcome resistance to EGFR inhibitors such as gefitinib and erlotinib. Preclinical evidence suggests that co-targeting these pathways can suppress compensatory NF-κB activation, leading to synergistic antitumor effects in cell lines and xenograft models.

Other names

CmpdA