BAY-888

BAY-888 is a first-in-class, potent, and selective small molecule inhibitor of Casein Kinase 1 Alpha 1 (CSNK1A1), developed by Bayer in collaboration with the Broad Institute. It utilizes a tetrahydro-pyrrolopyridinone scaffold and acts as an ATP-competitive inhibitor. Preclinical studies have demonstrated anti-tumor efficacy in solid tumor models, particularly those with high expression of FAM83 family members (FAM83B and FAM83H), which mediate the subcellular localization of CSNK1A1. BAY-888 is orally bioavailable and has shown activity in xenograft models of colorectal cancer, gastric cancer, urothelial cancer, and diffuse large B-cell lymphoma (DLBCL).