YK5

YK5 is a rationally designed, potent, and selective small molecule inhibitor of heat shock protein 70 (Hsp70). Developed by researchers at the Memorial Sloan Kettering Cancer Center and St. John's University, YK5 binds to an allosteric pocket in the nucleotide-binding domain of cytosolic Hsp70s, specifically forming a covalent bond with Cys267. By inhibiting Hsp70, YK5 disrupts the formation of active oncogenic Hsp70/Hsp90/client protein complexes, leading to the destabilization and proteasomal clearance of onco-client proteins such as HER2, Raf-1, and Akt. This mechanism induces apoptosis and inhibits cell proliferation in various cancer models, including breast cancer and acute myeloid leukemia.

Other names

N-(6-amino-2-((4,6-dimethoxy-2-(4-methylpiperazin-1-yl)pyrimidin-5-yl)thio)pyrimidin-4-yl)acrylamideN-[6-amino-2-[4,6-dimethoxy-2-(4-methylpiperazin-1-yl)pyrimidin-5-yl]sulfanylpyrimidin-4-yl]prop-2-enamide