JPC0661

JPC0661 is a direct and allosteric inhibitor of ΔFOSB. It inhibits the binding of ΔFOSB/JUND and ΔFOSB to DNA with a micromolar IC50 value (9-52 μM), and directly suppresses ΔFOSB-mediated transcription in vitro with an IC50 of 0.82 μM. In vivo, JPC0661 notably reduces the occupancy of ΔFOSB at genomic AP1 sites. JPC0661 disrupts the formation of the ΔFOSB/JUND-DNA complex by binding to a novel groove outside the ΔFOSBDNA binding cleft. JPC0661 is applicable in Alzheimer's disease research.