LMP2-IN-1 is an orally bioavailable, brain-permeable macrocyclic peptide epoxyketone, acts as a selective and irreversible inhibitor of LMP2 ( IC 50 = 87 nM). LMP2-IN-1 rapidly distributes to the brain and forms an irreversible LMP2:AR-01 adduct. LMP2-IN-1 improves memory function and rescues reactive astrocytes in 5xFAD mouse models of Alzheimer's disease (AD).
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