3056058-96-6
Chemical Structure
LMP2-IN-1
- CAS No.: 3056058-96-6
- Formula:C23H36FN3O6
- Molecular Weight:469.55
InChIKey: LUPXHLYUJILCJO-RBIWONGKSA-N
SMILES: F[C@@H]1C[C@@H](C(N[C@@H](COCCCCCC2=O)C(N[C@@H](CC(C)C)C([C@]3(C)OC3)=O)=O)=O)N2C1
Biological Activity: LMP2-IN-1 is an orally bioavailable, brain-permeable macrocyclic peptide epoxyketone, acts as a selective and irreversible inhibitor of LMP2 (IC50 = 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)[1][2].
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LMP2-IN-1 | LMP2-IN-1 is an orally bioavailable, brain-permeable macrocyclic peptide epoxyketone, acts as a selective and irreversible inhibitor of LMP2 (IC50 = 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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- [1]. Thapa Magar TB, et al. Pharmacokinetics, Target Engagement of an Immunoproteasome Subunit Low-Molecular-Mass Polypeptide 2 (LMP2) Inhibitor AR-01, and Its Anti-Alzheimer's Effects in Rodents. ACS Pharmacol Transl Sci. 2026 Jun 29;9(7):1869-1880. [Content Brief]
- [2]. Park JE, et al. Brain-Permeable Immunoproteasome-Targeting Macrocyclic Peptide Epoxyketones for Alzheimer's Disease. J Med Chem. 2024 May 9;67(9):7146-7157. [Content Brief]
Keywords
