842964-18-5

δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research[1].

Compound 11 (CP11) is an orally active and brain-penetrant delta-secretase (δ-secretase; AEP) inhibitor th at selectively blocks AEP (IC50 = 710 nM) but not other related cysteine proteases (Caspase-3/-8 IC50 = 31.86/86.71 μMCathepsin-S/-L IC50 >200 μM) via a dual active site-directed and allosteric mode of inhibition. CP11 inhibits Pala cellular AEP activity in cultures (IC50 = 800 nM) and improves cognitive functions in murine models of Alzheimerμs disease (AD) in vivo (10 mg/kg tau P301S or 5xFAD mice via daily p.o.) by reducing tau and APP cleavageameliorating synapse loss and augmenting long-term potentiation.

Caspase-3: 31.86 ± 1. μM (IC₅₀); Caspase-8: 86.71 ± 10 μM (IC₅₀)

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[1] Zhang Z, et al. Inhibition of delta-secretase improves cognitive functions in mouse models of Alzheimer's disease. Nat Commun. 2017 Mar 27;8:14740. DOI:10.1038/ncomms14740