delta-Secretase Inhibitor 11

delta-Secretase inhibitor 11 is an inhibitor of delta-secretase (IC50 = 0.7 µM), also known as asparagine endopeptidase (AEP) and legumain. It is selective for delta-secretase over cathepsin S, cathepsin L, caspase-3, and caspase-8 (IC50s = >200, >200, 31.86, and 86.71 µM, respectively). delta-Secretase inhibitor 11 inhibits delta-secretase in Pala B-lymphoblastoid cells (IC50 = 0.8 µM). It inhibits glucose-oxygen deprivation-induced cell death in primary mouse neurons when used at a concentration of 2 µM. In vivo, delta-secretase inhibitor 11 (10 mg/kg per day) inhibits brain delta-secretase in wild-type mice and transgenic mice expressing human tauP301S. It reduces the number of cortical and hippocampal tau N368-positive neurons, restores synaptic dysfunction, and improves spatial learning and memory in transgenic mice expressing human tauP301S. delta-Secretase inhibitor 11 (10 mg/kg) reduces hippocampal amyloid-beta (Abeta) deposition and attenuates cognitive deficits in the 5XFAD transgenic mouse model of Alzheimer's disease.Formal Name: 7-(4-morpholinyl)-2,1,3-benzoxadiazol-4-amine. CAS Number: 842964-18-5. Molecular Formula: C10H12N4O2. Formula Weight: 220.2. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, Ethanol: 2 mg/ml, PBS (pH 7.2): Slightly soluble. lambdamax: 234 nm. SMILES: NC1=CC=C(N2CCOCC2)C3=NON=C31. InChi Code: InChI=1S/C10H12N4O2/c11-7-1-2-8(10-9(7)12-16-13-10)14-3-5-15-6-4-14/h1-2H,3-6,11H2. InChi Key: LWCSTSZSZFUHAT-UHFFFAOYSA-N.