DBZ

gamma-Secretase is a multi-subunit aspartyl protease that cleaves amyloid precursor protein (APP) and many other type 1 transmembrane proteins, including Notch, E-cadherin, and ErbB4. The proteolysis of APP by secretases produces beta amyloid (Abeta), a 39- to 42-amino acid peptide which forms the amyloid plaques that are characteristic of Alzheimer's disease. DBZ is a dipeptidic inhibitor of gamma-secretase that potently blocks the cleavage of Notch into its active signaling effector, Notch intracellular domain, in human T cell lymphoma (SupT1) cells (IC50 = 1.7 nM). Within 4 hours after a single 100 µM/kg dose, DBZ demonstrates anti-Alzheimer activity in an APP transgenic mouse model characterized by high levels of Abeta40 by reducing Abeta40 levels by 71%.Formal Name: N-[(1S)-2-[[(7S)-6,7-dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluoro-benzeneacetamide. CAS Number: 209984-56-5. Synonyms: Dibenzazepine, YO-01027. Molecular Formula: C26H23F2N3O3. Formula Weight: 463.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 45 mg/ml. lambdamax: 232 nm. SMILES: O=C(CC1=CC(F)=CC(F)=C1)N[C@@H](C)C(N[C@H]2C(C=CC=C3)=C3C(C=CC=C4)=C4N(C)C2=O)=O. InChi Code: InChI=1S/C26H23F2N3O3/c1-15(29-23(32)13-16-11-17(27)14-18(28)12-16)25(33)30-24-21-9-4-3-7-19(21)20-8-5-6-10-22(20)31(2)26(24)34/h3-12,14-15,24H,13H2,1-2H3,(H,29,32)(H,30,33)/t15-,24-/m0/s1. InChi Key: QSHGISMANBKLQL-OWJWWREXSA-N.