DIBENZAZEPINE Chemical Properties

Melting point:

257-259?C

Boiling point:

801.3±65.0 °C(Predicted)

Density 

1.35

storage temp. 

-20°C

solubility 

DMSO: soluble15mg/mL, clear

pka

12.76±0.20(Predicted)

form 

White solid

color 

white to beige

InChIKey

QSHGISMANBKLQL-OWJWWREXSA-N

Safety Information

Hazard Codes 

Xi

Risk Statements 

36/37/38

Safety Statements 

26

WGK Germany 

3

HS Code 

29337900

DIBENZAZEPINE Usage And Synthesis

Description

γ-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 (Aβ), 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 γ-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 Aβ40 by reducing Aβ40 levels by 71%.

Chemical Properties

White Solid

Uses

γ-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 (Aβ), 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 γ-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 Aβ40 by reducing Aβ40 levels by 71%.

Uses

DIBENZAZEPINE is a dipeptidic-secretase inhibitor and a antiAlzheimer agent.

Uses

A dipeptidic γ-secretase inhibitor. AntiAlzheimer agent.

General Description

A cell-permeable, potent γ-secretase inhibitor that significantly lowers both brain and plasma Aβ₄₀ levels by ~72% in Tg2576 mutant APP transgenic mouse model (100 μmol/kg, b.i.d). Induces a heterogeneous reorganization of the crypt structural-proliferative units in the intestinal tract and of the stem cell niche in the colon. Also potently inhibits Notch processing (IC₅₀ = 1.7 nM in SupT1 cells) and induces conversion of proliferative crypt cells to post-mitotic goblet cells in both the C57BL/6 and Apc^Min mouse models (10 μmol/kg, i.p).

Biochem/physiol Actions

Cell permeable: yes

target

APPL

storage

-20°C

DIBENZAZEPINE(209984-56-5)Related Product Information

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• Semagacestat
• DAPT
• LY411575
• RO4929097
• MK-0752