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γ-Secretase Inhibitor BZ

Compound E

CAS 209986-17-4

C27H24F2N4O3  MW 490.51 

Purity: 99% (optically pure)

 

 

 

 

Ordering Information:

 

Cat. No. Axon 1487    Prime Source Promotion

 

Qty1: 1 mg (research sample) / €105  $137

 

Qty2: 5 mg (research sample) / €235  $306

 

Qty3: on request

 

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Biological Activity:

 

Very potent and cell-permeable inhibitor of γ-secretase; potently inhibits Notch processing (IC50 values to be 2.2 nM in SupT1 cells); inhibits β-ammyloid production in cell culture with an IC50 of 0.3 nM.

 

References:

 

D Seiffert et al. Presenilin-1 and -2 Are Molecular Targets for γ-Secretase
Inhibitors. J. Biol. Chem. 2000, 275, 34086-34091. [online]

 

J Milano et al. Modulation of Notch Processing by γ-Secretase Inhibitors Causes Intestinal Goblet Cell Metaplasia and Induction of Genes Known to Specify Gut Secretory Lineage Differentiation. Toxicol. Sci. 2004, 82(1), 341-358. [online]

 

T Aleksic and SM Feller. Gamma-secretase inhibition combined with platinum compounds enhances cell death in a large subset of colorectal cancer cells. Cell Communication and Signaling 2008, 6, 8. [online]

 

 

Chemical Name: (S)-2-[2-(3,5-Difluoro-phenyl)-acetylamino]-N-((S)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-propionamide; aka γ-Secretase inhibitor XXI, Compound E 

 

γ-Secretase inhibitor BZ | Axon Medchem | Axon 1487 | Compound E

 

Axon Ligands TM - Research chemicals for biological study. Some high-profile samples could be provided under terms of contract research synthesis.  

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Axon Ligands In The Field:

 

BACE-1 inhibitor | β-Secretase inh.

BZ | γ-Secretase inhibitor

DAPT | γ-Secretase inhibitor

DBZ | γ-Secretase inhibitor

 

 

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