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γ-Secretase Inhibitor BZ
- Compound E - Gamma-Secretase Inhibitor XXI
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C27H24F2N4O3
- MW: 490.5
Description
γ-Secretase Inhibitor BZ (Compound E) is a very potent and cell-permeable Gamma (γ)-secretase inhibitor (GSI) that potently inhibits Notch processing with an IC50 value of 2.2 nM in SupT1 cells. γ-Secretase Inhibitor BZ also inhibits β-amyloid production in cell culture with an IC50 value of 0.3 nM.
γ-Secretase is a multi-subunit protease complex responsible for the cleavage of Notch receptors and amyloid precursor protein (APP). Through inhibition of γ-secretase activity, Compound E suppresses Notch signaling and amyloidogenic processing, making it a valuable tool for studies of cell differentiation, developmental biology, neurodegeneration, and Alzheimer's disease-related pathways.
Key Features
- Very potent Gamma (γ)-secretase inhibitor
- IC50: 2.2 nM for inhibition of Notch processing
- IC50: 0.3 nM for inhibition of β-amyloid production
- Cell-permeable compound
- Widely used tool for Notch and amyloid biology research
Applications
- Notch signaling research
- Gamma (γ)-Secretase biology studies
- β-Amyloid and APP processing research
- Neurodegeneration and Alzheimer's disease studies
- Cell differentiation and developmental biology investigations
More Information
| Parent CAS No. | 209986-17-4 |
|---|---|
| Chemical Name | (S)-2-[2-(3,5-Difluoro-phenyl)-acetylamino]-N-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-propionamide |
| SMILES | C1(F)C=C(CC(=O)N[C@@H](C)C(=O)N[C@@H]2C(=O)N(C)C3C=CC=CC=3C(C3C=CC=CC=3)=N2)C=C(F)C=1 |&1:8,13,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C27H24F2N4O3/c1-16(30-23(34)14-17-12-19(28)15-20(29)13-17)26(35)32-25-27(36)33(2)22-11-7-6-10-21(22)24(31-25)18-8-4-3-5-9-18/h3-13,15-16,25H,14H2,1-2H3,(H,30,34)(H,32,35)/t16-,25?/m0/s1 |
| InChiKey | JNGZXGGOCLZBFB-YPHZTSLFSA-N |
| CID | 22984074 |
| Short Description | γ-Secretase inhibitor |
References
- D Seiffert et al. Presenilin-1 and -2 Are Molecular Targets for γ-Secretase Inhibitors. J. Biol. Chem. 2000, 275, 34086-34091.
- 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.
- 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.
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