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γ-Secretase Inhibitor DBZ
- Deshydroxy LY411575 - YO-01027- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C26H23F2N3O3
- MW: 463.48
Description
γ-Secretase Inhibitor DBZ (Dibenzazepine) is a very potent and cell-permeable Gamma (γ)-secretase inhibitor (GSI) that potently inhibits Notch processing with an IC50 value of 1.7 nM in SupT1 cells. By inhibiting γ-secretase activity, DBZ prevents cleavage and activation of Notch receptors, thereby suppressing downstream Notch signaling.
γ-Secretase is a multi-subunit protease complex responsible for the processing of Notch receptors and amyloid precursor protein (APP). Due to its central role in cell fate determination, lineage commitment, differentiation, and cancer biology, DBZ is widely used as a research tool for investigating Notch signaling and γ-secretase-dependent pathways.
Key Features
- Very potent Gamma (γ)-secretase inhibitor
- IC50: 1.7 nM in SupT1 cells
- Cell-permeable compound
- Potently inhibits Notch processing
- Widely used tool for Notch pathway research
Applications
- Notch signaling research
- γ-Secretase biology studies
- Cell differentiation and lineage commitment research
- Cancer and developmental biology investigations
- Amyloid processing and neurobiology studies
More Information
| Parent CAS No. | 209984-56-5 |
|---|---|
| Chemical Name | (S)-2-(2-(3,5-Difluorophenyl)acetamido)-N-((S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)propanamide |
| SMILES | C1(F)C=C(CC(=O)N[C@@H](C)C(=O)N[C@@H]2C(=O)N(C)C3C=CC=CC=3C3C=CC=CC2=3)C=C(F)C=1 |&1:8,13,r| |
| MFCD | N.A. |
| InChi | 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 |
| InChiKey | QSHGISMANBKLQL-FZADBTJQSA-N |
| CID | 11476771 |
| Short Description | γ-Secretase inhibitor |
References
- 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.
- TV Arumugam et al. Gamma secretase–mediated Notch signaling worsens brain damage and functional outcome in ischemic stroke. Nature Medicine 2006, 12, 621-623.
- 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.
- List of publications using γ-Secretase Inhibitor DBZ (Axon 1488) purchased from Axon Medchem
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