L505-yne
L505-yne is an active site-directed γ-secretase inhibitor. L505-yne blocks photoaffinity labeling of PS1-NTF, PS1-CTF, and SPP by clickable GSI photoprobes, binds the γ-secretase complex and inhibits Aβ42 production. L458-BPyne can be used for the research of Alzheimer’s disease.
For research use only. We do not sell to patients.
- CAS No.: 1374647-07-0
- Formula: C52H64N4O7
- Molecular Weight:857.11
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
L505-yne (Compound 5) potently inhibits γ-secretase-mediated Aβ42 production in cell-free HeLa membranes (IC50 = 0.3 nM) and in CHO-APP cells (IC50 = 36 nM)[1].
L505-yne (20 nM; 1 h) prefers for PS1-CTF with minimal PS1-NTF labeling, but also revealed significant labeling of SPP[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 1374647-07-0
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Molecular Weight 857.11
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Formula C52H64N4O7
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SMILES
[C@@H](CC1=CC=CC=C1)(C[C@H]([C@H](CC2=CC=CC=C2)NC(OC(C)(C)C)=O)O)C(N[C@H](C(N[C@@H](CC3=CC=C(C(=O)C4=CC=CC=C4)C=C3)C(NCCCCC#C)=O)=O)CC(C)C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Notch Pathway Solutions
The Notch pathway is a contact-dependent signaling pathway that controls cell-fate decisions, differentiation, proliferation, and tissue patterning through interactions between membrane-bound Notch receptors and membrane-bound ligands on neighboring cells. Canonical Notch signaling is activated when ligand engagement triggers proteolytic release of the Notch intracellular domain, which enters the nucleus and regulates transcription together with DNA-binding transcriptional complexes. In the canonical mechanism, ligand-dependent Notch activation leads to release of the intracellular Notch domain, and presenilin-dependent γ-secretase activity is required for production of the active intracellular signaling fragment. The released intracellular domain functions as a nuclear signal that converts Notch receptor activation at the membrane into transcriptional regulation of target programs such as HES/HEY-family genes and other context-dependent downstream targets. The literature links Notch p
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)