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^[1][2].

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.

857.11

C₅₂H₆₄N₄O₇

1374647-07-0

[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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Crump CJ, et al. Development of clickable active site-directed photoaffinity probes for γ-secretase. Bioorg Med Chem Lett. 2012;22(8):2997-3000.

  [2]. Ballard TE, et al. Investigating γ-secretase protein interactions in live cells using active site-directed clickable dual-photoaffinity probesMed. Chem. Commun. 2013 Nov 04;5:321-327.