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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1374647-07-0
- 分子式: C52H64N4O7
- 分子量:857.11
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
体外実験
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.
化学情報
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CAS 番号 1374647-07-0
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分子量 857.11
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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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
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)