Compound E (GMP) is a GMP-grade Compound E (HY-14176). GMP-grade small molecules can be used as adjuvant reagents in cell therapy. Compound E is a γ-secretase inhibitor. Compound E inhibits β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC50 values of 0.24, 0.37, and 0.32 nM, respectively.
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- CAS. Nr.: 209986-17-4
- Formel: C27H24F2N4O3
- Molecular Weight:490.50
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SH-SY5Y | IC50 |
1 nM
Compound: 66
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Displacement of [3H]5-chloro-N-((2S,3R)-5,5,5-trifluoro-1-hydroxy-3-methylpentan-2-yl)thiophene-2-sulfonamide from gamma secretase in human SH-SY5Y cells by competitive binding assay
Displacement of [3H]5-chloro-N-((2S,3R)-5,5,5-trifluoro-1-hydroxy-3-methylpentan-2-yl)thiophene-2-sulfonamide from gamma secretase in human SH-SY5Y cells by competitive binding assay
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[PMID: 19694467] |
| SH-SY5Y | IC50 |
2.7 nM
Compound: 66
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Inhibition of gamma secretase-mediated amyloid beta (1 to 40) production in human SH-SY5Y cells
Inhibition of gamma secretase-mediated amyloid beta (1 to 40) production in human SH-SY5Y cells
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[PMID: 19694467] |
Chemical Information
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CAS. Nr. 209986-17-4
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Molecular Weight 490.50
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Formel C27H24F2N4O3
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SMILES
FC1=CC(CC(N[C@@H](C)C(N[C@@H]2C(N(C)C(C=CC=C3)=C3C(C4=CC=CC=C4)=N2)=O)=O)=O)=CC(F)=C1
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Synonyms
γ-Secretase-IN-1 (GMP)
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Beher D, et al. Pharmacological knock-down of the presenilin 1 heterodimer by a novel γ-secretase inhibitor: implications for presenilin biology[J]. Journal of Biological Chemistry, 2001, 276(48): 45394-45402. [Content Brief]
[2]. Rasul S, et al. Inhibition of γ-secretase induces G2/M arrest and triggers apoptosis in breast cancer cells[J]. British journal of cancer, 2009, 100(12): 1879-1888. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)