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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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: 209986-17-4
- 分子式: C27H24F2N4O3
- 分子量:490.50
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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
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SH-SY5Y | IC50 |
1 nM
Compound: 66
|
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
|
[PMID: 19694467] |
| SH-SY5Y | IC50 |
2.7 nM
Compound: 66
|
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
|
[PMID: 19694467] |
化学情報
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CAS 番号 209986-17-4
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分子量 490.50
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分子式 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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別名
γ-Secretase-IN-1 (GMP)
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輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)