AChE/BuChE-IN-1
AChE/BuChE-IN-1 (Compound 1), a chrysin derivative, is a selective butyrylcholinesterase (BuChE) inhibitor with an IC50 of 0.48 μM. AChE/BuChE-IN-1 inhibits acetylcholinesterase (AChE) with an IC50 of 7.16 μM. AChE/BuChE-IN-1 shows strong scavenging ·OH activities with a IC50 of 0.1674 μM. AChE/BuChE-IN-1 inhibits reactive oxygen species (ROS), Aβ1-42 aggregation (self-, Cu2+-induced, AChE-induced). AChE/BuChE-IN-1 has high BBB permeability and bioavailability and low cell toxicity. AChE/BuChE-IN-1 has the potential for Alzheimer' disease (AD) research.
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- CAS 番号: 84212-49-7
- 分子式: C19H19NO4
- 分子量:325.36
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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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AChE |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| DU-145 | IC50 |
17.7 μM
Compound: 8f
|
Cytotoxicity against Homo sapiens (human) DU145 cells by MTT assay
Cytotoxicity against Homo sapiens (human) DU145 cells by MTT assay
|
10.1007/s00044-010-9395-1 |
| HCT-116 | IC50 |
6.2 μM
Compound: 8f
|
Cytotoxicity against Homo sapiens (human) HCT116 cells by MTT assay
Cytotoxicity against Homo sapiens (human) HCT116 cells by MTT assay
|
10.1007/s00044-010-9395-1 |
| HeLa | IC50 |
17.7 μM
Compound: 8f
|
Cytotoxicity against Homo sapiens (human) HeLa cells by MTT assay
Cytotoxicity against Homo sapiens (human) HeLa cells by MTT assay
|
10.1007/s00044-010-9395-1 |
| K562 | IC50 |
17.9 μM
Compound: 8f
|
Cytotoxicity against Homo sapiens (human) K562 cells by MTT assay
Cytotoxicity against Homo sapiens (human) K562 cells by MTT assay
|
10.1007/s00044-010-9395-1 |
| SGC-7901 | IC50 |
10.99 μM
Compound: 8f
|
Cytotoxicity against Homo sapiens (human) SGC7901 cells by MTT assay
Cytotoxicity against Homo sapiens (human) SGC7901 cells by MTT assay
|
10.1007/s00044-010-9395-1 |
AChE/BuChE-IN-1 (Compound 1) is mixed-type inhibitor of competitive inhibition and non-competitive inhibition that can simultaneously bind to CAS and PAS of the AChE and BuChE enzyme. AChE/BuChE-IN-1 has no significant inhibitory effect in the ·DPPH scavenging assay (IC50>500 μM)[1].
AChE/BuChE-IN-1 selectively chelates Cu2+, Fe2+, Zn2+ and Al3+ ions, while had no chelating ability to other biometals[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 84212-49-7
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分子量 325.36
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分子式 C19H19NO4
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SMILES
O=C1C=C(C2=CC=CC=C2)OC3=CC(OCCN(C)C)=CC(O)=C13
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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
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)