Aminogenistein
Aminogenistein is a p56lck inhibitor with a 1.2 μM IC50. Aminogenistein inhibits production of Aβ1-40 and Aβ1-42 peptides. Aminogenistein induces accumulation of APP-CTFα and APP-CTFβ, indicating γ-secretase cleavage inhibition. Aminogenistein can be used for the research of alzheimer's disease.
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- No. CAS: 132018-32-7
- Fòrmula: C15H11NO3
- Peso molecular:253.26
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
p56-Lck 1.2 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | ED50 |
2.72 μg/mL
Compound: 30
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Cytotoxicity against human A549 cells after 6 days by MTT assay
Cytotoxicity against human A549 cells after 6 days by MTT assay
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[PMID: 1812215] |
| HT-29 | ED50 |
2.65 μg/mL
Compound: 30
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Cytotoxicity against human HT-29 cells after 6 days by MTT assay
Cytotoxicity against human HT-29 cells after 6 days by MTT assay
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[PMID: 1812215] |
| Malme-3M | ED50 |
>25 μg/mL
Compound: 30
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Cytotoxicity against human MALME-3M cells after 6 days by MTT assay
Cytotoxicity against human MALME-3M cells after 6 days by MTT assay
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[PMID: 1812215] |
| MCF7 | ED50 |
>25 μg/mL
Compound: 30
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Cytotoxicity against human MCF7 cells after 6 days by MTT assay
Cytotoxicity against human MCF7 cells after 6 days by MTT assay
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[PMID: 1812215] |
| SK-MEL | ED50 |
2.03 μg/mL
Compound: 30
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Cytotoxicity against human SK-MEL cells after 6 days by MTT assay
Cytotoxicity against human SK-MEL cells after 6 days by MTT assay
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[PMID: 1812215] |
In Vitro
Aminogenistein (Compound 1) potently inhibits bovine thymus-derived p56lck with an IC50 of 1.2 μM, and is weakly active against protein kinase C and protein kinase A with IC50 values >300 μM[1].
Aminogenistein (24 h) dose-dependently inhibits Aβ1-40 and Aβ1-42 production in 7W CHO cells overexpressing human APP751, with IC50 values of 5.7 μM and 5.8 μM, respectively[2].
Aminogenistein (10-25 μM; 24 h) does not inhibit β-cleavage of APP in 7W CHO cells overexpressing human APP751 at 10 μM or 25 μM[2].
Aminogenistein (20 μM; 24 h) accumulates APP C-terminal fragments at 20 μM in 7W CHO cells overexpressing human APP751, indicating γ-secretase inhibition[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:7W CHO cells stably transfected with human APP751
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Concentration:10 μM; 25 μM
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Incubation Time:24 h
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Result:Did not impact sAPPβ production at 10 μM and 25 μM.
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Cell Line:7W CHO cells stably transfected with human APP751
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Concentration:20 μM
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Incubation Time:24 h
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Result:Induced accumulation of APP-CTFα and APP-CTFβ at 20 μM.
Did not inhibit APP-CTFβ generation at 20 μM.
Chemical Information
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No. CAS 132018-32-7
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Peso molecular 253.26
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Fòrmula C15H11NO3
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SMILES
O=C1C=C(OC2=CC=C(O)C=C12)C=3C=CC(N)=CC3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Cushman M, et al. Synthesis and biochemical evaluation of a series of aminoflavones as potential inhibitors of protein-tyrosine kinases p56lck, EGFr, and p60v-src. J Med Chem. 1994 Sep 30;37(20):3353-62. [Content Brief]
[2]. Paris D, et al. Flavonoids lower Alzheimer's Aβ production via an NFκB dependent mechanism. Bioinformation. 2011;6(6):229-236. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Aminogenistein Related Classifications
HY-133184 Related Classifications
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