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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- CAS. Nr.: 132018-32-7
- Formel: C15H11NO3
- Molecular Weight:253.26
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
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
|
[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
|
[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
|
[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. Further protocols information, click here.
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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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CAS. Nr. 132018-32-7
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Molecular Weight 253.26
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Formel C15H11NO3
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SMILES
O=C1C=C(OC2=CC=C(O)C=C12)C=3C=CC(N)=CC3
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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.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Reinheit & Dokumentation
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)