1. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Cell Cycle/DNA Damage Apoptosis
  2. Aryl Hydrocarbon Receptor Reactive Oxygen Species (ROS) DNA Alkylator/Crosslinker DNA/RNA Synthesis Caspase Apoptosis HIF/HIF Prolyl-Hydroxylase
  3. Aminoflavone

Aminoflavone is an anti-tumor agent. Aminoflavone inhibits the expression of ITGA6/SOX2 by activating the AhR-miR-125b-2-3p axis, thereby targeting breast cancer stem cells. Aminoflavone induces an increase in intracellular ROS, increases the level of oxidative DNA damage marker 8-oxodG and DNA-protein cross-links. Aminoflavone causes S-phase arrest, activates caspase-3/8/9 and induces apoptosis (apoptosis). Aminoflavone inhibits HIF-1α expression in a manner independent of AhR. Aminoflavone can be used for the study of breast cancer.

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Aminoflavone

Aminoflavone Chemical Structure

CAS No. : 165179-35-1

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Description

Aminoflavone is an anti-tumor agent. Aminoflavone inhibits the expression of ITGA6/SOX2 by activating the AhR-miR-125b-2-3p axis, thereby targeting breast cancer stem cells. Aminoflavone induces an increase in intracellular ROS, increases the level of oxidative DNA damage marker 8-oxodG and DNA-protein cross-links. Aminoflavone causes S-phase arrest, activates caspase-3/8/9 and induces apoptosis (apoptosis). Aminoflavone inhibits HIF-1α expression in a manner independent of AhR. Aminoflavone can be used for the study of breast cancer[1][2][3].

Cellular Effect
Cell Line Type Value Description References
HeLa IC50
>100 μM
Compound: 7a
In vitro cytotoxicity against HeLa S3 cell lines, treated for 3 days then uptake of neutral red dye was measured
In vitro cytotoxicity against HeLa S3 cell lines, treated for 3 days then uptake of neutral red dye was measured
[PMID: 9622547]
HeLa IC50
100 μM
Compound: 7a
In vitro cytotoxicity against HeLa S3 cell lines, treated for 3 days then uptake of neutral red dye was measured
In vitro cytotoxicity against HeLa S3 cell lines, treated for 3 days then uptake of neutral red dye was measured
[PMID: 9622547]
MCF7 IC50
0.013 μM
Compound: 7a
In vitro cytotoxicity against MCF-7 cell lines, treated for 3 days then uptake of neutral red dye was measured
In vitro cytotoxicity against MCF-7 cell lines, treated for 3 days then uptake of neutral red dye was measured
[PMID: 9622547]
MCF7 IC50
35 nM
Compound: 5-AF
Anticancer activity against human MCF7 cells assessed as inhibition of cell growth
Anticancer activity against human MCF7 cells assessed as inhibition of cell growth
[PMID: 26994845]
Clinical Trial
Molecular Weight

320.27

Formula

C16H11F3N2O2

CAS No.
SMILES

O=C1C=C(C2=CC=C(N)C(F)=C2)OC3=C(F)C(C)=C(F)C(N)=C13

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Purity & Documentation
References
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Aminoflavone
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HY-132974
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