1. JAK/STAT Signaling
  2. Pim

Quercetagetin (Synonyms: 6-Hydroxyquercetin)

Cat. No.: HY-N4149
Handling Instructions

Quercetagetin (6-Hydroxyquercetin) is the major flavonoid isolated from Citrus unshiu (C. unshiu) peel. Quercetagetin is a moderately potent and selective, cell-permeable pim-1 kinase inhibitor (IC50, 0.34 μM). Anti-inflammatory and anticancer properties.

For research use only. We do not sell to patients.

Quercetagetin Chemical Structure

Quercetagetin Chemical Structure

CAS No. : 90-18-6

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Quercetagetin (6-Hydroxyquercetin) is the major flavonoid isolated from Citrus unshiu (C. unshiu) peel[3]. Quercetagetin is a moderately potent and selective, cell-permeable pim-1 kinase inhibitor (IC50, 0.34 μM)[1]. Anti-inflammatory and anticancer properties.

IC50 & Target[1]

PIM1

0.34 μM (IC50)

PIM2

3.45 μM (IC50)

RSK2

2.82 μM (IC50)

PKA

21.2 μM (IC50)

In Vitro

Quercetagetin also inhibits PIM2, PKA, and RSK2 with IC50s of 3.45, 21.2, and 2.82 µM, respectively. Quercetagetin inhibits PIM1 activity in intact RWPE2 prostate cancer cells in a dose-dependent manner (ED50, 5.5 μM). Furthermore Quercetagetin inhibits the activity of the Aurora-A kinase (IC50, ~4 μM)[1].
When pim-1-expressing cells are treated with Quercetagetin, p-BAD(S112) levels are markedly reduced in proportion to the concentration of Quercetagetin. Half-maximal inhibition occurred at 5.5 μM extracellular concentration[1].
Quercetagetin shows strong 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical-scavenging activity (IC50 7.89 μM) but much lower hydroxyl radical-scavenging activity (IC50 203.82 μM)[3].
Furthermore, Quercetagetin significantly reduces ROS in Vero cells and shows a strong protective effect against hydrogen peroxide-induced DNA damage[3].

In Vivo

Quercetagetin significantly inhibits UVB-induced skin cancer development. Topical application of 4 or 20 nmol of Quercetagetin to mouse skin reduces tumor incidence by 32.0% and 46.7%, respectively[2].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1423 mL 15.7114 mL 31.4228 mL
5 mM 0.6285 mL 3.1423 mL 6.2846 mL
10 mM 0.3142 mL 1.5711 mL 3.1423 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

RWPE2 cells are treated with Quercetagetin (0-12.5 μM) for up to 72 h. Cell number is measured by crystal violet staining and read at 570 nm[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice[2]
UVB-induced skin tumorigenesis SKH-1 hairless mouse model are treated with topical application of 4 or 20 nmol of Quercetagetin. At the end of the study, the dimensions of each tumor in each mouse are recorded. Tumor volume is calculated[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

318.24

Formula

C₁₅H₁₀O₈

CAS No.

90-18-6

SMILES

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

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Quercetagetin

Cat. No.: HY-N4149