Fisetin [528-48-3]

Referentie HY-N0182-100mg

Formaat : 100mg

Merk : MedChemExpress

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Description

Fisetin is a natural flavonol found in many fruits and vegetables with various benefits, such as antioxidant, anticancer, neuroprotection effects.

IC50 & Target

Sirtuin, PPAR, TNF-alpha[1][2]

Cellular Effect
Cell Line Type Value Description References
BV-2 IC50
13.5 μM
Compound: Fisetin
Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production pretreated for 1 hr followed by LPS addition and measured after 24 hrs by Griess assay
Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production pretreated for 1 hr followed by LPS addition and measured after 24 hrs by Griess assay
[PMID: 28923363]
BV-2 IC50
73.02 μM
Compound: 13
Antineuroinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced NO production after 24 hrs in presence of LPS by Griess reaction based assay
Antineuroinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced NO production after 24 hrs in presence of LPS by Griess reaction based assay
[PMID: 28911817]
CWR22R IC50
25.9 μM
Compound: 22
Antiproliferative activity against human 22Rv1 cells incubated up to 144 hrs by Coulter particle count and size analyzer
Antiproliferative activity against human 22Rv1 cells incubated up to 144 hrs by Coulter particle count and size analyzer
[PMID: 22789812]
DU-145 IC50
> 50 μM
Compound: Fisetin
Antiproliferative activity against human DU145 cells after 3 days by WST-1 assay
Antiproliferative activity against human DU145 cells after 3 days by WST-1 assay
[PMID: 30165345]
DU-145 IC50
> 50 μM
Compound: 2
Antiproliferative activity against human DU145 cells after 3 days by WST-1 assay
Antiproliferative activity against human DU145 cells after 3 days by WST-1 assay
[PMID: 28760528]
H9 EC50
122 μM
Compound: 14
Antiviral activity against HIV1 3B infected in human H9 cells assessed as inhibition of viral replication after 3 days by p24 antigen capture assay
Antiviral activity against HIV1 3B infected in human H9 cells assessed as inhibition of viral replication after 3 days by p24 antigen capture assay
[PMID: 8158164]
H9 IC50
157 μM
Compound: 14
Cytotoxicity against human H9 cells after 3 days
Cytotoxicity against human H9 cells after 3 days
[PMID: 8158164]
HepG2 IC50
> 400 μM
Compound: 34
Cytotoxicity against human HepG2 cells by MTT assay
Cytotoxicity against human HepG2 cells by MTT assay
[PMID: 21726077]
HT-22 EC50
2.8 μM
Compound: fisetin
Neuroprotective effect against iodoacetic acid-induced ischemia in mouse HT22 cells treated simultaneously with iodoacetic acid for 2 hrs followed by incubation in fresh medium containing drug alone for 20 hrs measured after 4 hrs by MTT assay
Neuroprotective effect against iodoacetic acid-induced ischemia in mouse HT22 cells treated simultaneously with iodoacetic acid for 2 hrs followed by incubation in fresh medium containing drug alone for 20 hrs measured after 4 hrs by MTT assay
[PMID: 19537799]
HT-22 EC50
3 μM
Compound: Fisetin
Neuroprotective activity in mouse HT22 cells assessed as reduction in IAA-induced ischemia after 24 hrs by MTT assay
Neuroprotective activity in mouse HT22 cells assessed as reduction in IAA-induced ischemia after 24 hrs by MTT assay
[PMID: 22192055]
Huh-7 CC50
> 50 μM
Compound: 39
Cytotoxicity against human Huh7.5.1 cells by MTT assay
Cytotoxicity against human Huh7.5.1 cells by MTT assay
[PMID: 22445328]
L6 IC50
> 30 μg/mL
Compound: 20
Antitrypanosomal activity against trypomastigote forms of Trypanosoma cruzi Tulahuen C2C4 infected in rat L6 cells after 96 hrs by photometric method
Antitrypanosomal activity against trypomastigote forms of Trypanosoma cruzi Tulahuen C2C4 infected in rat L6 cells after 96 hrs by photometric method
10.1039/C5MD00481K
L6 IC50
38.5 μg/mL
Compound: 20
Cytotoxicity against rat L6 cells after 72 hrs by alamar blue staining based fluorescence analysis
Cytotoxicity against rat L6 cells after 72 hrs by alamar blue staining based fluorescence analysis
10.1039/C5MD00481K
LNCaP IC50
34.1 μM
Compound: Fisetin
Antiproliferative activity against human LNCAP cells after 3 days by WST-1 assay
Antiproliferative activity against human LNCAP cells after 3 days by WST-1 assay
[PMID: 30165345]
LNCaP IC50
34.1 μM
Compound: 2
Antiproliferative activity against human LNCAP cells after 3 days by WST-1 assay
Antiproliferative activity against human LNCAP cells after 3 days by WST-1 assay
[PMID: 28760528]
MCF-10A IC50
2.44 μM
Compound: Fisetin
Cytotoxicity against human MCF10A cells assessed as decrease in cell viability after 3 days by WST-1 assay
Cytotoxicity against human MCF10A cells assessed as decrease in cell viability after 3 days by WST-1 assay
[PMID: 30165345]
Monocyte IC50
3.7 μM
Compound: fisetin
Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs
Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs
[PMID: 8882428]
PC-3 IC50
> 50 μM
Compound: Fisetin
Antiproliferative activity against human PC3 cells after 3 days by WST-1 assay
Antiproliferative activity against human PC3 cells after 3 days by WST-1 assay
[PMID: 30165345]
PC-3 IC50
> 50 μM
Compound: 2
Antiproliferative activity against human PC3 cells after 3 days by WST-1 assay
Antiproliferative activity against human PC3 cells after 3 days by WST-1 assay
[PMID: 28760528]
PWR-1E IC50
5.39 μM
Compound: Fisetin
Cytotoxicity against human PWR-1E cells assessed as decrease in cell viability after 3 days by WST-1 assay
Cytotoxicity against human PWR-1E cells assessed as decrease in cell viability after 3 days by WST-1 assay
[PMID: 30165345]
RD EC50
84.48 μM
Compound: Fisetin
Antiviral activity against EV71 infected in human RD cells assessed as reduction in viral plaque formation after 1 hr by crystal violet staining method
Antiviral activity against EV71 infected in human RD cells assessed as reduction in viral plaque formation after 1 hr by crystal violet staining method
[PMID: 27776325]
THP-1 IC50
30 μM
Compound: Fisetin
Cytotoxicity against human THP1 cells after 24 hrs by MTS assay
Cytotoxicity against human THP1 cells after 24 hrs by MTS assay
[PMID: 19879672]
Vero IC50
55 μg/mL
Compound: fisetin
Antiviral activity against dengue virus 2 infected in african green monkey Vero cells assessed as reduction in viral replication dosed after adsorption with 200 FFU of virus for 1 hour by foci forming unit reduction assay
Antiviral activity against dengue virus 2 infected in african green monkey Vero cells assessed as reduction in viral replication dosed after adsorption with 200 FFU of virus for 1 hour by foci forming unit reduction assay
[PMID: 25564380]
In Vitro

Fisetin inhibits lipid accumulation and suppresses the expression of PPARγ in 3T3-L1 cells. Fisetin suppresses early stages of preadipocyte differentiation, and induces expression of Sirt1. Fisetin facilitates Sirt1-mediated deacetylation of PPARγ and FoxO1, and enhances the association of Sirt1 with the PPARγ promoter, leading to suppression of PPARγ transcriptional activity, thereby repressing adipogenesis[1]. Fisetin binds to tubulin and stabilizes microtubules with binding characteristics far superior than paclitaxel. Fisetin treatment of human prostate cancer cells results in robust up-regulation of microtubule associated proteins (MAP)-2 and -4. Fisetin significantly inhibits PCa cell proliferation, migration, and invasion. Nudc, a protein associated with microtubule motor dynein/dynactin complex that regulates microtubule dynamics, is inhibited with Fisetin treatment[2].

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

In Vivo

Fisetin treatment to UVB exposed mice results in decreased hyperplasia and reduces infiltration of inflammatory cells. Fisetin treatment also reduces inflammatory mediators such as COX-2, PGE2 as well as its receptors (EP1- EP4), and MPO activity. Furthermore, Fisetin reduces the level of inflammatory cytokines TNFα, IL-1β and IL-6 in UVB exposed skin. Fisetin treatment also reduces cell proliferation markers as well as DNA damage as evidenced by increased expression of p53 and p21 proteins[3].

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

Essai clinique
Masse moléculaire

286.24

Formule

C15H10O6

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Structure Classification
Initial Source
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvant et solubilité
In Vitro: 

DMSO : 25 mg/mL (87.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4936 mL 17.4679 mL 34.9357 mL
5 mM 0.6987 mL 3.4936 mL 6.9871 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (7.27 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (7.27 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  45% PEG300    5% Tween-80    50% Saline

    Solubility: 10 mg/mL (34.94 mM); Suspended solution; Need ultrasonic

  • Protocol 2

    Add each solvent one by one:  0.5% CMC/saline water

    Solubility: 25 mg/mL (87.34 mM); Suspended solution; Need ultrasonic

Pureté et documentation
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