| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| Other Sizes |
| Targets |
Sirtuin, PPAR, TNF-alpha[1][2]
Fisetin acts on multiple targets including Sirtuin 1 (Sirt1), PPARgamma, TNF-alpha, NF-kappaB, PI3K/Akt, and tubulin. It increases Sirt1 expression and facilitates Sirt1-mediated deacetylation of PPARgamma and FoxO1, thereby suppressing PPARgamma transcriptional activity and adipogenesis. Fisetin also binds to beta-tubulin and stabilizes microtubules. |
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| ln Vitro |
In 3T3-L1 cells, fisetin quarterhydrate suppresses PPARγ expression and lipid buildup. Fisetin quarterhydrate stimulates Sirt1 expression and suppresses preadipocyte development in its early phases. Fisetin quarterhydrate increases the binding of Sirt1 to the PPARγ promoter, which inhibits PPARγ transcriptional activity and adipogenesis by promoting Sirt1-mediated deacetylation of PPARγ and FoxO1 [1]. Fisetin quarterhydrate has considerably better binding characteristics than paclitaxel and stabilizes microtubules via binding tubulin. Microtubule-associated proteins (MAP)-2 and -4 were significantly upregulated in human prostate cancer cells treated with fisetin quarterhydrate. The proliferation, migration, and invasion of PCa cells were markedly reduced by fisetin quarterhydrate. Treatment with fisetin quarterhydrate inhibits Nudc, a protein linked to the microtubule motor dynamin/dynein complex, which controls microtubule dynamics [2].
In vitro, fisetin inhibits lipid accumulation and suppresses PPARgamma expression in 3T3-L1 cells, suppresses early stages of preadipocyte differentiation, and induces Sirt1 expression. It binds to tubulin with characteristics superior to paclitaxel, inhibits prostate cancer cell proliferation, migration, and invasion. Fisetin also reduces inflammatory mediators such as COX-2 and PGE2. |
| ln Vivo |
Treatment with fisetin quarterhydrate decreased inflammatory cell infiltration and proliferation in mice exposed to UVB radiation. In addition, treatment with fisetin quarterhydrate lowers the levels of inflammatory mediators such COX-2, PGE2 and its receptors (EP1–EP4), and MPO activity. Fisetin quarterhydrate also lowers UVB-exposed skin's levels of the inflammatory cytokines TNFα, IL-1β, and IL-6. Treatment with fisetin quarterhydrate also decreases DNA damage and indicators of cell growth, as shown by increased expression of the proteins p53 and p21 [3].
In vivo, fisetin administered topically or orally reduces UVB-induced skin hyperplasia, inflammatory cell infiltration, and levels of TNFalpha, IL-1beta, and IL-6. It decreases cell proliferation markers and DNA damage (increased p53/p21). In aged models, fisetin exhibits senolytic activity by selectively eliminating senescent cells and improving healthspan. |
| Enzyme Assay |
In a cell-free binding assay, incubate purified beta-tubulin with increasing concentrations of fisetin (1-100 uM) for 30-60 minutes at 25degC. Use fluorescence spectroscopy or surface plasmon resonance to measure binding affinity. For microtubule stabilization assays, incubate purified microtubules with fisetin and monitor polymerization by turbidity at 350 nm.
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| Cell Assay |
Culture 3T3-L1 preadipocytes in DMEM with 10% FBS. At confluence, induce differentiation with MDI (isobutylmethylxanthine, dexamethasone, insulin) in the presence or absence of fisetin (5-50 uM) for 48-72 hours. Assess lipid accumulation by Oil Red O staining. Measure PPARgamma and Sirt1 expression by Western blot. For cancer cells, treat PCa cells with fisetin (10-40 uM) for 24-72 hours and assess viability via MTT assay.
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| Animal Protocol |
Apply fisetin topically (dissolved in acetone, 1-5 umol) to UVB-exposed SKH-1 hairless mice 30 minutes before UVB irradiation. For oral administration, administer fisetin at 10-100 mg/kg by gavage for 1-4 weeks. Harvest skin or adipose tissues for histological analysis, immunohistochemistry, and cytokine quantification by ELISA. Assess DNA damage via p53/p21 staining.
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| ADME/Pharmacokinetics |
Fisetin is rapidly absorbed following oral administration but exhibits low bioavailability due to extensive first-pass metabolism. It is metabolized primarily by glucuronidation and sulfation. Peak plasma concentrations are reached within 0.5-2 hours. Tissue distribution is wide, with accumulation in the liver, kidney, and adipose tissue. Half-life ranges from 3-10 hours depending on species.
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| Toxicity/Toxicokinetics |
Fisetin has a favorable safety profile with low toxicity. In animal studies, no significant adverse effects are observed at doses up to 500 mg/kg orally. High concentrations may cause mild gastrointestinal disturbances. Ethyl maltol can enhance copper-mediated cytotoxicity and induce apoptosis in lung epithelial cells. Fisetin has been evaluated in multiple clinical trials for safety in healthy volunteers and older medical patients.
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| References |
[1]. Kim SC, et al. Fisetin induces Sirt1 expression while inhibiting early adipogenesis in 3T3-L1 cells. Biochem Biophys Res Commun. 2015 Nov 27;467(4):638-44.
[2]. Mukhtar E, et al. Dietary flavonoid fisetin binds to β-tubulin and disrupts microtubule dynamics in prostate cancer cells. Cancer Lett. 2015 Oct 28;367(2):173-83. |
| Additional Infomation |
The quarterhydrate form contains one water molecule per four fisetin molecules, enhancing stability. Fisetin is marketed as a dietary supplement for its antioxidant and senolytic properties. It has been investigated in clinical trials for healthy aging, metabolic syndrome, and cancer prevention. Its ability to modulate aging-related pathways makes it a promising candidate for therapeutic development.
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| Molecular Formula |
C15H10O6.1/4H2O
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| Molecular Weight |
290.75
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| Related CAS # |
Fisetin;528-48-3
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| Appearance |
Typically exists as solid at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4394 mL | 17.1969 mL | 34.3938 mL | |
| 5 mM | 0.6879 mL | 3.4394 mL | 6.8788 mL | |
| 10 mM | 0.3439 mL | 1.7197 mL | 3.4394 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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