1. Apoptosis Epigenetics Metabolic Enzyme/Protease MAPK/ERK Pathway PI3K/Akt/mTOR Immunology/Inflammation Stem Cell/Wnt
  2. Apoptosis Histone Methyltransferase Cytochrome P450 Caspase Survivin IAP p38 MAPK PI3K NO Synthase COX JNK ERK Akt
  3. Flavokawain A

Flavokawain A is a chalcone compound and an orally active inhibitor of PRMT5 and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer.

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

Flavokawain A Chemical Structure

Flavokawain A Chemical Structure

CAS No. : 3420-72-2

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Based on 2 publication(s) in Google Scholar

Other Forms of Flavokawain A:

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Flavokawain A is a chalcone compound and an orally active inhibitor of PRMT5 and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer[1][2][3][4][5].

In Vitro

Flavokawain A (0.05-25 μg/mL; 4-48 h) can inhibit the proliferation of multiple bladder cancer cells, cause the loss of mitochondrial membrane potential and the release of cytochrome c in T24 cells. The mechanism involves the activation of Bax and the inhibition of Bcl-x/L[1].
Flavokawain A (5-30 μg/mL; 4-24 h) induces apoptosis in T24 cells through the caspase pathway and by inhibiting XIAP and survivin[1].
Flavokawain A (20-40 μM; 24 h) can inhibit IL-1β-induced inflammation, the expression of senescence-related genes, apoptosis, and the phosphorylation of genes related to the MAPK and PI3K pathways in mouse chondrocytes[2].

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

Cell Viability Assay[1]

Cell Line: RT4, T24, and EJ cells
Concentration: RT4 cells (0.05, 0.5, 5, 12.5 and 25 μg/mL)
T24 and EJ cells (0.309, 0.625, 1.25, 2.5, 5, 12.5 and 25 μg/mL)
Incubation Time: 48 h
Result: Inhibited cell proliferation in RT4, T24, and EJ bladder cancer cell lines

Western Blot Analysis[1]

Cell Line: T24 cells
Concentration: 12.5 μg/mL
Incubation Time: 4, 8, 16 and 24 h
Result: Inhibited the level Bcl-x/L.
Increased the level Bax.

Western Blot Analysis[1]

Cell Line: T24 cells
Concentration: 5, 10, 20 and 30μg/mL
Incubation Time: 4, 8, 16 and 24 h
Result: Inhibited the levels of XIAP and survivin.

Western Blot Analysis[2]

Cell Line: IL-1β treated mouse chondrocyte cells
Concentration: 20 and 40 μM
Incubation Time: 24 h
Result: Inhibited the levels of iNOS and COX2.
Inhibited the levels of P16 and P21.
Inhibited the level of Bax and increased the level of Bcl2.
Inhibited the phosphorylation levels of JNK, P38, ERK, PI3K, AKT and mTOR.
In Vivo

Flavokawain A (30 mg/kg; peritumoral injection; once every 3 days; 24 days) exhibits anti-tumor activity in a mouse model of bladder cancer[3].
Flavokawain A (50 mg/kg; oral administration; 28 days) shows no toxicity and has certain immunomodulatory effects in Balb/c mice[4].

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

Animal Model: Male BALB/c mice aged 8 weeks old[4]
Dosage: 50 mg/kg/day
Administration: Oral administration (p.o.); 28 days
Result: Did not cause the death of mice during the 28-day treatment period, and there were no significant changes in the body weight of the mice.
Did not significantly alter several serum biochemical parameters.
Stimulated the proliferation of splenocytes, promoted the secretion of cytokines IL-2 and TNF-α, and increased the population of T cell subsets.
Decreased the levels of TNF-α and NO, and slightly reduced the level of IL-2.
Animal Model: Four-week-old Balb/c nude mice treated UMUC3 cells[3]
Dosage: 30 mg/kg
Administration: Peritumoral injection; once every 3 days; 24 days
Result: Significantly inhibited tumor size.
Decreased the arginine methylation level of histone and the expression of bladder-cancer-associated regulon genes.
Molecular Weight

314.33

Formula

C18H18O5

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C(OC)C=C(OC)C=C1O)/C=C/C2=CC=C(OC)C=C2

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (318.14 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 3.1814 mL 15.9069 mL 31.8137 mL
5 mM 0.6363 mL 3.1814 mL 6.3627 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.93%

References

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1814 mL 15.9069 mL 31.8137 mL 79.5343 mL
5 mM 0.6363 mL 3.1814 mL 6.3627 mL 15.9069 mL
10 mM 0.3181 mL 1.5907 mL 3.1814 mL 7.9534 mL
15 mM 0.2121 mL 1.0605 mL 2.1209 mL 5.3023 mL
20 mM 0.1591 mL 0.7953 mL 1.5907 mL 3.9767 mL
25 mM 0.1273 mL 0.6363 mL 1.2725 mL 3.1814 mL
30 mM 0.1060 mL 0.5302 mL 1.0605 mL 2.6511 mL
40 mM 0.0795 mL 0.3977 mL 0.7953 mL 1.9884 mL
50 mM 0.0636 mL 0.3181 mL 0.6363 mL 1.5907 mL
60 mM 0.0530 mL 0.2651 mL 0.5302 mL 1.3256 mL
80 mM 0.0398 mL 0.1988 mL 0.3977 mL 0.9942 mL
100 mM 0.0318 mL 0.1591 mL 0.3181 mL 0.7953 mL
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Flavokawain A
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