Cat. No.: HY-N2420

Flavokawain A

3 Cited Publications

Customer Review

Based on 3 publication(s) in Google Scholar

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.

Purity: 99.73%
CAS No.: 3420-72-2
Formula: C₁₈H₁₈O₅
Molecular Weight:314.33

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Flavokawain A Chemical Structure

CAS No.: 3420-72-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All Histone Methyltransferase Isoforms :

All Cytochrome P450 Isoforms :

All Caspase Isoforms :

All IAP Isoforms :

All p38 MAPK Isoforms :

All PI3K Isoforms :

All NO Synthase Isoforms :

All COX Isoforms :

All JNK Isoforms :

All ERK Isoforms :

All Akt Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>20 μM Compound: 6	Inhibition of TNFalpha induced NF-kappaB activation in human A549 cells by luciferase reporter gene assay Inhibition of TNFalpha induced NF-kappaB activation in human A549 cells by luciferase reporter gene assay	[PMID: 19883086]
A549	IC₅₀	11.6 μg/mL Compound: Flavokawain A	Inhibition of TNF-alpha-induced NF-kappaB expressed in human A549 cells treated 1 hr after TNFalpha challenge measured after 6 hrs by luciferase reporter gene assay Inhibition of TNF-alpha-induced NF-kappaB expressed in human A549 cells treated 1 hr after TNFalpha challenge measured after 6 hrs by luciferase reporter gene assay	[PMID: 19716299]
DU-145	GI₅₀	30.8 μM Compound: 4	Cytotoxicity against human DU145 cells after 48 hrs Cytotoxicity against human DU145 cells after 48 hrs	[PMID: 18798609]
HCT-116	IC₅₀	10.6 μM Compound: 1c	Antiproliferative activity against human HCT116 cells after 48 hrs by SRB assay Antiproliferative activity against human HCT116 cells after 48 hrs by SRB assay	[PMID: 30041135]
HT-29	GI₅₀	45.3 μM Compound: 4	Cytotoxicity against human HT29 cells after 48 hrs Cytotoxicity against human HT29 cells after 48 hrs	[PMID: 18798609]
K562	GI₅₀	20.5 μM Compound: 4	Cytotoxicity against human K562 cells after 48 hrs Cytotoxicity against human K562 cells after 48 hrs	[PMID: 18798609]
M14	GI₅₀	22.5 μM Compound: 4	Cytotoxicity against human M14 cells after 48 hrs Cytotoxicity against human M14 cells after 48 hrs	[PMID: 18798609]
MCF7	GI₅₀	17.5 μM Compound: 4	Cytotoxicity against human MCF7 cells after 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs	[PMID: 18798609]
MDCK-II	IC₅₀	3 μM Compound: 24	Inhibition of human BCRP expressed in MDCK2 cells assessed as Hoechst 33342 accumulation preincubated for 30 mins by fluorimetry Inhibition of human BCRP expressed in MDCK2 cells assessed as Hoechst 33342 accumulation preincubated for 30 mins by fluorimetry	[PMID: 22112540]
NCI-H460	GI₅₀	24.1 μM Compound: 4	Cytotoxicity against human H460 cells after 48 hrs Cytotoxicity against human H460 cells after 48 hrs	[PMID: 18798609]
NIH3T3	GI₅₀	17.2 μM Compound: 4	Cytotoxicity against BALB mouse 3T3 cells after 48 hrs Cytotoxicity against BALB mouse 3T3 cells after 48 hrs	[PMID: 18798609]
NIH3T3	IC₅₀	11 μM Compound: 2a	Inhibition of cobalt chloride-induced HIF-1 activation expressed in mouse NIH3T3 cells after 8 hrs by luciferase reporter gene assay Inhibition of cobalt chloride-induced HIF-1 activation expressed in mouse NIH3T3 cells after 8 hrs by luciferase reporter gene assay	[PMID: 21112783]
PC-3	GI₅₀	15.2 μM Compound: 4	Cytotoxicity against human PC3 cells after 48 hrs Cytotoxicity against human PC3 cells after 48 hrs	[PMID: 18798609]
Vero	IC₅₀	>25 μM Compound: 4	Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C4 in african green monkey Vero cells after 120 hrs Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C4 in african green monkey Vero cells after 120 hrs	[PMID: 18798609]

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.

Chemical Information

CAS No. 3420-72-2
Appearance Solid
Molecular Weight 314.33
Formula C₁₈H₁₈O₅
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
- Flavonoids
- Chalcones
- Phenols
- Monophenols
Initial Source
- Plants
- other families
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

Publications (3)

All OthersWBCell Proliferation/Viability Assay

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Journal Impact Factor

Phytomedicine

The kava chalcone flavokawain B exerts inhibitory activity and synergizes with BCL-2 inhibition in malignant B-cell lymphoma. [Abstract]

2023 Nov:120:155074. PMID: 37716033

Flavokawain A purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2023 Nov:120:155074. [Abstract]

SUDHL-4 and OCI-Ly3 cells were treated with FKA (Flavokawain A; HY-N2420; 1.25-20 µg/mL) or Doxorubicin (HY-15142A; 10 µM) for 24 and 48 h. Cell viability was measured using the MTS assay. *P < 0.05, #P < 0.01, †P < 0.001, and ‡P < 0.0001 versus control at corresponding time points.SUDHL-4 (A), OCI-Ly3 (B), Raji (C), and Jeko-1 (D) cells were treated with FKA (1.25-20 µg/mL) or doxorubicin (10 µM) for 24 and 48 h. Cell viability was measured using the MTS assay. *P < 0.05, #P < 0.01, †P < 0.001, and ‡P < 0.0001 versus control at corresponding time points.

Flavokawain A purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2023 Nov:120:155074. [Abstract]

Raji and Jeko-1 cells were treated with FKA (Flavokawain A; HY-N2420; 1.25-20 µg/mL) or Doxorubicin (HY-15142A; 10 µM) for 24 and 48 h. Cell viability was measured using the MTS assay. *P < 0.05, #P < 0.01, †P < 0.001, and ‡P < 0.0001 versus control at corresponding time points.SUDHL-4 (A), OCI-Ly3 (B), Raji (C), and Jeko-1 (D) cells were treated with FKA (1.25-20 µg/mL) or doxorubicin (10 µM) for 24 and 48 h. Cell viability was measured using the MTS assay. *P < 0.05, #P < 0.01, †P < 0.001, and ‡P < 0.0001 versus control at corresponding time points.
Phytother Res

Flavokawain A Targets CXCR4-Mediated Vasculogenic Mimicry to Reverse Hepatocellular Carcinoma Resistance to Tyrosine Kinase Inhibitors. [Abstract]

2026 Apr 29. PMID: 42052746
Toxicol Appl Pharmacol

Flavokawain a induces cell cycle arrest through CDT1-dependent p27 regulation and synergizes with venetoclax in acute myeloid leukemia. [Abstract]

2025 May:498:117305. PMID: 40113097

Flavokawain A purchased from MedChemExpress. Usage Cited in: Toxicol Appl Pharmacol. 2025 May:498:117305. [Abstract]

FKA (Flavokawain A; HY-N2420) decreases the viability in AML cell lines. MV4-11, MOLM-13, THP-1, and U937 cells were treated with or without various concentrations of FKA (2.5, 5, 10, and 20 μg/mL) for 24 and 48 h, and cell viability was detected by the MTS assay. Treatment with Cytarabine (HY-13605; 7.3 μg/mL) was used as a positive control.

Flavokawain A purchased from MedChemExpress. Usage Cited in: Toxicol Appl Pharmacol. 2025 May:498:117305. [Abstract]

FKA (Flavokawain A; HY-N2420) induces cell cycle arrest in AML cells. MV4–11 cells were treated with or without FKA (5 and 10 μg/mL) for 48 h an cell cycle was examined by flow cytometry.

Flavokawain A purchased from MedChemExpress. Usage Cited in: Toxicol Appl Pharmacol. 2025 May:498:117305. [Abstract]

FKA (Flavokawain A; HY-N2420) regulates p27 through CDT1 in AML cells. MV4–11 cells with or without CDT1 overexpression were treated with FKA (10 μg/mL), the expression of CDT1 and p27 were shown.

Flavokawain A purchased from MedChemExpress. Usage Cited in: Toxicol Appl Pharmacol. 2025 May:498:117305. [Abstract]

FKA (Flavokawain A; HY-N2420) targets primary AML blasts. Samples from AML patients were treated with or without various concentrations of FKA (2.5, 5, 10, and 20 μg/mL) for 48 h, and cell viability was detected by the MTS assay. Treatment with Cytarabine (HY-13605) was used as a positive control. Data were shown as mean ± SD from at least three independent experiments.

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.1814 mL

15.9069 mL

31.8137 mL

5 mM

0.6363 mL

3.1814 mL

6.3627 mL

10 mM

0.3181 mL

1.5907 mL

3.1814 mL

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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

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Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

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

Stock Solution Working Solution

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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Xiaolin Zi, et al. Flavokawain A, a novel chalcone from kava extract, induces apoptosis in bladder cancer cells by involvement of Bax protein-dependent and mitochondria-dependent apoptotic pathway and suppresses tumor growth in mice. Cancer Res. 2005 Apr 15;65(8):3479-86. [Content Brief]

[2]. Jing S, et al. Flavokawain A alleviates the progression of mouse osteoarthritis: An in vitro and in vivo study. Front Bioeng Biotechnol. 2022 Dec 5;10:1071776. [Content Brief]

[3]. Liu S, et al. Flavokawain A is a natural inhibitor of PRMT5 in bladder cancer. J Exp Clin Cancer Res. 2022 Oct 5;41(1):293. [Content Brief]

[4]. Abu N, et al. In vitro Toxicity and in vivo Immunomodulatory Effects of Flavokawain A and Flavokawain B in Balb/C Mice. Nat Prod Commun. 2015 Jul;10(7):1199-202. [Content Brief]

[5]. Niu L, et al. Flavokawain A inhibits Cytochrome P450 in in vitro metabolic and inhibitory investigations. J Ethnopharmacol. 2016 Sep 15;191:350-359. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Flavokawain A

3 Cited Publications

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Flavokawain A

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