Flavokawain B  (Synonyms: Flavokavain B)

Flavokawain B (Flavokavain B) is an orally active chalcone. Flavokawain B results in activation of caspase-9, -3 and -8, cleavage of PARP. Flavokawain B down-regulates Bcl-2 with concomitant increase in Bax level. Flavokawain B inhibits NF-κB, PI3K/Akt and MAPK signaling pathway. Flavokawain B exhibits Apoptotic effects. Flavokawain B inhibits MMP-9 and promotes ROS generation. Flavokawain B inhibits multiple tumors and inflammation^{[1][2][3][4][5][6][7][8][9][10][11][12][13]}.

Flavokawain B (1-5 µg/mL, 18-24 h) inhibits human brain endothelial cell (HUVEC) migration and tube formation^[1].
Flavokawain B (1.25-20 µg/mL, 18 h) induces proliferation inhibition and apoptosis in multiple B-cell lymphoma cell lines through downregulating the PI3K/Akt axis^[3].
Flavokawain B (5-40 µM, 1 h) shows anti-inflammatory activities, with inhibiting production of NO and PGE2 in LPS-induced RAW 264.7 cells^[4].
Flavokawain B (17.6-70.4 μM, 24 h) results in apoptosis of KB cells, evidenced by loss of cell viability, profound morphological changes, genomic DNA fragmentation and sub-G1 phase accumulation^[5].
Flavokawain B (2.5-7.5 µg/mL, 24 h) induces apoptosis in synovial sarcoma cell lines^[6].
Flavokawain B (2.5-7.5 µg/mL, 24 h) inhibits growth of human osteosarcoma cells (143B and saos-2) through G2/M cell cycle arrest and apoptosis^[7].
Flavokawain B (1.25-10 μg/mL, 24 h) induces apoptosis in human oral carcinoma HSC-3 cells through the intracellular ROS generation and downregulation of the Akt/p38 MAPK signaling pathway^[8].
Flavokawain B (2.5-5 μg/mL, 24 h) exhibits robust apoptotic effects and induces G2/M arrest of a uterine leiomyosarcoma cell line SK-LMS-1 and ECC-1^[9].

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

Flavokawain B (1-2.5 µg/mL, 24 h) suppresses angiogenesis in a zebrafish model^[1].
Flavokawain B (50-200 mg/kg, i.p.) shows anti-inflammatory activities in LPS-induced mice^[4].
Flavokawain B (0.35-0.75 mg/kg, i.p., every 2 days, 27 days) significantly inhibits in vivo growth of human KB cell-derived tumor xenografts in nude mice^[5].
Flavokawain B (20-40 mg/kg, p.o., 7 days) inhibits NF-κB inflammatory signaling pathway activation in colitis mice by targeting TLR2^[10].
Flavokawain B (25 mg/kg, p.o., daily for a week) induces GSH-sensitive oxidative stress in mice through modulation of IKK/NF-κB and MAPK signaling pathways^[11].
Flavokawain B (10-20 mg/kg, i.g., 3 consecutive days) alleviates LPS-induced acute lung injury in mice via targeting myeloid differentiation factor 2^[12].
Flavokawain B (25 mg/kg, i.p., twice-a-week for 2 weeks) in combination with Cisplatin (HY-17394)/Gemcitabine (HY-17026) significantly inhibits tumor growth in a xenograft mouse (SNU-478 cells) model^[13].

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

284.31

C₁₇H₁₆O₄

1775-97-9

Solid

Light yellow to yellow

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

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

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

* 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.

• [1]. Rossette MC, et al. The In Vitro and In Vivo Antiangiogenic Effects of Flavokawain B. Phytother Res. 2017 Oct;31(10):1607-1613.  [Content Brief]

  [2]. Li X, et al. Flavokawain B targets protein neddylation for enhancing the anti-prostate cancer effect of Bortezomib via Skp2 degradation. Cell Commun Signal. 2019 Mar 18;17(1):25.  [Content Brief]

  [3]. Zhao M, et al. The kava chalcone flavokawain B exerts inhibitory activity and synergizes with BCL-2 inhibition in malignant B-cell lymphoma. Phytomedicine. 2023 Nov;120:155074.  [Content Brief]

  [4]. Lin CT, et al. Anti-inflammatory activity of Flavokawain B from Alpinia pricei Hayata. J Agric Food Chem. 2009 Jul 22;57(14):6060-5.  [Content Brief]

  [5]. Lin E, et al. Flavokawain B inhibits growth of human squamous carcinoma cells: Involvement of apoptosis and cell cycle dysregulation in vitro and in vivo. J Nutr Biochem. 2012 Apr;23(4):368-78.  [Content Brief]

  [6]. Sakai T, et al. Flavokawain B, a kava chalcone, induces apoptosis in synovial sarcoma cell lines. J Orthop Res. 2012 Jul;30(7):1045-50.  [Content Brief]

  [7]. Ji T, et al. Flavokawain B, a kava chalcone, inhibits growth of human osteosarcoma cells through G2/M cell cycle arrest and apoptosis. Mol Cancer. 2013 Jun 10;12:55.  [Content Brief]

  [8]. Hseu YC, et al. The chalcone flavokawain B induces G2/M cell-cycle arrest and apoptosis in human oral carcinoma HSC-3 cells through the intracellular ROS generation and downregulation of the Akt/p38 MAPK signaling pathway. J Agric Food Chem. 2012 Mar 7;60(9):2385-97.  [Content Brief]

  [9]. Eskander RN, et al. Flavokawain B, a novel, naturally occurring chalcone, exhibits robust apoptotic effects and induces G2/M arrest of a uterine leiomyosarcoma cell line. J Obstet Gynaecol Res. 2012 Aug;38(8):1086-94.  [Content Brief]

  [10]. Chen Y, et al. Flavokawain B inhibits NF-κB inflammatory signaling pathway activation in inflammatory bowel disease by targeting TLR2. Toxicol Appl Pharmacol. 2024 May;486:116922.  [Content Brief]

  [11]. Zhou P, et al. Flavokawain B, the hepatotoxic constituent from kava root, induces GSH-sensitive oxidative stress through modulation of IKK/NF-kappaB and MAPK signaling pathways. FASEB J. 2010 Dec;24(12):4722-32.  [Content Brief]

  [12]. Luo W, et al. Flavokawain B alleviates LPS-induced acute lung injury via targeting myeloid differentiation factor 2. Acta Pharmacol Sin. 2022 Jul;43(7):1758-1768.  [Content Brief]

  [13]. Son JH, et al. Flavokawain B Inhibits Growth of Cholangiocarcinoma Cells by Suppressing the Akt Pathway. In Vivo. 2023 May-Jun;37(3):1077-1084.  [Content Brief]