1. Apoptosis Epigenetics Cell Cycle/DNA Damage NF-κB PI3K/Akt/mTOR MAPK/ERK Pathway Metabolic Enzyme/Protease Immunology/Inflammation
  2. Apoptosis Caspase PARP Bcl-2 Family NF-κB PI3K Akt p38 MAPK MMP Reactive Oxygen Species (ROS)
  3. Flavokawain B

Flavokawain B  (Synonyms: Flavokavain B)

目录号: HY-N2132 纯度: 99.99%
COA 产品使用指南 技术支持

Flavokawain B (Flavokavain B) 是一种口服活性的查耳酮。Flavokawain B 可激活 caspase-9、-3 和 -8,切割 PARP。Flavokawain B 可下调 Bcl-2,同时增加 Bax 水平。Flavokawain B 可抑制 NF-κBPI3K/AktMAPK 信号通路。Flavokawain B 具有凋亡 (Apoptotic) 作用。Flavokawain B 可抑制 MMP-9 和促进 ROS 生成。Flavokawain B 可抑制多种肿瘤和炎症。

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Flavokawain B

Flavokawain B Chemical Structure

CAS No. : 1775-97-9

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Other Forms of Flavokawain B:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 20 μM
Compound: 7
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
19.7 μM
Compound: 21
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay
[PMID: 31673309]
A549 IC50
8 μg/mL
Compound: Flavokawain B
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]
B16-F10 IC50
7.7 μM
Compound: 1a
Antimelanogenic activity in mouse B16F10 cells assessed as inhibition of melanin production after 4 days
Antimelanogenic activity in mouse B16F10 cells assessed as inhibition of melanin production after 4 days
[PMID: 25597012]
Caco-2 IC50
9.9 μM
Compound: 2
Cytotoxicity against human Caco2 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay
Cytotoxicity against human Caco2 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay
[PMID: 28214231]
Fibroblast IC50
> 20 μM
Compound: 2
Cytotoxicity against human fibroblasts assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay
Cytotoxicity against human fibroblasts assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay
[PMID: 28214231]
HaCaT IC50
13.6 μM
Compound: 2
Cytotoxicity against human HaCaT cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay
Cytotoxicity against human HaCaT cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay
[PMID: 28214231]
HCT-116 IC50
> 20 μM
Compound: 21
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay
[PMID: 31673309]
HCT-116 IC50
7.5 μM
Compound: 2
Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay
Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay
[PMID: 28214231]
HeLa IC50
> 20 μM
Compound: 21
Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay
[PMID: 31673309]
Huh-7 IC50
15.9 μM
Compound: 2
Cytotoxicity against human HuH7 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay
Cytotoxicity against human HuH7 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay
[PMID: 28214231]
MCF7 IC50
15.5 μM
Compound: 2
Cytotoxicity against human MCF7 assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay
Cytotoxicity against human MCF7 assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay
[PMID: 28214231]
MDA-MB-231 IC50
16.3 μM
Compound: 2
Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay
Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay
[PMID: 28214231]
MIA PaCa-2 IC50
18.2 μM
Compound: 21
Cytotoxicity against human MIAPaCa2 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay
Cytotoxicity against human MIAPaCa2 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay
[PMID: 31673309]
NCI-H727 IC50
11.3 μM
Compound: 2
Cytotoxicity against human NCI-H727 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay
Cytotoxicity against human NCI-H727 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay
[PMID: 28214231]
NIH3T3 IC50
3.3 μM
Compound: 2b
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 IC50
9.1 μM
Compound: 2
Cytotoxicity against human PC3 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay
Cytotoxicity against human PC3 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay
[PMID: 28214231]
RAW264.7 IC50
26.5 μM
Compound: FK B
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 32208222]
RAW264.7 IC50
4.2 μM
Compound: FK B
Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells measured after 24 hrs by Griess reagent based assay
Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells measured after 24 hrs by Griess reagent based assay
[PMID: 32208222]
REH IC50
> 20 μM
Compound: 21
Cytotoxicity against human REH cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay
Cytotoxicity against human REH cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay
[PMID: 31673309]
RL IC50
8.2 μM
Compound: 2
Cytotoxicity against human RL assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay
Cytotoxicity against human RL assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay
[PMID: 28214231]
U-937 IC50
> 20 μM
Compound: 21
Cytotoxicity against human U937 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay
Cytotoxicity against human U937 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay
[PMID: 31673309]
体外研究
(In Vitro)

Flavokawain B (1-5 µg/mL,18-24 h) 抑制人脑内皮细胞 (HUVEC) 迁移和管形成[1]
Flavokawain B (1.25-20 µg/mL,18 h) 通过下调 PI3K/Akt 轴诱导多种 B 细胞淋巴瘤细胞系增殖抑制和凋亡[3]
Flavokawain B (5-40 µM,1 h) 具有抗炎活性,可抑制 LPS 诱导的 RAW 264.7 细胞中 NO 和 PGE2 的产生[4]
Flavokawain B (17.6-70.4 μM,24 h) 导致 KB 细胞凋亡,表现为细胞活力丧失、形态学改变变化、基因组 DNA 碎片化和亚 G1 期积累[5]
Flavokawain B (2.5-7.5 µg/mL,24 h) 诱导滑膜肉瘤细胞系凋亡[6]
Flavokawain B (2.5-7.5 µg/mL,24 h) 通过 G2/M 细胞周期停滞和凋亡抑制人骨肉瘤细胞 (143B 和 saos-2) 的生长[7]
Flavokawain B (1.25-10 μg/mL,24 h) 通过细胞内 ROS 生成和 Akt/p38 MAPK 信号下调诱导人口腔癌 HSC-3 细胞凋亡通路[8]
Flavokawain B (2.5-5 μg/mL,24 h) 表现出强大的凋亡作用,并诱导子宫平滑肌肉瘤细胞系 SK-LMS-1 和 ECC-1 的 G2/M 停滞[9]

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

Cell Viability Assay[3]

Cell Line: SUDHL-4, OCI-Ly3, Raji, and Jeko-1
Concentration: 1.25, 2.5, 5, 10, 20 µg/mL
Incubation Time: 24  h, 48 h
Result: Showed dose- and time-dependent inhibition of cell proliferation (SUDHL-4).
Mildly affected cell (SUDHL-4) viability at a concentration of 1.25 μg/mL (24 h).

Apoptosis Analysis[3]

Cell Line: SUDHL-4, OCI-Ly3, Raji, and Jeko-1
Concentration: 2.5, 5, and 10 µg/mL
Incubation Time: 12  h, 24 h
Result: Increased the number of cleaved PARP and caspase-3 fragments.
Reduced the expression of BCL-XL (an anti-apoptotic member of the BCL-2 family).
Induced the breakdown of MMP.
体内研究
(In Vivo)

Flavokawain B (1-2.5 µg/mL,24 h) 抑制斑马鱼模型中的血管生成[1]
Flavokawain B (50-200 mg/kg,腹腔注射) 在 LPS 诱导的小鼠中表现出抗炎活性[4]
Flavokawain B (0.35-0.75 mg/kg,腹腔注射,每 2 天一次,27 天) 显着抑制裸鼠体内人类 KB 细胞衍生肿瘤异种移植瘤的生长[5]
Flavokawain B (20-40 mg/kg,口服,7 天) 通过靶向 TLR2 抑制结肠炎小鼠中的 NF-κB 炎症信号通路激活[10]
Flavokawain B (25 mg/kg,口服,每天一次,持续一周) 通过调节 IKK/NF-κB 和 MAPK 信号通路,在小鼠中诱导 GSH 敏感的氧化应激[11]
Flavokawain B (10-20 mg/kg,例如,连续 3 天) 通过靶向髓系分化因子 2,缓解小鼠 LPS 诱导的急性肺损伤[12]
Flavokawain B (25 mg/kg,腹腔注射,每周两次,持续 2 周) 与 Cisplatin (HY-17394)/Gemcitabine (HY-17026) 联合使用,可显著抑制异种移植小鼠 (SNU-478 细胞) 模型中的肿瘤生长[13]

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

Animal Model: Nude mice injected human KB cell[5]
Dosage: 0.35, 0.75 mg/kg
Administration: Intraperitoneal injection (i.p.), every 2 days, 27 days
Result: Showed no loss of body weight.
Showed time-dependent growth inhibition of tumor.
Showed tumor cell inactivity or regression.
Showed augmentation of apoptotic DNA fragmentation.
分子量

284.31

Formula

C17H16O4

CAS 号
性状

固体

颜色

Light yellow to yellow

中文名称

黄卡瓦胡椒素B

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

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

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 5 mg/mL (17.59 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.5173 mL 17.5864 mL 35.1729 mL
5 mM 0.7035 mL 3.5173 mL 7.0346 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.99%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.5173 mL 17.5864 mL 35.1729 mL 87.9322 mL
5 mM 0.7035 mL 3.5173 mL 7.0346 mL 17.5864 mL
10 mM 0.3517 mL 1.7586 mL 3.5173 mL 8.7932 mL
15 mM 0.2345 mL 1.1724 mL 2.3449 mL 5.8621 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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