1. MAPK/ERK Pathway Anti-infection
  2. p38 MAPK MEK Bacterial
  3. Gossypetin

Gossypetin 是六羟基化的类黄酮,是一种有效的 MKK3MKK6 抑制剂,可强烈减弱 MKK3/6-p38 信号传导途径,具有多种药理活性,包括抗氧化,抗菌和抗癌活性。

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Gossypetin

Gossypetin Chemical Structure

CAS No. : 489-35-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Gossypetin is a hexahydroxylated flavonoid and is a potent mitogen-activated protein kinase kinase (MKK)3 and MKK6 inhibitor with strongly attenuates the MKK3/6-p38 signaling pathway, has various pharmacological activities, including antioxidant, antibacterial and anticancer activities[1].

IC50 & Target[1]

p38 MAP kinase

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Huh-7 CC50
> 50 μM
Compound: 36
Cytotoxicity against human Huh7.5.1 cells by MTT assay
Cytotoxicity against human Huh7.5.1 cells by MTT assay
[PMID: 22445328]
Huh-7 EC50
47 μM
Compound: 36
Antiviral activity against HCV JFH-1 J399EM infected in Human Huh7.5.1 cells assessed as suppression of viral replication after 72 hrs by EGFP assay
Antiviral activity against HCV JFH-1 J399EM infected in Human Huh7.5.1 cells assessed as suppression of viral replication after 72 hrs by EGFP assay
[PMID: 22445328]
MDCK CC50
283 μM
Compound: 6
Cytotoxicity against MDCK cells after 48 hrs by MTT assay
Cytotoxicity against MDCK cells after 48 hrs by MTT assay
[PMID: 19729316]
体外研究
(In Vitro)

Gossypetin (20-60 μM; 48 hours; KYSE30, KYSE450 and KYSE510 cells) treatment significantly inhibits anchorage-dependent esophageal cancer cell growth in dose dependent manner. Gossypetin strongly suppresses anchorage-independent cell growth in esophageal cancer cells[1].
Gossypetin (60 μM; 3 hours; KYSE30 and KYSE410 cells) treatment strongly inhibits p38 activity in a dose-dependent manner and confirms that Gossypetin directly suppresses MKK3 or MKK6 activity[1].
Gossypetin (20-40 μM; 48 hours; KYSE450 and KYSE510 cells) treatment reduces S phase and induces G2 phase cell cycle arrest in a dose-dependent manner[1].
Gossypetin (20-40 μM; 72 hours; esophageal cancer cells) treatment induces intrinsic apoptosis of esophageal cancer cells[1].

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

Cell Proliferation Assay[1]

Cell Line: KYSE30, KYSE450 and KYSE510 cells
Concentration: 20 μM, 40 μM, 60 μM
Incubation Time: 48 hours
Result: Anchorage-dependent esophageal cancer cell growth was significantly inhibited.

Western Blot Analysis[1]

Cell Line: KYSE30 and KYSE410 ccells
Concentration: 60 μM
Incubation Time: 3 hours
Result: p38 activity was strongly inhibited in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: KYSE450 and KYSE510 cells
Concentration: 20 μM, 40 μM
Incubation Time: 48 hours
Result: Reduced S phase and induces G2 phase cell cycle arrest in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: Esophageal cancer cells
Concentration: 20 μM, 40 μM
Incubation Time: 72 hours
Result: Induced apoptosis of esophageal cancer cells.
体内研究
(In Vivo)

Gossypetin (100 mg/kg; oral administration; 5 times per week; for 21 days; severe combined immunodeficiency (SCID) female mice) treatment significantly decreases the volume of esophageal tumor growth and without significant loss of body weight. The expression of Ki67 is significantly decreased by Gossypetin. There are no obvious morphological differences between tissues from treated or untreated mic. The phosphorylation of p38, the direct downstream protein of MKK3/6 strongly inhibited in the Gossypetin-treated group[1].

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

Animal Model: Severe combined immunodeficiency (SCID) female mice (6-9 weeks old) injection with esophageal cancer tissue[1]
Dosage: 100 mg/kg
Administration: Oral administration; 5 times per week; for 21 days
Result: Suppressed patient-derived esophageal xenograft tumor growth in an in vivo mouse model.
分子量

318.24

Formula

C15H10O8

CAS 号
性状

固体

颜色

Light yellow to yellow

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 125 mg/mL (392.79 mM; 超声助溶; 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 3.1423 mL 15.7114 mL 31.4228 mL
5 mM 0.6285 mL 3.1423 mL 6.2846 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 (stored under nitrogen)。-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

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (6.54 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (6.54 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
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
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.82%

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 (stored under nitrogen)。-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 3.1423 mL 15.7114 mL 31.4228 mL 78.5571 mL
5 mM 0.6285 mL 3.1423 mL 6.2846 mL 15.7114 mL
10 mM 0.3142 mL 1.5711 mL 3.1423 mL 7.8557 mL
15 mM 0.2095 mL 1.0474 mL 2.0949 mL 5.2371 mL
20 mM 0.1571 mL 0.7856 mL 1.5711 mL 3.9279 mL
25 mM 0.1257 mL 0.6285 mL 1.2569 mL 3.1423 mL
30 mM 0.1047 mL 0.5237 mL 1.0474 mL 2.6186 mL
40 mM 0.0786 mL 0.3928 mL 0.7856 mL 1.9639 mL
50 mM 0.0628 mL 0.3142 mL 0.6285 mL 1.5711 mL
60 mM 0.0524 mL 0.2619 mL 0.5237 mL 1.3093 mL
80 mM 0.0393 mL 0.1964 mL 0.3928 mL 0.9820 mL
100 mM 0.0314 mL 0.1571 mL 0.3142 mL 0.7856 mL
Help & FAQs
  • 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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产品名称:
Gossypetin
目录号:
HY-119917
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