1. Apoptosis Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR
  2. Apoptosis VEGFR PI3K Akt
  3. Thymoquinone

Thymoquinone  (Synonyms: 百里醌)

目录号: HY-D0803 纯度: 99.48%
COA 产品使用指南

Thymoquinone 是从 N. sativa 中分离得到的口服活性天然产物。Thymoquinone 下调 VEGFR2-PI3K-Akt 通路。Thymoquinone 具有抗氧化、抗炎、抗癌、抗病毒、抗惊厥、抗真菌、抗病毒、抗血管生成活性和保肝作用。Thymoquinone 可用于阿尔茨海默病、癌症、心血管疾病、感染病和炎症等方面研究。

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Thymoquinone Chemical Structure

Thymoquinone Chemical Structure

CAS No. : 490-91-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥275
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500 mg ¥250
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1 g ¥400
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Other Forms of Thymoquinone:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Thymoquinone is an orally active natural product isolated from N. sativa Thymoquinone down-regulates the VEGFR2-PI3K-Akt pathway. Thymoquinone has antioxidant, anti-inflammatory, anticancer, antiviral, anticonvulsant, antifungal, antiviral, antiangiogenic activity and hepatoprotective effects. Thymoquinone can be used to study Alzheimer's disease, cancer, cardiovascular disease, infectious disease and inflammation [1][2][3][4][5].

IC50 & Target

VEGFR2

 

PI3K

 

Akt

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
518A2 IC50
28 μM
Compound: TQ
Cytotoxicity against human 518A2 cells after 72 hrs by MTT assay
Cytotoxicity against human 518A2 cells after 72 hrs by MTT assay
[PMID: 21216607]
A2780 IC50
7.9 μM
Compound: 1; TQ
Growth inhibition of human A2780 cells after 72 hrs by SRB assay
Growth inhibition of human A2780 cells after 72 hrs by SRB assay
[PMID: 29519737]
A2780cis IC50
7.8 μM
Compound: 1; TQ
Growth inhibition of human A2780cis cells after 72 hrs by SRB assay
Growth inhibition of human A2780cis cells after 72 hrs by SRB assay
[PMID: 29519737]
ADR5000 cell line EC50
0.3 μM
Compound: 3; TQ
Cytotoxicity against human CEM/ADR5000 cells overexpressing P-gp assessed as reduction in cell viability after 72 hrs by resazurin dye based assay
Cytotoxicity against human CEM/ADR5000 cells overexpressing P-gp assessed as reduction in cell viability after 72 hrs by resazurin dye based assay
[PMID: 29937978]
ADR5000 cell line EC50
0.3 μM
Compound: 6
Cytotoxicity against human CEM/ADR5000 cells over-expressing P-gp assessed as reduction in cell viability after 72 hrs by resazurin dye based assay
Cytotoxicity against human CEM/ADR5000 cells over-expressing P-gp assessed as reduction in cell viability after 72 hrs by resazurin dye based assay
[PMID: 29887512]
CCRF-CEM EC50
0.3 μM
Compound: 3; TQ
Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by resazurin dye based assay
Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by resazurin dye based assay
[PMID: 29937978]
CCRF-CEM EC50
0.3 μM
Compound: 6
Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by resazurin dye based assay
Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by resazurin dye based assay
[PMID: 29887512]
HEK-293T CC50
140 μg/mL
Compound: Thymoquinone
Cytotoxicity against human 293T cells after 72 hrs by MTT assay
Cytotoxicity against human 293T cells after 72 hrs by MTT assay
[PMID: 29100732]
HeLa IC50
2.06 μM
Compound: Thymoquinone
Antiproliferative activity against human HeLa cells assessed as growth inhibition after 72 hrs by MTT assay
Antiproliferative activity against human HeLa cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 25556101]
HFF IC50
33 μM
Compound: TQ
Cytotoxicity against human HFF after 72 hrs by MTT assay
Cytotoxicity against human HFF after 72 hrs by MTT assay
[PMID: 21216607]
HL-60 IC50
28 μM
Compound: TQ
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
[PMID: 21216607]
HT-29 IC50
47 μM
Compound: TQ
Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
[PMID: 21216607]
MCF7 IC50
6.19 μM
Compound: Thymoquinone
Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 25556101]
OVCAR-8 IC50
11.6 μM
Compound: 1; TQ
Growth inhibition of human OVCAR8 cells after 72 hrs by SRB assay
Growth inhibition of human OVCAR8 cells after 72 hrs by SRB assay
[PMID: 29519737]
U-937 IC50
101.9 μM
Compound: 5
Antiinflammatory activity in PMA-activated human U937 cells assessed as inhibition of LPS-induced TNF-alpha expression preincubated for 2 hrs followed by LPS challenge measured after 6 hrs by ELISA
Antiinflammatory activity in PMA-activated human U937 cells assessed as inhibition of LPS-induced TNF-alpha expression preincubated for 2 hrs followed by LPS challenge measured after 6 hrs by ELISA
[PMID: 24491635]
体外研究
(In Vitro)

Thymoquinone (20-100 μM, 24-72 h) 在非小细胞肺癌 SCLC 细胞系中具有抗增殖和促凋亡活性,且与顺铂 Cisplatin (CDDP) (HY-17394) 具有协同作用[3]
Thymoquinone (100 nM, 24 h) 通过 VEGFR2/PI3K/Akt 信号通路抑制 HUVECs 细胞 VEGF 的表达[5]

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

Cell Proliferation Assay[3]

Cell Line: SCLC cell line NCI-H146
Concentration: 20-100 μM
Incubation Time: 24-72 h
Result: Thymoquinone of 80 and 100 μM showed significant inhibition of cell proliferation, most pronounced at 24 hours. The effect of Thymoquinone alone on cell proliferation diminished over time.
体内研究
(In Vivo)

Thymoquinone (每日腹腔注射 5-20 mg/kg,持续 3 天) 可通过激活百草枯介导的 SOD 抑制来发挥对百草枯致小鼠肝毒性的保护作用[1]
Thymoquinone (每日口服 10 mg/kg,持续 5 天) 可通过超氧化物清除和抗脂质过氧化作用实现对阿霉素 Doxorubicin (HY-15142A) 诱导的大鼠心脏毒性的保护作用[2]
Thymoquinone (每周的周三、周五和周日皮下注射 5-20 mg/kg,持续 3 周) 单独使用可有效减小 NCI-H460 小鼠异种移植模型的肿瘤体积,且可克服 Cisplatin (CDDP) (HY-17394) 耐药,提高 CDDP 抗癌活性[3]
Thymoquinone (每日灌胃服用 10 or 20 mg/kg,持续 15 天) 具有清除 Aβ plaques 和恢复神经元活力的功能,可以提高 Aβ1-42 灌注大鼠的记忆能力[4]
Thymoquinone (单次注射 3 mg/kg, i.p.) 下调 VEGFR2-PI3K-Akt 通路,抑制哮喘小鼠体内的炎症和新血管生成[5]

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

Animal Model: Male albino mice (22-27g), Paraquat-induced hepatotoxicity in mice[1]
Dosage: 5-20 mg/kg/day for 3days
Administration: i.p.
Result: Significantly reduced the level of LPO and restored the endogenous antioxidant capacity of liver tissue.
Restored SOD activity inhibited by Paraquat.
Thymoquinone’s optimum, safe, and protective dose against Paraquat-hepatotoxicity is about 10 mg/kg, which is comparable to the antioxidant properties of Vitamin E.
Clinical Trial
分子量

164.20

Formula

C10H12O2

CAS 号
性状

固体

颜色

Light yellow to yellow

中文名称

百里醌

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 : ≥ 100 mg/mL (609.01 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 6.0901 mL 30.4507 mL 60.9013 mL
5 mM 1.2180 mL 6.0901 mL 12.1803 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: ≥ 2.5 mg/mL (15.23 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 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: ≥ 2.5 mg/mL (15.23 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 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 (protect from light)

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: 99.59%

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 6.0901 mL 30.4507 mL 60.9013 mL 152.2534 mL
5 mM 1.2180 mL 6.0901 mL 12.1803 mL 30.4507 mL
10 mM 0.6090 mL 3.0451 mL 6.0901 mL 15.2253 mL
15 mM 0.4060 mL 2.0300 mL 4.0601 mL 10.1502 mL
20 mM 0.3045 mL 1.5225 mL 3.0451 mL 7.6127 mL
25 mM 0.2436 mL 1.2180 mL 2.4361 mL 6.0901 mL
30 mM 0.2030 mL 1.0150 mL 2.0300 mL 5.0751 mL
40 mM 0.1523 mL 0.7613 mL 1.5225 mL 3.8063 mL
50 mM 0.1218 mL 0.6090 mL 1.2180 mL 3.0451 mL
60 mM 0.1015 mL 0.5075 mL 1.0150 mL 2.5376 mL
80 mM 0.0761 mL 0.3806 mL 0.7613 mL 1.9032 mL
100 mM 0.0609 mL 0.3045 mL 0.6090 mL 1.5225 mL
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产品名称:
Thymoquinone
目录号:
HY-D0803
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