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

Thymoquinone 是從 N. sativa 中分離得到的口服活性天然產(chǎn)物。Thymoquinone 下調(diào) VEGFR2-PI3K-Akt 通路。Thymoquinone 具有抗氧化、抗炎、抗癌、抗病毒、抗驚厥、抗真菌、抗病毒、抗血管生成活性和保肝作用。Thymoquinone 可用于阿爾茨海默病、癌癥、心血管疾病、感染病和炎癥等方面研究。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Thymoquinone Chemical Structure

Thymoquinone Chemical Structure

CAS No. : 490-91-5

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥275
In-stock
500 mg ￥250
In-stock
1 g ￥400
In-stock
5 g   詢價(jià)  
10 g   詢價(jià)  

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Customer Review

Other Forms of Thymoquinone:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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

 

細(xì)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]
體外研究
(In Vitro)

Thymoquinone (20-100 μM, 24-72 h) 在非小細(xì)胞肺癌 SCLC 細(xì)胞系中具有抗增殖和促凋亡活性，且與順鉑 Cisplatin (CDDP) (HY-17394) 具有協(xié)同作用[3]。
Thymoquinone (100 nM, 24 h) 通過 VEGFR2/PI3K/Akt 信號(hào)通路抑制 HUVECs 細(xì)胞 VEGF 的表達(dá)[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.
體內(nèi)研究
(In Vivo)

Thymoquinone (每日腹腔注射 5-20 mg/kg，持續(xù) 3 天) 可通過激活百草枯介導(dǎo)的 SOD 抑制來發(fā)揮對(duì)百草枯致小鼠肝毒性的保護(hù)作用[1]。
Thymoquinone (每日口服 10 mg/kg，持續(xù) 5 天) 可通過超氧化物清除和抗脂質(zhì)過氧化作用實(shí)現(xiàn)對(duì)阿霉素 Doxorubicin (HY-15142A) 誘導(dǎo)的大鼠心臟毒性的保護(hù)作用[2]。
Thymoquinone (每周的周三、周五和周日皮下注射 5-20 mg/kg，持續(xù) 3 周) 單獨(dú)使用可有效減小 NCI-H460 小鼠異種移植模型的腫瘤體積，且可克服 Cisplatin (CDDP) (HY-17394) 耐藥，提高 CDDP 抗癌活性[3]。
Thymoquinone (每日灌胃服用 10 or 20 mg/kg，持續(xù) 15 天) 具有清除 Aβ plaques 和恢復(fù)神經(jīng)元活力的功能，可以提高 Aβ1-42 灌注大鼠的記憶能力[4]。
Thymoquinone (單次注射 3 mg/kg, i.p.) 下調(diào) VEGFR2-PI3K-Akt 通路，抑制哮喘小鼠體內(nèi)的炎癥和新血管生成[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 號(hào)
性狀

固體

顏色

Light yellow to yellow

中文名稱

百里醌
結(jié)構(gòu)分類
初始來源
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式

4°C, protect from light

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

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : ≥ 100 mg/mL (609.01 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (15.23 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (15.23 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。

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

您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.59%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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
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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產(chǎn)品名稱：
Thymoquinone
目錄號(hào)：
HY-D0803
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