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

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 .

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Thymoquinone Chemical Structure

Thymoquinone Chemical Structure

CAS No. : 490-91-5

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Customer Review

Based on 7 publication(s) in Google Scholar

Thymoquinone Related Antibodies

Top Publications Citing Use of Products

View All VEGFR Isoform Specific Products:

View All Isoforms
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

View All PI3K Isoform Specific Products:

View All Isoforms
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

 

In Vitro

Thymoquinone (20-100 μM, 24-72 h) has anti-proliferation and pro-apoptotic activity in non-small cell lung cancer SCLC cell lines, and has a synergistic effect with Cisplatin (CDDP) (HY-17394) [3].
Thymoquinone (100 nM, 24 h) inhibits VEGF expression in HUVECs cells through the VEGFR2/PI3K/Akt signaling pathway[5].

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

Thymoquinone Related Antibodies

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.
In Vivo

Thymoquinone (5-20 mg/kg/day for 3 days, i.p.) can play a protective role against hepatotoxicity induced by paraquat by activating SOD inhibition mediated by paraquat[1].
Thymoquinone (10 mg/kg/day for 5 days, p.o.) can protect against Doxorubicin (HY-15142A)-induced cardiotoxicity in rats through superoxide clearance and anti-lipid peroxidation[2].
Thymoquinone (5-20 mg/kg subcutaneously (s.c.) on Monday, Wednesday and Friday for 3 weeks) alone can effectively reduce the tumor volume of NCI-H460 mouse xenograft model, overcome Cisplatin (CDDP) (HY-17394) resistance, and improve its efficacy [3].
Thymoquinone (10 or 20 mg/kg/day for 15 days, i.g.) could clear Aβ plaques and restore neuronal vitality, which could improve the memory ability of Aβ1-42 perfusion rats[4].
Thymoquinone (single 3 mg/kg, i.p.) down-regulates the VEGFR2-PI3K-Akt pathway and inhibits inflammation and new angiogenesis in asthmatic mice[5].

MedChemExpress (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
Molecular Weight

164.20

Formula

C10H12O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C(C)=CC(C(C(C)C)=C1)=O
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (609.01 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (15.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (15.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.59%

COA (251 KB) LCMS (262 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 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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Thymoquinone Related Classifications

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.

Keywords:

Thymoquinone490-91-5ApoptosisVEGFRPI3KAktVascular endothelial growth factor receptorPhosphoinositide 3-kinasePKBProtein kinase BN. sativaAlzheimer's diseasecancerapoptosisproliferationangiogenesisinflammationHUVECsparaquatsuperoxidelipid peroxidationInhibitorinhibitorinhibit

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