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Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) is an orally active gallic tannin compound and an inducer of apoptosis and autophagy. Pentagalloglucose induces cell apoptosis and autophagy through the GSK3β/β-catenin pathway. Pentagalloglucose has antioxidant, anti mutagenic, anti-inflammatory, anticonvulsant, cardioprotective, anti allergic, cholesterol lowering, and anti-tumor activities.
For research use only. We do not sell to patients.
In human PC organoids, Pentagalloylglucose (PGG; 100 nM) upregulates p53, decreases RRM1 and RRM2 levels, and aggravates gemcitabine-induced replication stress.
Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) is an orally active gallic tannin compound and an inducer of apoptosis and autophagy. Pentagalloglucose induces cell apoptosis and autophagy through the GSK3β/β-catenin pathway. Pentagalloglucose has antioxidant, anti mutagenic, anti-inflammatory, anticonvulsant, cardioprotective, anti allergic, cholesterol lowering, and anti-tumor activities[1][2][3].
Cellular Effect
Cell Line
Type
Value
Description
References
A549
ED50
> 10 μg/mL
Compound: 10
Cytotoxicity against human A549 cells by tetrazolium salt-based colorimetric assay
Cytotoxicity against human A549 cells by tetrazolium salt-based colorimetric assay
Pentagalloylglucose (1 μM, 5 days) inhibits the proliferation and survival of breast cancer cells and medulloblastoma cells, with IC50 values of 3.24 μM and 1.47 μM, respectively[1].
Pentagalloylglucose (10-20 μM, 24 h) reduces AGE induced inflammation by activating Nrf2/HO-1 in mesangial cells and inhibiting the JAK2/STAT3 pathway[2].
Pentagalloylglucose (40 μM, 24 h) inhibits the growth and migration of human nasopharyngeal carcinoma cells through the GSK3β/β - catenin pathway, blocks the cell cycle, and induces apoptosis and autophagy[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pentagalloylglucose (10 mg/kg, three times a week, i.v.) enhances tumor sensitivity to PARP inhibitors and radiotherapy by disrupting the PALB2-BRCA2 interaction in MDA-MB-231 xenograft nude mice[1].
Pentagalloylglucose (10, 20 mg/kg, once every two days, i.p.) reduces tumor lung metastasis and exhibits anti-tumor activity in a CNE2 cell xenograft nude mouse model[3].
Pentagalloylglucose (5, 10 mg/kg, 7 days, i.p.) has an improving effect on the Ischemia and reperfusion-induced brain injury in rats[4].
Pentagalloylglucose (10 mg/kg, 28 days, p.o.) increases T regulatory cell populations and inhibits IgE production in ovalbumin sensitized mice through immunosuppressive activity[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
MDA-MB-231 xenograft and DAOY xenograft female BALB/c nude mice[1].
Dosage:
10 mg/kg
Administration:
Intravenous injection (i.v.); 3 days per week; 5 weeks
Room temperature in continental US; may vary elsewhere.
Storage
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
1 year
-20°C
6 months
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (106.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 6 mg/mL (6.38 mM; Need ultrasonic and warming)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
1.0631 mL
5.3153 mL
10.6306 mL
5 mM
0.2126 mL
1.0631 mL
2.1261 mL
10 mM
0.1063 mL
0.5315 mL
1.0631 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
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.
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO 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 (2.66 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 μLDMSO 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.
Protocol 3
Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (2.66 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μLCorn oil, and mix evenly.
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time. 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: PBS
Solubility: 1.43 mg/mL (1.52 mM); Clear solution; Need ultrasonic
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).
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.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
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.
*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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
H2O / DMSO
1 mM
1.0631 mL
5.3153 mL
10.6306 mL
26.5765 mL
5 mM
0.2126 mL
1.0631 mL
2.1261 mL
5.3153 mL
DMSO
10 mM
0.1063 mL
0.5315 mL
1.0631 mL
2.6577 mL
15 mM
0.0709 mL
0.3544 mL
0.7087 mL
1.7718 mL
20 mM
0.0532 mL
0.2658 mL
0.5315 mL
1.3288 mL
25 mM
0.0425 mL
0.2126 mL
0.4252 mL
1.0631 mL
30 mM
0.0354 mL
0.1772 mL
0.3544 mL
0.8859 mL
40 mM
0.0266 mL
0.1329 mL
0.2658 mL
0.6644 mL
50 mM
0.0213 mL
0.1063 mL
0.2126 mL
0.5315 mL
60 mM
0.0177 mL
0.0886 mL
0.1772 mL
0.4429 mL
80 mM
0.0133 mL
0.0664 mL
0.1329 mL
0.3322 mL
100 mM
0.0106 mL
0.0532 mL
0.1063 mL
0.2658 mL
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
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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