1. Apoptosis
  2. Apoptosis IAP
  3. Polygalacin D

Polygalacin D (PGD) is a bioactive compound isolated from Platycodon grandiflorum with anticancer and anti-proliferative properties. PGD suppresses the expression of the IAP family of proteins including survivin, cIAP-1 and cIAP-2 and blocks the PI3K/Akt pathway by inhibiting the phosphorylation of GSK3β, Akt and the expression of PI3K. Polygalacin D induces apoptosis

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Polygalacin D Chemical Structure

Polygalacin D Chemical Structure

CAS No. : 66663-91-0

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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE Polygalacin D

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Description

Polygalacin D (PGD) is a bioactive compound isolated from Platycodon grandiflorum with anticancer and anti-proliferative properties. PGD suppresses the expression of the IAP family of proteins including survivin, cIAP-1 and cIAP-2 and blocks the PI3K/Akt pathway by inhibiting the phosphorylation of GSK3β, Akt and the expression of PI3K. Polygalacin D induces apoptosis[1]

IC50 & Target

IC50: IAP[1]

Cellular Effect
Cell Line Type Value Description References
HCT-15 IC50
> 10 μM
Compound: 9
Antiproliferative activity against human HCT15/CL02 cells after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human HCT15/CL02 cells after 48 hrs by sulforhodamine B assay
[PMID: 20939516]
HCT-15 IC50
8.5 μM
Compound: 9
Antiproliferative activity against human HCT15 cells after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human HCT15 cells after 48 hrs by sulforhodamine B assay
[PMID: 20939516]
MES-SA IC50
5 μM
Compound: 9
Antiproliferative activity against human MESSA cells after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human MESSA cells after 48 hrs by sulforhodamine B assay
[PMID: 20939516]
MES-SA/Dx5 IC50
7.7 μM
Compound: 9
Antiproliferative activity against human MESSA/DX5 cells after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human MESSA/DX5 cells after 48 hrs by sulforhodamine B assay
[PMID: 20939516]
In Vitro

Polygalacin D (0-40 µM; 48 hours) inhibits cell proliferation with IC50s of 26.49 µM in the A549 cells and 20.52 µM in the H460 cells[1].
Polygalacin D (0-20 µM; 48 hours) increases the proportion of early and late apoptotic cells, and nuclear condensation is observed in A549 and H460 cells[1].
Polygalacin D (0-20 µM; 48 hours) may exerts its apoptotic effects by regulating the apoptotic proteins and the IAP family of proteins in A549 and H460 cells[1].

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

Cell Proliferation Assay[1]

Cell Line: A549 and H460 cancer cell lines
Concentration: 10 µM, 20 µM, 40µM
Incubation Time: 48 hours
Result: Inhibited the proliferation of NSCLC cell lines.

Apoptosis Analysis[1]

Cell Line: A549 and H460 cancer cell lines
Concentration: 10 µM, 20 µM
Incubation Time: 48 hours
Result: Induced apoptosis of NSCLC cell lines.

Western Blot Analysis[1]

Cell Line: A549 and H460 cancer cell lines
Concentration: 10 µM, 20 µM
Incubation Time: 48 hours
Result: Decreased survivin, c-IAP-1 and c-IAP-2 expression.
Molecular Weight

1209.32

Formula

C57H92O27

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@H]([C@@H]([C@@H](O[C@@]1([H])[C@@H]([C@H]([C@H](O)CO1)O[C@@]2([H])[C@@H]([C@](CO)(O)CO2)O)O)[C@H](C)O3)O)[C@]3([H])O[C@H]([C@H]([C@@H](O)CO4)O)[C@@H]4OC([C@]56[C@](CC(C)(C)CC6)([H])C7=CC[C@@]([C@@]8([C@@]([C@](C)([C@@H](O[C@]9([H])O[C@@H]([C@@H](O)[C@H](O)[C@H]9O)CO)[C@@H](O)C8)CO)([H])CC%10)C)([H])[C@]%10(C)[C@]7(C)C[C@H]5O)=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 (82.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8269 mL 4.1346 mL 8.2691 mL
5 mM 0.1654 mL 0.8269 mL 1.6538 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)

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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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Concentration (final)

C2

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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 (2.07 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 (2.07 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: 99.95%

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 0.8269 mL 4.1346 mL 8.2691 mL 20.6728 mL
5 mM 0.1654 mL 0.8269 mL 1.6538 mL 4.1346 mL
10 mM 0.0827 mL 0.4135 mL 0.8269 mL 2.0673 mL
15 mM 0.0551 mL 0.2756 mL 0.5513 mL 1.3782 mL
20 mM 0.0413 mL 0.2067 mL 0.4135 mL 1.0336 mL
25 mM 0.0331 mL 0.1654 mL 0.3308 mL 0.8269 mL
30 mM 0.0276 mL 0.1378 mL 0.2756 mL 0.6891 mL
40 mM 0.0207 mL 0.1034 mL 0.2067 mL 0.5168 mL
50 mM 0.0165 mL 0.0827 mL 0.1654 mL 0.4135 mL
60 mM 0.0138 mL 0.0689 mL 0.1378 mL 0.3445 mL
80 mM 0.0103 mL 0.0517 mL 0.1034 mL 0.2584 mL
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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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Polygalacin D
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HY-N6064
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