Polygalacin D
Based on 3 publication(s) in Google Scholar
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
For research use only. We do not sell to patients.
- Purity : 99.68%
- CAS No.: 66663-91-0
- Formula: C57H92O27
- Molecular Weight:1209.32
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications Citing Use of MedChemExpress (MCE) Polygalacin D
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Biological Activity
Description
IC50 & Target
IC50: IAP[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-15 | IC50 |
>10 μM
Compound: 9
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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
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[PMID: 20939516] |
| HCT-15 | IC50 |
8.5 μM
Compound: 9
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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
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[PMID: 20939516] |
| HSC-T6 | IC50 |
1.04 μM
Compound: 151
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Antiproliferative activity against rat HSC-T6 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against rat HSC-T6 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 29353722] |
| MES-SA | IC50 |
5 μM
Compound: 9
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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
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[PMID: 20939516] |
| MES-SA/Dx5 | IC50 |
7.7 μM
Compound: 9
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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
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[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. Further protocols information, click here.
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Cell Line:A549 and H460 cancer cell lines
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Concentration:10 µM, 20 µM, 40µM
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Incubation Time:48 hours
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Result:Inhibited the proliferation of NSCLC cell lines.
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Cell Line:A549 and H460 cancer cell lines
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Concentration:10 µM, 20 µM
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Incubation Time:48 hours
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Result:Induced apoptosis of NSCLC cell lines.
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Cell Line:A549 and H460 cancer cell lines
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Concentration:10 µM, 20 µM
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Incubation Time:48 hours
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Result:Decreased survivin, c-IAP-1 and c-IAP-2 expression.
Chemical Information
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CAS No. 66663-91-0
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Appearance Solid
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Molecular Weight 1209.32
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Formula C57H92O27
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Color White to off-white
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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
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (3)
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Journal Impact Factor
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Most Recent
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Free Radic Biol Med
Polygalacin D suppresses esophageal squamous cell carcinoma growth and metastasis through regulating miR-142-5p/Nrf2 axis. [Abstract]2021 Feb 20:164:58-75. PMID: 33307164 -
Cancer Gene Ther
2025 Oct 2. PMID: 41039015 -
Biol Pharm Bull
Polygalacin D Prevents Breast Cancer Progression through Proteasome-Mediated Degradation of HDAC1 and HDAC2. [Abstract]2025;48(12):1897-1905. PMID: 41371635
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocols
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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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 | 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 |