Gambogenic acid
Based on 2 publication(s) in Google Scholar
Gambogenic acid is an active ingredient that can be isolated from gamboge. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH2 ubiquitination. Gambogenic acid can be used for the research of cancer.
For research use only. We do not sell to patients.
- Purity: 99.88%
- CAS No.: 173932-75-7
- Formula: C38H46O8
- Molecular Weight:630.77
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Gambogenic acid
MoreAll Histone Methyltransferase Isoforms
More
Biological Activity
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EZH2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
3.49 μM
Compound: GNA
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Cytotoxicity against human A549 cells by MTT assay
Cytotoxicity against human A549 cells by MTT assay
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10.1039/C4MD00407H |
| HepG2 | IC50 |
3.23 μM
Compound: GNA
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Cytotoxicity against human HepG2 cells by MTT assay
Cytotoxicity against human HepG2 cells by MTT assay
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10.1039/C4MD00407H |
| PANC-1 | IC50 |
4.16 μM
Compound: GNA
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Cytotoxicity against human PANC1 cells by MTT assay
Cytotoxicity against human PANC1 cells by MTT assay
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10.1039/C4MD00407H |
| U-251 | IC50 |
3.22 μM
Compound: GNA
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Cytotoxicity against human U251 cells by MTT assay
Cytotoxicity against human U251 cells by MTT assay
|
10.1039/C4MD00407H |
Gambogenic acid (0.6-2.4 µM, 1.2-3.2 µM; 24-72 h) inhibits the proliferation of SCLC cell lines (NCI-H446/NCI-H1688)[2].
Gambogenic acid (0.6-1.2 µM, 1.5-2.2 µM; 24 h) arrests cell cycle at various stages in SCLC cell lines (NCI-H446/NCI-H1688)[2].
Gambogenic acid (1.4-2 µM, 2.4-3 µM; 24 h) increases the rate of cell apoptosis in a dose-dependent manner in SCLC cell lines (NCI-H446/NCI-H1688)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SCLC cell lines (NCI-H446/NCI-H1688)
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Concentration:1.1-1.3 µM for NCI-H446 cells, 2-2.3 µM for NCI-H1688 cells
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Incubation Time:24 h
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Result:Increased the expression of cleaved caspase-3, -8 and -9, Bax, cleaved PARP and p53 proteins.
Decreased Bcl-2 expression.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCLC mouse xenograft model[1]
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Dosage:4-12 mg/kg
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Administration:i.v., every 2 days, 14 days
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Result:Increased the expression of pro-apoptotic proteins (cleaved caspase-3, -8 and -9, Bax, cleaved PARP and p53 proteins).
Decreased the anti-apoptotic proteins (Bcl-2).
Chemical Information
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CAS No. 173932-75-7
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Appearance Solid
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Molecular Weight 630.77
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Formula C38H46O8
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Color Light yellow to yellow
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SMILES
O=C(O)/C(C)=C\C[C@@]1(C2=O)OC(C)(C)[C@]([C@]31OC4=C5C(O)=C(C/C=C(C)/CC/C=C(C)\C)C(O)=C4C/C=C(C)\C)([H])C[C@@]2([H])C=C3C5=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 (2)
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Journal Impact Factor
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Most Recent
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Phytomedicine
Gambogenic acid alleviates kidney fibrosis via epigenetic inhibition of EZH2 to regulate Smad7-dependent mechanism. [Abstract]2022 Nov:106:154390. PMID: 35994849 -
Int Immunopharmacol
2026 May 15:177:116529. PMID: 41871492
Solvent & Solubility
DMSO : 100 mg/mL (158.54 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)
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: ≥ 4 mg/mL (6.34 mM); Clear solution
This protocol yields a clear solution of ≥ 4 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (40.0 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.
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.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Wang X, et al. A covalently bound inhibitor triggers EZH2 degradation through CHIP-mediated ubiquitination. EMBO J. 2017 May 2;36(9):1243-1260. [Content Brief]
[2]. Huang T, et al. Gambogenic acid inhibits the proliferation of small‑cell lung cancer cells by arresting the cell cycle and inducing apoptosis. Oncol Rep. 2019 Mar;41(3):1700-1706. [Content Brief]
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 | 1.5854 mL | 7.9268 mL | 15.8536 mL | 39.6341 mL |
| 5 mM | 0.3171 mL | 1.5854 mL | 3.1707 mL | 7.9268 mL | |
| 10 mM | 0.1585 mL | 0.7927 mL | 1.5854 mL | 3.9634 mL | |
| 15 mM | 0.1057 mL | 0.5285 mL | 1.0569 mL | 2.6423 mL | |
| 20 mM | 0.0793 mL | 0.3963 mL | 0.7927 mL | 1.9817 mL | |
| 25 mM | 0.0634 mL | 0.3171 mL | 0.6341 mL | 1.5854 mL | |
| 30 mM | 0.0528 mL | 0.2642 mL | 0.5285 mL | 1.3211 mL | |
| 40 mM | 0.0396 mL | 0.1982 mL | 0.3963 mL | 0.9909 mL | |
| 50 mM | 0.0317 mL | 0.1585 mL | 0.3171 mL | 0.7927 mL | |
| 60 mM | 0.0264 mL | 0.1321 mL | 0.2642 mL | 0.6606 mL | |
| 80 mM | 0.0198 mL | 0.0991 mL | 0.1982 mL | 0.4954 mL | |
| 100 mM | 0.0159 mL | 0.0793 mL | 0.1585 mL | 0.3963 mL |
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