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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.88%
- No. CAS: 173932-75-7
- Fòrmula: C38H46O8
- Peso molecular:630.77
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Gambogenic acid
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Customer Validation & Images
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Histological Imaging/Staining
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RT-PCR
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WB
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IHC
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IF
Ver todos los productos específicos de isoformas Histone Methyltransferase
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Actividad biológica
Descripciòn
IC50 & Target
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EZH2 |
Cellular Effect
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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
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10.1039/C4MD00407H |
In Vitro
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.
In Vivo
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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No. CAS 173932-75-7
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Appearance Solid
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Peso molecular 630.77
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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
Gambogenic acid purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2022 Nov:106:154390. [Abstract]
Photomicrographs illustrated HE (× 200/400) staining and tubular injury scores treated with Gambogenic acid (3, 6 mg/kg, i.p.).
Gambogenic acid purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2022 Nov:106:154390. [Abstract]
Quantitative real-time PCR analysis of collagen I, IV and fibronectin in mouse kidneys treated with Gambogenic acid (3, 6 mg/kg, i.p.).
Gambogenic acid purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2022 Nov:106:154390. [Abstract]
Immunoblot analysis of collagen I, collagen VI, fibronectin, and quantifications by densitometry normalized with GAPDH in kidneys treated with Gambogenic acid (3, 6 mg/kg, i.p.).
Gambogenic acid purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2022 Nov:106:154390. [Abstract]
Immunochemistry staining (× 200/400) of EZH2 in kidneys treated with Gambogenic acid (3, 6 mg/kg, i.p.).
Gambogenic acid purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2022 Nov:106:154390. [Abstract]
Immunofluorescence (× 200/400) of EZH2 in kidneys treated with Gambogenic acid (3, 6 mg/kg, i.p.).
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Int Immunopharmacol
2026 May 15:177:116529. PMID: 41871492
Solvente y solubilidad
In Vitro:
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)
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: ≥ 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.
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.
Pureza y Documentación
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Ficha de datos (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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Instrucciones de manejo (2659 KB)
Referencias
[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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