2. Epigenetics
  3. Histone Methyltransferase
  4. Gambogenic acid

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.

Gambogenic acid Chemical Structure

Gambogenic acid Chemical Structure

CAS No. : 173932-75-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 167 In-stock
Solution
10 mM * 1 mL in DMSO USD 167 In-stock
Solid
1 mg USD 33 In-stock
5 mg USD 120 In-stock
10 mg USD 200 In-stock
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100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Gambogenic acid Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Gambogenic acid

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

IC50 & Target

EZH2

 

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.

Gambogenic acid Related Antibodies

Western Blot Analysis[2]

Cell Line: SCLC cell lines (NCI-H446/NCI-H1688)
Concentration: 1.1-1.3 µM for NCI-H446 cells, 2-2.3 µM for NCI-H1688 cells
Incubation Time: 24 h
Result: Increased the expression of cleaved caspase-3, -8 and -9, Bax, cleaved PARP and p53 proteins.
Decreased Bcl-2 expression.
In Vivo

Gambogenic acid (4-12 mg/kg, i.v., every 2 days, 14 days) inhibits tumor growth in SCLC mouse xenograft model[2].

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

Animal Model: SCLC mouse xenograft model[1]
Dosage: 4-12 mg/kg
Administration: i.v., every 2 days, 14 days
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).
Molecular Weight

630.77

Formula

C38H46O8
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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
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 (158.54 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 1.5854 mL 7.9268 mL 15.8536 mL
5 mM 0.3171 mL 1.5854 mL 3.1707 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)

Mass
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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

×
Volume (start)

V1

=
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: ≥ 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:

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: 99.94%

COA (254 KB) RP-HPLC (205 KB)

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 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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Gambogenic acid Related Classifications

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.

Keywords:

Gambogenic acid173932-75-7Histone MethyltransferaseEZH2cancerSCLCNCI-H446NCI-H1688Inhibitorinhibitorinhibit

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