Gambogenic acid

Name: Gambogenic acid
Brand: MedChemExpress
SKU: HY-N5024
Rating: 4.5 (1 reviews)

Cat. No.: HY-N5024 Purity: 99.94%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

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	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 167	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 200	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE Gambogenic acid

•Phytomedicine. 11 August 2022, 154390.

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•Related Screening Libraries:

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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

IC₅₀ & Target

EZH2

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	3.49 μM Compound: GNA	Cytotoxicity against human A549 cells by MTT assay Cytotoxicity against human A549 cells by MTT assay	10.1039/C4MD00407H
HepG2	IC₅₀	3.23 μM Compound: GNA	Cytotoxicity against human HepG2 cells by MTT assay Cytotoxicity against human HepG2 cells by MTT assay	10.1039/C4MD00407H
PANC-1	IC₅₀	4.16 μM Compound: GNA	Cytotoxicity against human PANC1 cells by MTT assay Cytotoxicity against human PANC1 cells by MTT assay	10.1039/C4MD00407H
U-251	IC₅₀	3.22 μM Compound: GNA	Cytotoxicity against human U251 cells by MTT assay Cytotoxicity against human U251 cells by MTT assay	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.

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.

173932-75-7

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

Ketones, Aldehydes, Acids

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
10 mM	0.1585 mL	0.7927 mL	1.5854 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

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)

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%

Select Batch:

Data Sheet (278 KB) SDS (251 KB)

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

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

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

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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Gambogenic acid

Customer Review

Gambogenic acid Related Antibodies

1 Publications Citing Use of MCE Gambogenic acid

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Gambogenic acid Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Gambogenic acid Related Classifications

Keywords:

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