Gambogenic acid

Catalog No.S9031 Batch:S903104

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Technical Data

Formula

C38H46O8
Molecular Weight 630.77 CAS No. 173932-75-7
Solubility (25°C)* In vitro DMSO 100 mg/mL (158.53 mM)
 
 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Gambogenic Acid, identified from Gamboge, is an inhibitor of the FGFR signaling pathway in erlotinib-resistant non-small-cell lung cancer (NSCLC) and exhibits anti-tumor effects. Gambogenic acid acts is also an effective inhibitor of EZH2 that specifically and covalently binds to Cys668 within the EZH2-SET domain, and triggers EZH2 ubiquitination.
Targets
FGFR [1] EZH2 [2]
In vitro

Gambogenic acid as a novel agent that specifically and covalently bound to Cys668 within the EZH2‐SET domain, triggers EZH2 degradation through COOH terminus of Hsp70‐interacting protein (CHIP)‐mediated ubiquitination. Gambogenic acid significantly suppresses H3K27Me3 and effectively reactivated polycomb repressor complex 2 (PRC2)‐silenced tumor suppressor genes. Gambogenic acid significantly suppresses tumor growth in an EZH2‐dependent manner.[1]
In vivo

In xenograft mouse model, gambogenic acid derivative GNA002 significantly decreases the volumes of Cal‐27‐derived tumors, and reduces H3K27Me3 levels in tumor tissues.

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    Head and neck cancer cell lines, humen breast cancer cell lines, mouse embryonic fibroblasts (MEFs)

  • Concentrations

    0.2 -10 µM

  • Incubation Time

    24 h, 48 h

  • Method

    Cancer cells are treated with 2 μM GNA or GNA002 for 24 h. The cells are then harvested and re‐suspended with 500 μl of binding buffer. The cell suspension (100 μl) is incubated with various cell dye. The stained cells are analyzed with fluorescent‐activated cell sorting using the flow cytometry machine.

Selleck's Gambogenic acid has been cited by 3 publications

Gambogenic acid induces cell death in human osteosarcoma through altering iron metabolism, disturbing the redox balance, and activating the P53 signaling pathway [ Chem Biol Interact, 2023, 382:110602] PubMed: 37302459
A high-content AlphaScreen™ identifies E6-specific small molecule inhibitors as potential therapeutics for HPV+ head and neck squamous cell carcinomas [ Oncotarget, 2021, 12(6):549-561] PubMed: 33796223
Targeting USP9x/SOX2 axis contributes to the anti-osteosarcoma effect of neogambogic acid. [ Cancer Lett, 2020, 469:277-286] PubMed: 31605775

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.