Home Angiogenesis FGFR inhibitor - EZH1/2 inhibitor Gambogenic acid For research use only.

Gambogenic acid

Gambogenic Acid, identified from Gamboge, is an inhibitor of the FGFR signaling pathway in 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.

Gambogenic acid Chemical Structure

Gambogenic acid Chemical Structure

CAS No. 173932-75-7

Purity & Quality Control

Gambogenic acid Related Products

Signaling Pathway

FGFR Signaling Pathways

FGFR Signaling Pathway

Biological Activity

Description Gambogenic Acid, identified from Gamboge, is an inhibitor of the FGFR signaling pathway in 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
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]
Cell Research 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.
In Vivo
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.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06199531 Recruiting
NGLY1 Deficiency
Grace Science LLC
 February 13 2024 Phase 1|Phase 2
NCT05179174 Unknown status
Uveal Melanoma
University of Catania
 April 20 2021 --
NCT03838913 Unknown status
Bile Duct Neoplasms|Intraductal Papillary Mucinous Neoplasm
Fujian Provincial Hospital|Fujian Medical University Union Hospital|First Affiliated Hospital of Fujian Medical University
 February 15 2019 --
NCT03671525 Completed
Schizophrenia|Schizo Affective Disorder
Johns Hopkins University
 October 5 2018 Early Phase 1
NCT02849145 Completed
Uveal Melanoma
Institut Curie
 September 2014 Not Applicable

Chemical Information & Solubility

Molecular Weight 630.77 Formula

C38H46O8
CAS No. 173932-75-7 SDF --
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (158.53 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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