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[1][2].

Product Specifications

CAS Number

[173932-75-7]

UNSPSC

12352005

Target

Histone Methyltransferase

Type

Natural Products

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/gambogenic-acid.html

Purity

99.91

Solubility

DMSO : 100 mg/mL (ultrasonic)

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

Molecular Formula

C38H46O8

Molecular Weight

630.77

References & Citations

[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.|[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.