Gambogenic acid

Overview

Gambogenic acid is a polyprenylated xanthone isolated from Garcinia hanburyi (gamboge resin). It is an inhibitor of the FGFR signaling pathway and a covalent inhibitor of EZH2 that specifically binds to Cys668 within the EZH2-SET domain, triggering EZH2 ubiquitination and degradation. Gambogenic acid exhibits potent antitumor effects across a wide range of cancers including lung, liver, colorectal, breast, gastric, bladder, and prostate cancers. It prevents cancer cell proliferation by inducing apoptosis, ferroptosis, and necroptosis, and controlling the cell cycle and autophagy. The compound also hinders tumor cell invasion and metastasis by downregulating metastasis-related proteins, and increases the sensitivity of cancer cells to chemotherapy. Additionally, gambogenic acid shows anti-fibrotic activity by epigenetically inhibiting EZH2 to regulate Smad7-dependent TGF-β/Smad3 signaling, with potential applications in kidney fibrosis treatment.

Application

Products > Drug Discovery > Inhibitor | Products > Drug Discovery > Inhibitor | Cancer | EZH2

Product Information

• Catalog No.: B2703-334164
• CAS No.: 173932-75-7
• Molecular Formula: C38H46O8
• Molecular Weight: 630.77
• Purity: 98%
• Storage: Store at 2-8 °C, protect from light
• Solubility: Soluble in DMSO

Source

Original product source