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Gambogenic acid

Chemical Structure : Gambogenic acid

CAS No.: 173932-75-7

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Gambogenic acid (GNA)

Catalog No.: PC-35432Not For Human Use, Lab Use Only.

Gambogenic acid (GNA) is a polyprenylated xanthone isolated from gamboge, shows potent antitumor activity and can effectively inhibit the survival and proliferation of cancer cells, specifically and covalently binds to Cys668 within the EZH2-SET domain.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Gambogenic acid (GNA) is a polyprenylated xanthone isolated from gamboge, shows potent antitumor activity and can effectively inhibit the survival and proliferation of cancer cells, specifically and covalently binds to Cys668 within the EZH2-SET domain.
Gambogenic acid specifically and covalently binds to Cys668 within the EZH2-SET domain, trigges EZH2 degradation (IC50=8.6 uM) through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination.
Gambogenic acid synergistically potentiates bortezomib-induced apoptosis in multiple myeloma.
Gambogenic acid also induces proteasomal degradation of CIP2A and sensitizes hepatocellular carcinoma to anticancer agents.

Physicochemical Properties

M.Wt 630.778
Formula C38H46O8
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(Z)-4-((1S,3aR,5S,12aS)-9-((E)-3,7-dimethylocta-2,6-dien-1-yl)-8,10-dihydroxy-2,2-dimethyl-11-(3-methylbut-2-en-1-yl)-4,7-dioxo-1,2,5,7-tetrahydro-1,5-methanofuro[2,3-d]xanthen-3a(4H)-yl)-2-methylbut-2-enoic acid

References

1. Xu L, et al. Cell Death Dis. 2018 Feb 15;9(3):262.

2. Liu P, et al. J Cancer. 2017 Sep 16;8(16):3278-3286.

3. Wang X, et al. EMBO J. 2017 May 2;36(9):1243-1260.

4. Li F, et al. Exp Ther Med. 2017 May;13(5):2456-2462.

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