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Gambogic acid

Cat. No. 3590

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Chemical Name: (2Z)-2-Methyl-4-[(1R,3aS,5S,11R,14aS)-3a,4,5,7-tetrahydro-8-hydroxy-3,3,11-trimethyl-13-(3-methyl-2-butenyl)-11-(4-methyl-3-pentenyl)-7,15-dioxo-1,5-methano-1H,3H,11H-furo[3,4-g]pyrano[3,2-b]xanthen-1-yl]-2-butenoic acid

Biological Activity

Natural product isolated from the Garcinia hanburyi tree. Induces apoptosis in several tumor cell lines including T47D cells. Activates caspases with an EC₅₀ value of 0.78 - 1.64 μM and competitively inhibits antiapoptotic Bcl-2 family proteins (IC₅₀ values are 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM for Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 respectively). Also blocks K_ir2.1 channels (EC₅₀ ≤ 100 nM).

Technical Data

M.Wt:

628.75

Formula:

C₃₈H₄₄O₈

Solubility:

Soluble to 75 mM in DMSO and to 100 mM in ethanol

Storage:

Store at -20°C

CAS No:

2752-65-0

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

References

Zhang et al (2004) Discovery, characterization and SAR of gambogic acid as a potent apoptosis inducer by a HTS assay. Bioorg.Med.Chem. 12 309. PMID: 14723951.

Qi et al (2008) Anti-invasive effect of gambogic acid in MDA-MB-231 human breast carcinoma cells. Biochem.Cell Biol. 86 386. PMID: 18923540.

Zhai et al (2008) Gambogic acid is an antagonist of antiapoptotic Bcl-2 family proteins. Mol.Cancer Ther. 7 1639. PMID: 18566235.

Zaks-Makhina et al (2009) Specific and slow inhibition of the Kir2.1 K⁺ channel by Gambogic acid. J.Biol.Chem. 284 15432. PMID: 19366693.

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