Gambogic acid

Cat. No. 3590

Gambogic acid C38H44O8 [2752-65-0]

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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

Apoptosis inducer in several tumor cell lines including T47D cells. Activates caspases (EC50 values are 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). Reverses gefitinib-resistance in mice bearing tumors with EGFR-T790M mutation. Also blocks Kir2.1 channels (EC50 ≤ 100 nM).

Technical Data

Soluble to 75 mM in DMSO and to 100 mM in ethanol
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Wang et al (2015) Combined therapy with EGFR TKI and gambogic acid for overcoming resistance in EGFR-T790M mutant lung cancer. Oncol.Lett. 10 2063. PMID: 26622796.

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.

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.

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.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for Gambogic acid include:

Tan et al (2015) Brown Adipose Tissue Thermogenic Capacity Is Regulated by Elovl6. Proc Natl Acad Sci U S A 13 2039. PMID: 26628376.

Kühn et al (2013) Label-free cytotoxicity screening assay by digital holographic microscopy. Assay Drug Dev Technol 11 101. PMID: 23062077.

Do you know of a great paper that uses Gambogic acid from Tocris? If so please let us know.

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