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).
|Storage||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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 628.75. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.59 mL||7.95 mL||15.9 mL|
|5 mM||0.32 mL||1.59 mL||3.18 mL|
|10 mM||0.16 mL||0.8 mL||1.59 mL|
|50 mM||0.03 mL||0.16 mL||0.32 mL|
References are publications that support the biological activity of the product.
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
Zhai et al (2008) Gambogic acid is an antagonist of antiapoptotic Bcl-2 family proteins. Mol.Cancer Ther. 7 1639 PMID: 18566235
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
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
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
If you know of a relevant reference for Gambogic acid, please let us know.
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3 Citations for Gambogic acid
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
Mathieu et al (2014) Identification of Small Inhibitory Molecules Targeting the Bfl-1 Anti-Apoptotic Protein That Alleviates Resistance to ABT-737. J Biomol Screen 19 1035 PMID: 24809353
Do you know of a great paper that uses Gambogic acid from Tocris? Please let us know.
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Literature in this Area
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Programmed Cell Death Poster
There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.