Gambogic acid

Biological Activity

Gambogic acid is an 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 K_ir2.1 channels (EC₅₀ ≤ 100 nM).

Technical Data

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

Background References

1. Combined therapy with EGFR TKI and gambogic acid for overcoming resistance in EGFR-T790M mutant lung cancer.
   Wang et al.
   Oncol.Lett., 2015;10:2063
2. Discovery, characterization and SAR of gambogic acid as a potent apoptosis inducer by a HTS assay.
   Zhang et al.
   Bioorg.Med.Chem., 2004;12:309
3. Gambogic acid is an antagonist of antiapoptotic Bcl-2 family proteins.
   Zhai et al.
   Mol.Cancer Ther., 2008;7:1639
4. Anti-invasive effect of gambogic acid in MDA-MB-231 human breast carcinoma cells.
   Qi et al.
   Biochem.Cell Biol., 2008;86:386
5. Specific and slow inhibition of the Kir2.1 K⁺ channel by Gambogic acid.
   Zaks-Makhina et al.
   J.Biol.Chem., 2009;284:15432

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