Apoptosis inducer in several tumor cell lines including T47D cells. Activates caspases (EC50
values are 0.78 - 1.64 μ
M) and competitively inhibits antiapoptotic Bcl-2 family proteins (IC50
values are 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μ
M 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 Kir
2.1 channels (EC50
≤ 100 nM).
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.
Discovery, characterization and SAR of gambogic acid as a potent apoptosis inducer by a HTS assay.
Zhang et al.
Gambogic acid is an antagonist of antiapoptotic Bcl-2 family proteins.
Zhai et al.
Mol.Cancer Ther., 2008;7:1639
Anti-invasive effect of gambogic acid in MDA-MB-231 human breast carcinoma cells.
Qi et al.
Biochem.Cell Biol., 2008;86:386
Specific and slow inhibition of the Kir2.1 K+ channel by Gambogic acid.
Zaks-Makhina et al.
Combined therapy with EGFR TKI and gambogic acid for overcoming resistance in EGFR-T790M mutant lung cancer.
Wang et al.
The citations listed below are publications that use Tocris products. Selected citations for Gambogic acid include:
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