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 ActivityGambogic 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 Kir2.1 channels (EC50 ≤ 100 nM).
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Combined therapy with EGFR TKI and gambogic acid for overcoming resistance in EGFR-T790M mutant lung cancer.
Wang et al.
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.
Citations for Gambogic acid
The citations listed below are publications that use Tocris products. Selected citations for Gambogic acid include:
3 Citations: Showing 1 - 3
Brown Adipose Tissue Thermogenic Capacity Is Regulated by Elovl6.
Authors: Tan Et al.
Proc Natl Acad Sci U S A 2015;13:2039
Identification of Small Inhibitory Molecules Targeting the Bfl-1 Anti-Apoptotic Protein That Alleviates Resistance to ABT-737.
Authors: Mathieu Et al.
J Biomol Screen 2014;19:1035
Label-free cytotoxicity screening assay by digital holographic microscopy.
Authors: Kühn Et al.
Assay Drug Dev Technol 2013;11:101
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