Catalog Number: 3590
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
  • M.Wt:
    628.75
  • Formula:
    C38H44O8
  • Solubility:
    Soluble to 75 mM in DMSO and to 100 mM in ethanol
  • Storage:
    Store at -20°C
  • CAS No:
    2752-65-0
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.
Background References
  1. 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
  2. Gambogic acid is an antagonist of antiapoptotic Bcl-2 family proteins.
    Zhai et al.
    Mol.Cancer Ther., 2008;7:1639
  3. Anti-invasive effect of gambogic acid in MDA-MB-231 human breast carcinoma cells.
    Qi et al.
    Biochem.Cell Biol., 2008;86:386
  4. Specific and slow inhibition of the Kir2.1 K+ channel by Gambogic acid.
    Zaks-Makhina et al.
    J.Biol.Chem., 2009;284:15432
  5. 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
Citations:

The citations listed below are publications that use Tocris products. Selected citations for Gambogic acid include:

2 Citations: Showing 1 - 2
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  1. Brown Adipose Tissue Thermogenic Capacity Is Regulated by Elovl6.
    Authors: Tan Et al.
    Proc Natl Acad Sci U S A 2015;13:2039
  2. Label-free cytotoxicity screening assay by digital holographic microscopy.
    Authors: Kühn Et al.
    Assay Drug Dev Technol 2013;11:101

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