Gambogic acid

1,5-Methano-1H,3H,11H-furo(3,4-g)pyrano(3,2-b)xanthene-1-crotonic acid, B"-Guttiferrin, Beta-Guttiferrin, Beta-Guttilactone, Cambogic acid, Guttatic acid, Guttic acid
Kir2.1 Channel Blocker, Apoptosis Inducer, Caspase Activator and Bcl-2 Inhibitor
    Cat #: G-250
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 628.75
    Purity: >98%
    Effective concentration 0.1-1 µM.
    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.
    Molecular formula C38H44O8.
    CAS No.: 2752-65-0.
    Activity Gambogic acid is a cell-permeable apoptosis inducer in multiple cancer cell lines, acting via activation of caspases (EC50 of 0.78-1.64 µM), competitive inhibition of Bcl-2 family proteins (IC50 of 0.66-2.02), altering the expression of Bcl-2 and Bax genes, and binding CD71 transferrin receptors to prevent their internalization (IC50 = 4.1 µM). Gambogic acid is also a slow blocker of Kir2.1 channels (IC50 ≤ 100 nM)1-3.
    References - Activity
    1. Zhai, D. et al. (2008) Mol. Cancer Ther. 7, 1639.
    2. Zaks-Makhina, E. et al. (2009) J. Biol. Chem. 284, 15432.
    3. Shi, X. et al. (2013) Clin. Cancer Res. 20, 151.
    Storage before reconstitution Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Reconstitution Soluble up to 100 mM in DMSO. Centrifuge all products before handling (10000 x g 5 min).
    Storage after reconstitution -20°C up to four months. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.
    Our bioassay
    Alomone Labs Gambogic acid inhibits the proliferation of K562 human chronic myelogenous leukemia cells.
    Dose-response curve of Gambogic acid (#G-250) inhibition of K562 cell viability. Cell viability was determined by the XTT method and normalized to control. IC50 was calculated at 284 nM.
    References - Scientific Background
    1. Zhai, D. et al. (2008) Mol. Cancer Ther. 7, 1639.
    2. Zaks-Makhina, E. et al. (2009) J. Biol. Chem. 284, 15432.
    Scientific background

    Gambogic acid is a compound originally derived from the gamboges resin of the tree, Garcinia hanburyi. Gambogic acid has been shown to pose cytotoxic activity against tumor cells in culture through a mechanism involving apoptosis1.

    Gambogic acid was found to act as a slow blocker of Kir2.1 with relatively potent IC50 values of 100 nM and lower2.

    Gambogic acid is better known for its agonistic action on caspases, proteases involved in apoptosis and as a Bcl-2 inhibitor. Bcl-2-family proteins are regulators of apoptosis1.

    Target Caspases, Bcl-2, Bax, CD71, Kir2.1
    Last update: 22/11/2018

    Gambogic acid (#G-250) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use