Gambogic amide

Gambogic acid amide
A Selective Agonist of TrkA Receptors
    Cat #: G-235
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 627.78
    Purity: >95%
    Effective concentration 0.1-1 µM.
    Structure
    Chemical name (2Z)-4-[(1S,2S,8R,17S,19R)-12-Hydroxy-8,21,21-trimethyl-5-(3-methyl-2-buten-1-yl)-8-(4-methyl-3-penten-1-yl)-14,18-dioxo-3,7,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.06,11]docosa-4(13),5,9,
 11,15-pentaen-19-yl]-2-methyl-2-butenamide.
    Molecular formula C38H45NO7.
    CAS No.: 286935-60-2.
    Activity Gambogic amide, an NGF-mimetic small molecule, is a TrkA receptor agonist, shown to selectively bind, activate and upregulate the expression of TrkA receptors at nanomolar concentrations (Kd = 75 nM). Gambogic amide shows antiapoptotic activity (EC50 = 5 nM), neuroprotective and anti-cancer effects in vitro and in vivo1-3.
    References - Activity
    1. Jang, S.W. et al. (2007) Proc. Natl. Acad. Sci. U.S.A. 104, 16329.
    2. Chan, C.B. et al. (2009) Oncogene 28, 3825.
    3. Shen, J. and Yu, Q. (2015) Pharmacol. Rep. 67, 217.
    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. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.
    Our bioassay
    Alomone Labs Gambogic amide inhibits the proliferation of K562 human chronic myelogenous leukemia cells.
    Dose-response curve of Gambogic amide (#G-235) inhibition of K562 cell viability. Cell viability was determined by the XTT method and normalized to control. IC50 was calculated at 204 nM.
    References - Scientific Background
    1. Jang, S.W. et al. (2007) Proc. Natl. Acad. Sci. U.S.A. 104, 16329.
    2. Chan, C.B. et al. (2009) Oncogene 28, 3825.
    3. Shen, J. and Yu, Q. (2015) Pharmacol. Rep. 67, 217.
    Scientific background

    Gambogic amide, is a small molecule that mimics nerve growth factor (NGF) and is a selective agonist of TrkA receptor that strongly induces its tyrosine phosphorylation and downstream signaling activation.

    Gambogic amide interacts with the cytoplasmic juxtamembrane domain of TrkA receptor and triggers its dimerization. It selectively binds, activates and upregulates the expression of TrkA receptors at nanomolar concentrations but not TrkB or TrkC.

    Gambogic acid is a major active ingredient of gamboge, a resin exuded from the Garcinia hanburryi tree in southeast Asia. Gambogic amide also possesses neurotrophic activity in various neural injury animal models and prevents glutamate-induced neuronal cell death1,2.

    Gambogic amide shows antiapoptotic activity and demonstrates EC50 value of 5 nM3.

    Target TrkA receptors
    Last update: 22/11/2018

    Gambogic amide (#G-235) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use