Catalog Number: 3570
Chemical Name: (Z)-Pregna-4,17(20)-diene-3,16-dione
Biological Activity
Broad spectrum steroid receptor ligand; mineralocorticoid, progesterone and glucocorticoid receptor antagonist (Ki values are 37, 224 and 252 nM respectively) and weak androgen receptor agonist (Ki = 315 nM). Induces apoptosis in prostate cancer cells and inhibits angiogenesis via suppression of the VEGF-VEGFR2-Akt signaling pathway. Exhibits antilipidemic activity via antagonism of the farnesoid X receptor (FXR) and displays antiseptic, antirheumatic and anti-inflammatory activity in vivo. More active isomer of guggulsterone (Cat. No. 2013).
Technical Data
  • M.Wt:
    312.45
  • Formula:
    C21H28O2
  • Solubility:
    Soluble to 20 mM in DMSO with gentle warming and to 10 mM in ethanol with gentle warming
  • Purity:
    >98%
  • Storage:
    Store at RT
  • CAS No:
    39025-23-5
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. Guggulsterone-induced apoptosis in human prostate cancer cells is caused by reactive oxygen intermediate-dependent activation of c-Jun NH2-terminal kinase.
    Singh et al.
    Cancer Res., 2007;67:7439
  2. z-Guggulsterone, a constituent of Ayurvedic medicinal plant Commiphora mukul, inhibits angiogenesis in vitro and in vivo.
    Xiao and Singh
    Mol.Cancer Ther., 2008;7:171
  3. Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study.
    Meyer et al.
    J.Med.Chem., 2005;48:6955
Tocris Small Molecules
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Guggulsterone

2013  
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