Chemical Name: (Z)-Pregna-4,17(20)-diene-3,16-dione
Biological ActivityZ-Guggulsterone is a 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).
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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
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
Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study.
Meyer et al.
Citation for Z-Guggulsterone
The citations listed below are publications that use Tocris products. Selected citations for Z-Guggulsterone include:
1 Citation: Showing 1 - 1
C-terminal truncated hepatitis B virus X protein promotes hepatocellular carcinogenesis through induction of cancer and stem cell-like properties.
Authors: Ng Et al.
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