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Z-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).
Z-Guggulsterone is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|DMSO||6.25||20 with gentle warming|
|ethanol||3.12||10 with gentle warming|
The following data is based on the product molecular weight 312.45. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.2 mM||16 mL||80.01 mL||160.03 mL|
|1 mM||3.2 mL||16 mL||32.01 mL|
|2 mM||1.6 mL||8 mL||16 mL|
|10 mM||0.32 mL||1.6 mL||3.2 mL|
References are publications that support the biological activity of the product.
Singh et al (2007) Guggulsterone-induced apoptosis in human prostate cancer cells is caused by reactive oxygen intermediate-dependent activation of c-Jun NH2-terminal kinase. Cancer Res. 67 7439 PMID: 17671214
Xiao and Singh (2008) z-Guggulsterone, a constituent of Ayurvedic medicinal plant Commiphora mukul, inhibits angiogenesis in vitro and in vivo. Mol.Cancer Ther. 7 171 PMID: 18202020
Meyer et al (2005) Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. J.Med.Chem. 48 6955 PMID: 16250653
If you know of a relevant reference for Z-Guggulsterone, please let us know.
Keywords: Z-Guggulsterone, Z-Guggulsterone supplier, Broad, spectrum, steroid, receptor, ligands, Nuclear, Receptors, progesterone, mineralocorticoid, glucocorticoid, Other, 3570, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Z-Guggulsterone include:
Ng et al (2016) C-terminal truncated hepatitis B virus X protein promotes hepatocellular carcinogenesis through induction of cancer and stem cell-like properties. Oncotarget 7 24005 PMID: 27006468
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