Guggulsterone

Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt[1][2]. Guggulsterone, a farnesoid X receptor (FXR) antagonist, with IC50s of 24.06 μM and 39.05 μM for (-) - (E) -Guggulsterone (HY-N7781) and (Z) -Guggulsterone (HY-110066), respectively[3].

Product Specifications

CAS Number

[95975-55-6]

Product Name Alternative

Z/E-Guggulsterone

UNSPSC

12352211

Hazard Statement

H315, H319, H335

Target

Akt; Apoptosis; Autophagy; Caspase; FXR; JNK

Type

Natural Products

Related Pathways

Apoptosis; Autophagy; MAPK/ERK Pathway; Metabolic Enzyme/Protease; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/guggulsterone.html

Concentration

10mM

Purity

99.83

Solubility

DMSO : 20.83 mg/mL (ultrasonic)

Smiles

C[C@@]1(/C2=C/C)[C@](CC2=O)([H])[C@@]3([H])[C@]([C@@]4(C(CC3)=CC(CC4)=O)C)([H])CC1

Molecular Formula

C21H28O2

Molecular Weight

312.45

Precautions

H315, H319, H335

References & Citations

[1]Shishodia S, et al. Guggulsterone for Chemoprevention of Cancer. Curr Pharm Des. 2016;22 (3) :294-306.|[2]Che X, et al. Protective effects of guggulsterone against colitis are associated with the suppression of TREM-1 and modulation of macrophages. Am J Physiol Gastrointest Liver Physiol. 2018 Jul 1;315 (1) :G128-G139.|[3]Hsu CW, et al. Quantitative high-throughput profiling of environmental chemicals and drugs that modulate farnesoid X receptor. Sci Rep. 2014 Sep 26;4:6437.