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. Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively.

Fexaramine is a small molecule farnesoid X receptor (FXR) agonist with 100-fold increased affinity relative to natural compounds.

T0901317 is a selective agonist for LXR and FXR with EC50 of 50 nM and 5 μM, respectively.

WAY-362450 is an agonist of farnesoid X receptor (FXR) with EC50 of 4 nM. WAY-362450 is used to the treatment of dyslipidemia.

Tropifexor is a potent agonist of FXR with EC50 of 0.26 nM.

Cilofexor is a FXR agonist. 

Nidufexor is a potent farnesoid X receptor (FXR) agonist for the treatment of non-alcoholic steatohepatitis (NASH) and hepatobiliary disorders.

Obeticholic acid is a selective FXR agonist with EC50 of 99 nM and it has anticholestatic activity.

Vonafexor is a farnesoid X receptor agonist.

LY2562175 is a selective and partial FXR agonist with EC50 of 193 nM.

(Z)-Guggulsterone is a broad spectrum steroid receptor ligand and an antagonist of FXR with antiseptic, antirheumatic and anti-inflammatory activity in vivo.

GW4064 is a selective, non-steroidal farnesoid X receptor (FXR) agonist (EC50 = 15 nM).