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Kd = 8.34 μM

G3335 is a PPARγ antagonist.

The peroxisome proliferator-activated receptor gamma (PPARgamma) is a key therapeutic drug target for several conditions, such as inflammation, diabetes, hypertension, dyslipidemia, and cancer.

In vitro: Biacore 3000 study based on the surface plasmon resonance technique found that G3335 exhibited a highly specific binding affinity against PPARgamma and was able to block rosiglitazone, a potent PPARgamma agonist, in the stimulation of the interaction between the PPARgamma ligand-binding domain (LBD) and RXRalpha-LBD. Moreover, the yeast two-hybrid assays indicated that G3335 had strong antagonistic activity in perturbing rosiglitazone in the promotion of the PPARgamma-LBD-CBP interaction. In addition, G3335 could competitively bind to PPARgamma against 0.1 microM rosiglitazone to repress reporter-gene expression [1].

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