GW 6471

GW 6471 is a potent antagonist of PPARα with IC50 of 0.24 μM.

GW6471 completely inhibits GW409544-induced activation of PPARα with IC50 of 0.24 μM. GW6471 at concentration ranging from 0.001-10 μM disrupts the interactions between PPAR and coactivator motifs derived from SRC-1 or CBP, but promotes the binding of the co-repressor motifs from SMRT or N-CoR. GW6471 adopts a U-shaped configuration and wraps around C276 of helix 3, destroys the integrity of the charge clamp but leaves sufficient space to accommodate the additional helical turn of the co-repressor motif in the PPAR/GW6471/SMRT complexes. [1] GW6471 at concentration of 10 μM significantly prevents cardiomyocyte differentiation and results in the reduced expression of cardiac sarcomeric proteins (ie α-actinin, troponin-T) and specific genes (ie α-MHC, MLC2v) in a time-dependent manner through inhibiting PPARα.

PPARα

GW 6471 is a peroxisome proliferator-activated receptor α (PPARα) antagonist. GW 6471 has been shown to enhance the binding affinity of the PPARα ligand-binding domain to the co-repressor proteins SMRT and NCoR.

GW6471 prevents apoptosis and cell cycle arrest at G₀/G₁ in renal cell carcinoma. It reduces enhanced fatty acid oxidation and oxidative phosphorylation associated with glycolysis inhibition.

GW6471 is a PPARα antagonist, which completely inhibits GW409544-induced activation of PPARα with an IC50 = 0.24 μM. GW6471 induces a PPARα conformation that interacts efficiently with co-repressors.

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