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BAY-4931 is a PPARγ inverse agonist.1 It acts as an inverse agonist in a co-repressor reporter assay with a peptide from nuclear receptor co-repressor 2 (NCOR2; EC50 = 5.8 nM). BAY-4931 selectively induces PPARγ-mediated gene transcription (IC50 = 0.4 nM for the human receptor) over PPARα- or PPARδ-mediated gene transcription in reporter assays using CHO cells (IC50s = >50 µM for both for the human receptors). BAY-4931 inhibits the proliferation of UM-UC-9 human bladder cancer cells that endogenously contain a focal amplification of PPARG, the gene encoding PPARγ (IC50 = 3.4 nM).
WARNING This product is not for human or veterinary use.
1. Discovery and structure-