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Description

Category: Inhibitors /// Appearance: Light Orange Solid /// Application Notes: A cell-permeable chloro-nitro-benzamido compound that acts as a potent, specific, irreversible, and high-affinity antagonist of PPARgamma with a Ki of 1 nM. Displays >800-fold greater selectivity for PPARgamma over PPARalpha and PPARdelta (Ki = 0.85 µM and 1.8 µM, respectively). Blocks hormone- and agonist-induced adipogenesis in 3T3-L1 cells. It suppresses interactions between PPARgamma and coactivator-derived peptides, while promotes the recruitment of corepressor-derived peptides. Shown to modulate the interaction of PPARgamma2 with the cofactor proteins through covalent binding to Cys313 in its ligand-binding domain. /// References: Lee, G., et al: J. Biol. Chem., 277, 19649 (2003), Schaefer, K.L., et al: Cancer Res., 65, 2251 (2005), Masuda, T., et al.: Clin. Cancer Res., 11, 4012 (2005), Raikwar, H.P., et al.: J. Neuroimmunol., 167, 99 (2005)