2-Chloro-5-nitro-N-(4-pyridyl)benzamide White solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable chloro-nitro-benzamido compound that acts as a potent, specific, irreversible, and high-affinity antagonist of PPARg with a Ki of 1 nM. Displays >800-fold greater selectivity for PPARg over PPARa and PPARd (Ki = 0.85 µM and 1.8 µM, respectively). Blocks hormone- and agonist-induced adipogenesis in 3T3-L1 cells. It suppresses interactions between PPARg and coactivator-derived peptides, while promotes the recruitment of corepressor-derived peptides. Shown to modulate the interaction of PPARg2 with the cofactor proteins through covalent binding to Cys313 in its ligand-binding domain. Purity: ≥97% by HPLC. CAS 313516-66-4. Ref.: Lee, G., et al. 2002. J. Biol. Chem. 277, 19649. |
