CAS:313516-66-4|2-Chloro-5-nitro-N-4-pyridinylbenzamide

Catalogue Number:C374760
Chemical Name:2-Chloro-5-nitro-N-4-pyridinylbenzamide
Synonyms:T0070907
CAS Number:313516-66-4
Molecular Formula:C₁₂H₈ClN₃O₃
Appearance:Light Beige to Light Brown Solid
Melting Point:>184°C (dec.)
Molecular Weight:277.66
Storage:4°C
Solubility:DMSO (Slightly), Methanol (Slightly)
Category:Standards; Enzyme Activators and Inhibitors;
Applications:A cell-permeable chloro-nitro-benzamido compound that acts as a potent, specific, irreversible, and high-affinity antagonist of PPARγ with a Ki of 1 nM. Displays >800-fold greater selectivity for PPARγ over PPARa and PPARδ (Ki = 0.85 uM and 1.8 uM, respectively). Blocks hormone- and agonist-induced adipogenesis in 3T3-L1 cells. It suppresses interactions between PPARγ and coactivator-derived peptides, while promotes the recruitment of corepressor-derived peptides. Shown to modulate the interaction of PPARγ2 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)
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