338773-13-0

R-8507 is a small molecule antagonist of the TNF-α type 1 receptor (TNF-αRI).¹ It inhibits the expression of intercellular adhesion molecule-1 (ICAM-1) induced by TNF-α and IL-1β with EC₅₀ values of 2.45 and 3.79 μM, respectively, in an ELISA using A549 lung epithelial cells.{|Gururaja2007|} It also disrupts the interaction of the TNF-αRI with receptor interacting protein 1 (RIP1) and TNF-αR-associated death domain protein (TRADD), preventing internalization of the receptor complex.

1. Gururaja, T.L., Yung, S., Ding, R., et al. A class of small molecules that inhibit TNFα-induced survival and death pathways via prevention of interactions between TNFαRI, TRADD, and RIP1 Chem. Biol. 14(10),1105-1118(2007).