Description
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 EC
50 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.
References
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).
![1-(4-CHLOROPHENYL)-4-(TRIFLUOROMETHYL)[1,2,4]TRIAZOLO[4,3-A]QUINOXALINE Structure](https://www.chemicalbook.com/StructureFile/ChemBookStructure3/GIF/CB9238349.gif)