tnfα antagonist

TNF-α antagonist is an exocyclic peptide that mimics the critical TNF-α recognition loop on TNF receptor I complex and, thus, prevents ligand interaction with the receptor. By blocking the TNF receptor ligand contact site, this peptide interferes with both activating receptor activator of NF-κB (RANK) and TNF-α's recruitment and activation of osteoclasts. TNF-α antagonist has been used to block bone resorption in the study of systemic bone loss in rheumatoid arthritis and inflammatory bone destruction.

R-7050 (TNF-α Antagonist III) is a tumor necrosis factor receptor (TNFR) antagonist that exhibits heightened selectivity for TNFα.

ASTX660 is an innovative non-peptide mimic antagonist targeting cIAP1/2 and XIAP, effectively inducing TNFα-dependent apoptosis in cancer cell lines and inhibiting tumor growth.

GNE-5472 is a potent dual-function ERαPRRTAC degrader featuring an E3 ligase ligand that acts as a pan-IAP antagonist. By antagonizing cIAP1/2, GNE-5472 activates the non-canonical NF-κB pathway, resulting in a significant upregulation of TNFα expression. It inhibits the proliferation of breast cancer cells and induces apoptosis. GNE-5472 is applicable in breast cancer research.

IW-927 is a potent and selective TNFα/TNFRc1 interaction antagonist.

Dersalazine, a PAF antagonist and TNFα inhibitor, is used potentially for the treatment of ulcerative colitis. It showed anti-inflammatory effect in reactivated colitis in rats, as evidenced by a significant reduction in MPO activity.

Larsucosterol trimethylamine (DUR-928 trimethylamine) is a potent liver X receptor (LXR) antagonist that modulates endogenous epigenetics, reduces lipid accumulation in hepatocytes, attenuates lipopolysaccharide (LPS) and TNFα-induced inflammatory responses in macrophages, and alleviates LPS- and acetaminophen (ATMP)-induced multi-organ damage.