RAGE antagonist peptide acetate is an advanced antagonist of glycation end products (RAGE). RAGE antagonist peptide acetate possesses anti-tumor and anti-inflammatory activities. RAGE antagonist peptide acetate prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4.

In cancer cells, RAGE antagonist peptide acetate reduces the ability of the ligands to stimulate RAGE activation of NFκB[2].

In mice bearing asthma, RAGE antagonist peptide acetate (RAP; 4 mg/kg; i.p.) blunts airway reactivity, airway inflammation and goblet cell metaplasia, and decreases release of Th2 cytokines. RAGE antagonist peptide acetate also reduces total, cytoplasmic and nuclear levels of β-catenin, enhanced β-catenin phosphorylation at Ser33/37/Thr41, which triggers ubiquitination, down-regulated expression of β-catenin targeted genes, and tends to keep β-catenin at the cytomembrane, shifting β-catenin from a signalling active pattern to an adhesive function[1]. RAGE antagonist peptide acetate reduces the growth and metastasis of pancreatic tumors and also inhibited glioma tumor growth. RAGE antagonist peptide acetate (100 μg) inhibits RAGE-mediated Basal NFκB Activity in PDAC cells in vivo[2].