IL-13 Modulator

Oxazolone is a haptenizing agent that induces acute or chronic inflammation of the large intestine and is used to construct models of colitis. Oxazolone can cause Th1/Th2-dependent colitis with weight loss and diarrhea. Oxazolone-induced inflammation can be mitigated by neutralizing anti-IL-4 or anti-TNF-α antibodies or decoy IL-13R2-α-FC proteins.

APH003 is an orally active IRAK4 PROTAC degrader with a DC₅₀ of 0.74 nM in human peripheral blood mononuclear cells (hPBMCs). APH003 recruits IRAK4 to CRBN to form a ternary complex, mediates the ubiquitination and degradation of IRAK4 via the ubiquitin-proteasome pathway, and inhibits the kinase activity of IRAK4. APH003 inhibits LPS- or IL-1β/LPS-induced phosphorylation of ERK, JNK and NF-κB. APH003 inhibits the secretion of TNF-α, IL-6, IL-8 and IL-13 by stimulated hPBMCs. APH003 exhibits anti-inflammatory activity in rat TNBS-induced intestinal inflammation models and mouse IL-33-induced skin inflammation models. APH003 can be used in research related to inflammatory bowel disease and skin inflammation.