APH003

Overview

APH003 is an orally active IRAK4 PROTAC degrader with a DC 50 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. (Pink: IRAK4 ligand ( HY-184916 ); Blue: Cereblon ligand ( HY-49385 ); Black: linker).

Application

Products | Products > Disease Areas > Inflammation or Immune System Disease | Products > Disease Areas > Digestive System Disease | Products > Disease Areas > Skin Inflammation | Products > Disease Areas > Digestive System Inflammation | Products > Signaling Pathways > PROTAC | Products > Signaling Pathways > Immunology/Inflammation | Products > Signaling Pathways > Stem Cell/Wnt | Products > Signaling Pathways > MAPK/ERK Pathway | Products > Signaling Pathways > NF-κB | Products > Research Areas > Inflammation/Immunology | Products > Signaling Pathways > ERK | Products > Signaling Pathways > JNK | Products > Signaling Pathways > NF-κB | Products > Signaling Pathways > PROTACs | Products > Signaling Pathways > IRAK | Products > Signaling Pathways > Interleukin Related

Product Information

• Catalog No.: HY-184915
• CAS No.: 3065495-08-8
• Molecular Formula: C44H50FN11O7
• Molecular Weight: 863.94
• Storage: Please store the product under the recommended conditions in the Certificate of Analysis.

Source

Original product source