产品描述:
STING PROTAC SP23 is a proteolysis-targeting chimera (PROTAC) containing the stimulator of interferon genes (STING) inhibitor C-170 (Item No. 30157) conjugated to the cereblon (CRBN) inhibitor pomalidomide (Item No. 19877) via an α,β-unsaturated carbonyl linker.{72246} It degrades STING in THP-1 cells with a half-maximal degradation concentration (DC50) of 3.2 µM, an effect that can be blocked by the proteasome inhibitor MG132 but not the lysosome inhibitor bafilomycin. STING PROTAC SP23 (2.5-20 µM) decreases cGAMP-induced increases in the levels of IFN-β, IL-6, and chemokine (C-X-C motif) ligand 10 (CXCL10) in THP-1 cells. It also reduces kidney weight, improves kidney function, and increases the survival rate in a mouse model of acute kidney injury induced by the DNA-crosslinking agent cisplatin (Item No. 13119) when administered at doses of 30 and 60 mg/kg.