MilliporeSigma™ Calbiochem™ RXRα Inhibitor, K-80003

Description

• A cell permeable, Sulindac analog with IC 50 =2.4μM for RXRα binding, and unlike other NSAIDs, is inactive toward COX2 and COX1 even at 1 mM
• The compound displays potent inhibition of RXRα dependent AKT Activation in both PC3 and A549 cells, and is RXRα but not RXRγ expression dependent as shown in PC3 cells
• It is further shown to inhibit the interaction of RXRα/δ80 with p85α either in the absence or presence of TNF-α
• Induces PARP cleavage and caspase-8 activation at 50μM when used with TNF-α
• Furthermore, it almost completely suppresses colony formation of HeLa/RXRα/1-134 and RXRα/δ80 cells at 25μM in vitro, and exhibits potent inhibition of tumor growth in vivo when dosed at 60mg/kg.