MilliporeSigma™ Calbiochem™ RXRα Inhibitor, K-80003

Description

The RXRα Inhibitor, K-80003 controls the biological activity of RXRα. This small molecule/inhibitor is primarily used for Cell Signaling applications.

A cell permeable, Sulindac analog with IC₅₀=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.

Specifications

• Color: Yellow
• Description: 95% by HPLC
• Molecular Formula: C₂₃H₂₃FO₂
• Formula Weight: 350.4g/mol
• Solubility: DMSO
• Form: Solid
• Quantity: 10 mg