RXRalpha Inhibitor, K-80003 - Calbiochem (C15-1305-720)

General description

A cell permeable, Sulindac analog with IC₅₀=2.4 µM 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 50 µM when used with TNF-α. Furthermore, it almost completely suppresses colony formation of HeLa/RXRα/1-134 and RXRα/Δ80 cells at 25 µM in vitro, and exhibits potent inhibition of tumor growth in vivo when dosed at 60mg/kg.

A cell permeable, Sulindac analog with IC₅₀=2.4 µM 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 50 µM when used with TNF-α. Furthermore, it almost completely suppresses colony formation of HeLa/RXRα/1-134 and RXRα/Δ80 cells at 25 µM in vitro, and exhibits potent inhibition of tumor growth in vivo when dosed at 60 mg/kg.

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C.

Other Notes

Zhou, H., et al. 2010. Cancer Cell17, 560.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Molecular Weight: 336.40. Empirical Formula: C₂₂H₂₁FO₂. Quality Level: 100. Assay: ≥. 95% (HPLC). form: solid. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze. color: yellow. solubility: DMSO: 50 . mg/mL. shipped in: wet ice. storage temp.: 2-8°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 2. Flash Point(F): Not applicable. Flash Point(C): Not applicable.