557451
RXRα Inhibitor, K-80003
The RXRα Inhibitor, K-80003 controls the biological activity of RXRα. This small molecule/inhibitor is primarily used for Cell Signaling applications.
别名:
RXRα Inhibitor, K-80003, K-80003
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
yellow
solubility
DMSO: 50 mg/mL
shipped in
wet ice
Quality Level
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.
Preparation Note
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
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Hua Li et al.
Scientific reports, 11(1), 16956-16956 (2021-08-22)
Osteoarthritis (OA), a most common and highly prevalent joint disease, is closely associated with dysregulated expression and modification of RXRα. However, the role of RXRα in the pathophysiology of OA remains unknown. The present study aimed to investigate whether RXRα
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