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Description_x000D_
Application_x000D_
SPD304 has been used in the inhibition of tumor necrosis factor receptor 1 (TNFR1) in dorsal root ganglion neurons and tumor necrosis factor alpha in colonic epithelial cell lines._x000D_
SPD304 may be used in TNF-α-mediated cell signaling studies._x000D_
Packaging_x000D_
1, 5 mg in glass bottle_x000D_
Biochem/physiol Actions_x000D_
SPD304 is a small molecule inhibitor of TNF-a activity with a novel mechanism of action. It interferes with protein-protein interactions on the contact surfaces of the trimeric TNF-a subunits, displacing one of the trimer units, resulting in dissociation of the trimer and loss of activity at the receptor TNFR1. SPD304 inhibits TNFR1 receptor binding to TNF-a with an IC50 of 22μM in vitro and inhibits TNF-a-mediated stimulation of IkB degradation in HeLa cells with an IC50 of 4.6 μM._x000D_
Trimerization of TNF-α is essential for its biological activity. SPD304 inhibits the trimerization by interacting with Glycine 122 residue. It also inhibits the activity of Receptor activator of nuclear factor-κB ligand (RANKL) by similar interaction.
- Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, Cytokines and Growth Factors, Cytokines, Growth Factors and Hormones, S, TNF-α, Tumor Necrosis Factor (TNF) SuperfamilyMore... Quality Level