SPD304, >=98% (HPLC), solid

Descriptions

Application

SPD304 may be used in TNF-α-mediated cell signaling studies.

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.

Biochem/physiol Actions

Trimerization of TNF-? 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-?B ligand (RANKL) by similar interaction.

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.

Packaging

1, 5 mg in glass bottle

Specifications

Colour	white
Quality Level	100
InChI key	GOZMBJCYMQQACI-UHFFFAOYSA-N
InChI	1S/C32H32F3N3O2.2ClH/c1-21-14-28-30(15-22(21)2)40-20-24(31(28)39)18-37(4)13-12-36(3)17-23-19-38(29-11-6-5-10-27(23)29)26-9-7-8-25(16-26)32(33,34)35;;/h5-11,14-
Manufacturer	SIGMA-ALDRICH
Form	solid
Assay	≥98% (HPLC)