SPD304 |
Catalog No.GC33133 |
Le SPD304 est un inhibiteur sélectif du TNF-α, qui favorise la dissociation des trimères du TNF et bloque donc l'interaction du TNF et de son récepteur. SPD304 a une IC50 de 22 μM pour inhiber la liaison in vitro du récepteur 1 du TNF (TNFR1) au TNF-α.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 869998-49-2
Sample solution is provided at 25 µL, 10mM.
SPD304 is a selective inhibitor of tumor necrosis factor α (TNFα) and promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor, with an IC50 of 22 µM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α[1][2]. SPD304 cannot be used in vivo due to its high toxicity[3].
SPD304 (2 μM) significantly rescues the survivability of aHSCs, reduces the production of lipid hydroxides, and increased intracellular GSH. The co-treatment of GA (75 μM) and SPD304 (2 μM), down-regulate TRADD almost 2-fold (w/o inhibitor vs. w/ inhibitor) and p-RIP3 1.4-fold compared to GA alone, and promotes caspase 8 activation[4].
[1]. Molly M. He, et al. Small-Molecule Inhibition of TNF-α. Science 11 Nov 2005. [2]. Alexiou P, et al. Rationally designed less toxic SPD-304 analogs and preliminary evaluation of their TNF inhibitory effects. Arch Pharm (Weinheim). 2014 Nov;347(11):798-805. [3]. Mouhsine H, et al. Identification of an in vivo orally active dual-binding protein-protein interaction inhibitor targeting TNFα through combined in silico/in vitro/in vivo screening. Sci Rep. 2017 Jun 13;7(1):3424. [4]. Gallic acid induces necroptosis via TNF-α signaling pathway in activated hepatic stellate cells. Chang YJ, et al. PLoS One. 2015 Mar 27;10(3):e0120713.
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