ST 2825
Names
Biological Activity
[Description]:
ST 2825 is a MyD88 dimerization inhibitor.
[Related Catalog]:
[Target]
MyD88[1]
[In Vitro]
ST2825 blocks IL-1R/TLR signaling by interfering with MyD88 homodimerization. ST2825 inhibits this interaction in a concentration-dependent manner with ~40% inhibition of dimerization at 5 μM ST2825 and 80% inhibition at 10 μM ST2825[1].
[In Vivo]
ST2825 dose-dependently inhibits IL-1β-induced production of IL-6 in treated mice after oral administration. The animals are administered orally with the appropriate vehicles or ST2825 at doses ranging from 50 to 200 mg/kg, 5 min prior to i.p. injection with 20 μg/kg IL-1β. ST2825 exertes a significant inhibition of IL-1β-stimulated production of IL-6 at 100 and 200 mg/kg[1].
[Cell Assay]
HeLa cells are seeded at 105 cells/mL in a 96-well tissue-culture plate. After incubating overnight, the medium is discarded, and the cells are added with tissue culture medium, 10% FBS, containing ST2825 at concentrations ranging from 0.1 to 10 μM and DMSO at 0.1% final concentration. The cells are incubated for 6 and 18 h and then added with the yellow XTT (0.3 mg/mL) for further 2 h of incubation. At the end of the incubation periods, reactions are quantified by using a Sirio S Seac microplate reader[1].
[Animal admin]
Mice[1] Mice (female C57Bl/6) are divided into experimental groups of 15 mice. They are injected i.p. with saline (control animals) or recombinant murine IL-1β (20 μg/kg). A time-course analysis of IL-6 production established that the peak of cytokine is reached 2 h after IL-1β injection. ST2825, administered orally as 0.5% suspension in carboxymethylcellulose (CMC) or CMC alone, is supplied to the experimental mice groups. Two hours after IL-1β injection, the animals are killed, and sera are collected to assay IL-6 levels. Mice, which are treated orally with 100 and 200 mg/kg ST2825, shows lower levels of IL-6 versus CMC-treated mice.
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C27H28Cl2N4O5S
[ Molecular Weight ]:
591.50600
[ Exact Mass ]:
590.11600
[ PSA ]:
148.33000
[ LogP ]:
4.56230
[ Storage condition ]:
2-8℃