Molecular Formula | C28H28N4O2 |
Molar Mass | 452.56 |
Density | 1.23±0.1 g/cm3(Predicted) |
Boling Point | 731.6±60.0 °C(Predicted) |
Solubility | DMSO : 100 mg/mL |
pKa | 14.05±0.20(Predicted) |
Storage Condition | -20℃ |
Use | GSK717 is a potent, selective inhibitor of NOD2 (nucleotide-binding oligomeric domain 2). GSK717 inhibits NOD2-mediated signal transduction induced by mural acyl dipeptide (MDP), and the IC50 in the secretion IL-8 of HEK293/hNOD2 cells stimulated by MDP is 400 nM. |
In vitro study | GSK717 blocks synergy between NOD2 and TLR2. GSK717 does not affect NOD1, TNFR1 and TLR2-mediated responses. GSK717 (5 μM) inhibits the release of IL-8, IL-6, TNFα and IL-1β in primary human monocytes stimulated with MDP. |
Reference Show more | 1. Rickard DJ, et al. Identification of benzimidazole diamides as selective inhibitors of the nucleotide-binding oligomerization domain 2 (NOD2) signaling pathway. PLoS One. 2013;8(8):e69619. Published 2013 Aug 1. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.21 ml | 11.049 ml | 22.097 ml |
5 mM | 0.442 ml | 2.21 ml | 4.419 ml |
10 mM | 0.221 ml | 1.105 ml | 2.21 ml |
5 mM | 0.044 ml | 0.221 ml | 0.442 ml |
biological activity | GSK717 is an effective and selective NOD2 (nucleotide binding oligomeric domain 2) inhibitor. GSK717 inhibits NOD2-mediated signal transduction induced by mural acyl dipeptide (MDP), and the IC50 in the secretion IL-8 of HEK293/hNOD2 cells stimulated by MDP is 400 nM. |
in vitro studies | GSK717 blocks synergy between NOD2 and TLR2. GSK717 doesnot affect NOD1, TNFR1 and TLR2-mediated responses. GSK717 (5 μM) inhibits the release of IL-8, IL-6, TNFα and IL-1β in primary human monocytes stimulated with MDP. |