GSK717 是NOD2(核苷酸结合寡聚结构域 2) 的选择性抑制剂。它抑制壁酰二肽 (MDP) 诱导的 NOD2 介导的信号转导,抑制 MDP 刺激的 HEK293/hNOD2 细胞分泌 IL-8 (IC50为 400 nM)。
产品描述
GSK717 is a potent and selective inhibitor of nucleotide-binding oligomerization domain 2 (NOD2). GSK717 blocks synergy between NOD2 and TLR2. GSK717 does not affect NOD1, TNFR1 and TLR2-mediated responses.
体外活性
GSK717 (5 μM) inhibits the release of IL-8, IL-6, TNFα and IL-1β in primary human monocytes stimulated with MDP. GSK717 inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells[1].
Cas No.
1595278-21-9
分子式
C28H28N4O2
分子量
452.55
储存和溶解度
DMSO:250 mg/mL (552.43 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years