GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor. 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 .
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描述 | As a NLR family member, NOD2 (nucleotide-binding oligomerization domain 2) is an intracellular pattern recognition receptor that assembles with receptor-interacting protein (RIP)-2 kinase in response to the presence of bacterial muramyl dipeptide (MDP) in the host cell cytoplasm, thereby inducing signals leading to the production of pro-inflammatory cytokines. GSK717 is a potent and selective NOD2 inhibitor. GSK717 (0.5-16 μM; 1 hour) blocked synergy between NOD2 and TLR2 (Toll-like receptor 2) in primary human monocytes. GSK717 does not affect NOD1, TNFR1 (tumour necrosis factor receptor-1) and TLR2-mediated responses. GSK717 (5 μM) inhibited the release of IL-8, IL-6, TNFα and IL-1β in primary human monocytes stimulated with MDP (muramyl dipeptide). GSK717 inhibited MDP-induced NOD2-mediated signaling with an IC50 of 400 nM for IL-8 secretion stimulated by MDP in HEK293/hNOD2 cells[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.21mL 0.44mL 0.22mL |
11.05mL 2.21mL 1.10mL |
22.10mL 4.42mL 2.21mL |
CAS号 | 1595278-21-9 |
分子式 | C28H28N4O2 |
分子量 | 452.548 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 250 mg/mL(552.43 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |