1595278-21-9|N-(2-(1-(2-((2,3-Dihydro-1H-inden-5-yl)amino)-2-oxoethyl)-1H-benzo[d]imidazol-2-yl)ethyl)-N-methylbenzamide|CsnPharm

CAS No.: 1595278-21-9

GSK717 Catalog No. CSN27580

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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400-920-2911

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400-920-2911

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技术信息

生物活性

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].
参考文献

[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.
[2] Rickard DJ, et al. Identification of benzimidazole diamides as selective inhibitors of the nucleotide-binding oligomerization domain 2 (NOD2) signaling pathway. PLoS One. 2013 Aug 1;8(8):e69619

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2097 mL
- 11.0486 mL
- 22.0971 mL
- 5 mM
- 0.4419 mL
- 2.2097 mL
- 4.4194 mL
- 10 mM
- 0.2210 mL
- 1.1049 mL
- 2.2097 mL

技术信息

CAS号	1595278-21-9	储存条件	粉末 Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C28H28N4O2	运输	蓝冰
分子量	452.55	别名

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