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CAS No.: 799264-47-4

Nodinitib-1 Catalog No. CSN16516

Synonyms: ML130;CID-1088438

ML130 is a selective and potent NOD1 inhibitor with IC50 of 560 nM. It inhibits NOD1-induced NF-κB activation.

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实验方案

技术信息

生物活性

描述ML130 is a potent and selective NOD1 inhibitor with IC50 value of 0.56μM^[4]. It selectively inhibited IL-8 production induced by NOD1 ligand and also inhibited γ-tri-DAP-induced expression of the prototypical NF-kB target gene IκBα at the mRNA level as well as inhibited MAPK (p38 phosphorylation) signaling. ML130 caused conformational changes of NOD1 in vitro and altered NOD1 subcellular targeting in cells. It reduced membrane localization of RIP2, a NOD1-binding partner required for NF-kB induction^[3].
作用机制ML130 causes conformational changes of NOD1 and alters its subcellular localization.^[3]
动物研究
剂量
Mice: 5 mg/kg^[3] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 5 mg/kg^[3] (i.p.)
给药途径	i.p.

[1] Khan PM, Correa RG, et al. Identification of Inhibitors of NOD1-Induced Nuclear Factor-κB Activation. ACS Med Chem Lett. 2011 Oct 13;2(10):780-785. Epub 2011 Aug 5.
[2] Correa RG, Khan PM, et al. Discovery and characterization of 2-aminobenzimidazole derivatives as selective NOD1 inhibitors. Chem Biol. 2011 Jul 29;18(7):825-32.
[3] Correa RG, Khan PM, Askari N, Zhai D, Gerlic M, Brown B, Magnuson G, Spreafico R, Albani S, Sergienko E, Diaz PW, Roth GP, Reed JC. Discovery and characterization of 2-aminobenzimidazole derivatives as selective NOD1 inhibitors. Chem Biol. 2011 Jul 29;18(7):825-32. doi: 10.1016/j.chembiol.2011.06.009. PMID: 21802003; PMCID: PMC3152441.
[4] Khan PM, Correa RG, Divlianska DB, Peddibhotla S, Sessions EH, Magnuson G, Brown B, Suyama E, Yuan H, Mangravita-Novo A, Vicchiarelli M, Su Y, Vasile S, Smith LH, Diaz PW, Reed JC, Roth GP. Identification of Inhibitors of NOD1-Induced Nuclear Factor-κB Activation. ACS Med Chem Lett. 2011 Oct 13;2(10):780-785. doi: 10.1021/ml200158b. Epub 2011 Aug 5. PMID: 22003428; PMCID: PMC3193285.

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
- 3.4802 mL
- 17.4012 mL
- 34.8024 mL
- 5 mM
- 0.6960 mL
- 3.4802 mL
- 6.9605 mL
- 10 mM
- 0.3480 mL
- 1.7401 mL
- 3.4802 mL

技术信息

CAS号

799264-47-4

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H13N3O2S

运输

蓝冰

分子量

287.34

别名

ML130;CID-1088438

溶解度

DMSO	57.0 mg/mL (198.4 mM)
Water	Insoluble
Ethanol	2.0 mg/mL (7.0 mM)

动物实验配方

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