1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENodinitib-1Cat. No.: HY-18639CAS No.: 799264-47-4Synonyms: ML130; CID-1088438分式: CHNOS分量: 287.34作靶點(diǎn): NOD-like Receptor (NLR)作通路: Immunology/Inflammation儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體

2、外實(shí)驗(yàn) DMSO : 20 mg/mL (69.60 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.4802 mL 17.4010 mL 34.8020 mL5 mM 0.6960 mL 3.4802 mL 6.9604 mL10 mM 0.3480 mL 1.7401 mL 3.4802 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Nodinitib-1 (ML130;CID-

3、1088438)是NOD1抑制劑，IC50值為0.56 M。IC50 & Target IC50: 0.56 M (NOD1) 1體外研究Nodinitib-1 selectively inhibits IL-8 production induced by NOD1 ligand. Nodinitib-1 also inhibits -tri-DAP-induced expression of the prototypical NF-B target gene IB at the mRNA level. Nodinitib-1 inhibits -tri-1/2 Master of Small

4、 Molecules 您邊的抑制劑師www.MedChemEDAP-dependent activation of NF-B (IB phosphorylation and degradation) and MAPK (p38phosphorylation) signalings, without affecting Akt survival pathway. Nodinitib-1 selectively inhibits responsesof primary dendritic cells to NOD1 ligand. Nodinitib-1 reduces cell surface

5、expression of co-stimulatorymolecules CD83, CD86 and HLA-DR and also inhibits expression of IL-1, IL-6 and TNF elicited by -tri-DAP (but not by LPS), without causing cytoxicity 1. Nodinitib-1 is identified as NOD1-selective moleculesfrom an HTS campaign involving 290,000 compounds. Nodinitib-1 inhib

6、its -tri-DAP-stimulated luciferaseproduction in HEK 293T cells, which has endogenous NOD1 levels at submicromolar concentration asdetermined in a NF-B-linked reporter assay 2.PROTOCOLCell Assay 1 RAW264.7 cells are treated with 5 M of CID-1088438 or CID-44229067 alone, or also infected with S.typhim

7、urium at multiplicity of infection (MOI) of 20 and 200 bacteria per mammalian cell. Cell viability isanalyzed two hours after Salmonella infection by measuring ATP levels. Percentage viability is calculatedaccording to the ATP levels of respective non-infected cells. Values presented are averages of

8、 two replicates(+ SEM) 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Front Immunol. 2018 Jul 2;9:1528.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Correa RG, et al. Discovery and characterization of 2-aminobenzim

9、idazole derivatives as selective NOD1 inhibitors. Chem Biol. 2011 Jul29;18(7):825-32.2. Hershberger PM, et al. Synthesis and physicochemical characterization of novel phenotypic probes targeting the nuclear factor-kappa Bsignaling pathway. Beilstein J Org Chem. 2013 May 8;9:900-7.McePdfHeightCaution: Product has not been fully validated for medica