Nodinitib-1-ML130-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemENodinitib-1Cat.No.:HY-18639CASNo.:799264-47-4Synonyms:ML130;CID-1088438分⼦式:C₁₄H₁₃N₃O₂S分⼦量:287.34作⽤靶点:NOD-likeReceptor(NLR)作⽤通路:Immunology/Inflammation储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:20mg/mL(69.60mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.4802mL17.4010mL34.8020mL5mM0.6960mL3.4802mL6.9604mL10mM0.3480mL1.7401mL3.4802mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>90%cornoil1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(8.70mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Nodinitib-1(ML130;CID-1088438)NOD1抑制剂，IC50值为0.56μM。IC50&TargetIC50:0.56μM(NOD1)[1]体外研究Nodinitib-1selectivelyinhibitsIL-8productioninducedbyNOD1ligand.Nodinitib-1alsoinhibitsγ-tri-DAP-inducedexpressionoftheprototypicalNF-κBtargetgeneIκBαatthemRNAlevel.Nodinitib-1inhibitsγ-tri-DAP-dependentactivationofNF-κB(IκBαphosphorylationanddegradation)andMAPK(p38phosphorylation)signalings,withoutaffectingAktsurvivalpathway.Nodinitib-1selectivelyinhibitsresponsesofprimarydendriticcellstoNOD1ligand.Nodinitib-1reducescellsurfaceexpressionofco-stimulatorymoleculesCD83,CD86andHLA-DRandalsoinhibitsexpressionofIL-1β,IL-6andTNFαelicitedbyγ-tri-DAP(butnotbyLPS),withoutcausingcytoxicity[1].Nodinitib-1isidentifiedasNOD1-selectivemoleculesfromanHTScampaigninvolving~290,000compounds.Nodinitib-1inhibitsγ-tri-DAP-stimulatedluciferaseproductioninHEK293Tcells,whichhasendogenousNOD1levelsatsubmicromolarconcentrationasdeterminedinaNF-κB-linkedreporterassay[2].PROTOCOLCellAssay[1]RAW264.7cellsaretreatedwith5μMofCID-1088438orCID-44229067alone,oralsoinfectedwithS.typhimuriumatmultiplicityofinfection(MOI)of20and200bacteriapermammaliancell.CellviabilityisanalyzedtwohoursafterSalmonellainfectionbymeasuringATPlevels.PercentageviabilityiscalculatedaccordingtotheATPlevelsofrespectivenon-infectedcells.Valuespresentedareaveragesoftworeplicates(+SEM)[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•FrontImmunol.2018Jul2;9:1528.•FrontPharmacol.2022Jul22;13:920928.•CellSignal.2022Feb14;93:110283.•MolOralMicrobiol.2021Mar14.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].CorreaRG,etal.Discoveryandcharacterizationof2-aminobenzimidazolederivativesasselectiveNOD1inhibitors.ChemBiol.2011Jul29;18(7):825-32.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[2].HershbergerPM,etal.Synthesisandphysicochemicalcharacterizationofnovelphenotypicprobestargetingthenuclearfactor-kappaBsignalingpathway.BeilsteinJOrgChem.2013May8;9:900-7.McePdfHeightCaution:Producthasnotbeenfull