KRN2-bromide-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEKRN2bromideCat.No.:HY-112125ACASNo.:1390654-28-0分?式:C??H??BrFNO?分?量:524.38作?靶點:NuclearFactorofactivatedTCells(NFAT)作?通路:Immunology/Inflammation儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數據體外實驗DMSO:18.33mg/mL(34.96mM;Needultrasonic)H2O:1.1mg/mL(2.10mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.9070mL9.5351mL19.0701mL5mM0.3814mL1.9070mL3.8140mL10mM0.1907mL0.9535mL1.9070mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥1.83mg/mL(3.49mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥1.83mg/mL(3.49mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥1.83mg/mL(3.49mM);ClearsolutionBIOLOGICALACTIVITY?物活性KRN2bromide選擇性的T細胞激活核因?(NFAT5)的抑制劑，IC50值為100nM。KRN2bromide有潛??于NFAT5-介導的慢性關節(jié)炎的潛能。IC50&TargetIC50:100nM(NFAT5)[1]體外研究KRN2selectivelysuppressestheexpressionofpro-inflammatorygenes,includingNos2andIl6,withouthamperinghigh-salt-inducedNFAT5anditstargetgeneexpressions[1].KRN2dose-dependentlyinhibitstheNF-κBp65bindingtoNfat5promoter1anddirectlyblockstheinteractionbetweenNF-κBp65anditsDNAbindingsequenceintheupstreamsite(basepairs-3000to+1)ofNfat5exon1[1].體內研究KRN2(3mg/kg,i.p.,dailyfor2weeks)effectivelysuppressesAIAinwhichinnateimmunecellsplayapredominantrole[1].KRN2(3mg/kg,i.p.,daily)effectivelysuppressesCIAaswellasAIAinmice,decreasingtheproductionofpro-inflammatorycytokinesandautoantibodiesaswellasmacrophageinfiltration[1].AnimalModel:8-week-oldC57BL/6miceinjectedintradermallywith2mgofcompleteFreund'sadjuvant[1].Dosage:3mg/kg.Administration:Peritoneally(i.p.)dailyfor2weeks.Result:EffectiveinsuppressingAIA.AnimalModel:8-week-oldDBA/1JmiceimmunizedwithbovinetypeIIcollagen[1].Dosage:3mg/kg.Administration:Peritoneally(i.p.)daily.Result:EffectiveinsuppressingCIAaswellasAIAinmice,decreasingtheproductionofpro-inflammatorycytokinesandautoantibodiesaswellasmacrophageinfiltration.戶使?本產品發(fā)表的科研?獻?JImmunol.2021Jun1;206(11):2652-2667.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].HanEJ,etal.SuppressionofNFAT5-mediatedInflammationandChronicArthritisbyNovelκB-bindingInhibitors.EBioMedicine.2017Apr;18:261-273.McePdfHeightCaution:Producthasnotbeenfullyvalidated