KRN2-bromide-DataSheet-生命科學(xué)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(diǎn):NuclearFactorofactivatedTCells(NFAT)作?通路:Immunology/Inflammation儲(chǔ)存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:18.33mg/mL(34.96mM;Needultrasonic)H2O:1.1mg/mL(2.10mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.9070mL9.5351mL19.0701mL5mM0.3814mL1.9070mL3.8140mL10mM0.1907mL0.9535mL1.9070mL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(chǔ)備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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(xiàn)沉淀、析出現(xiàn)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(xì)胞激活核因?(NFAT5)的抑制劑，IC50值為100nM。KRN2bromide有潛??于NFAT5-介導(dǎo)的慢性關(guān)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(nèi)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(chǎn)品發(fā)表的科研?獻(xiàn)?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