ADU-S100-disodium-salt-MIW815-disodium-salt-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEADU-S100disodiumsaltCat.No.:HY-12885ACASNo.:1638750-95-4Synonyms:MIW815disodiumsalt;MLRR-S2CDAdisodiumsalt分⼦式:C₂₀H₂₂N₁₀Na₂O₁₀P₂S₂分⼦量:734.51作⽤靶点:STING作⽤通路:Immunology/Inflammation储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验H2O:35mg/mL(47.65mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.3615mL6.8073mL13.6145mL5mM0.2723mL1.3615mL2.7229mL10mM0.1361mL0.6807mL1.3615mL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(sealedstorage,awayfrommoisture)。-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：PBSSolubility:100mg/mL(136.15mM);Clearsolution;Needultrasonic1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性ADU-S100disodiumsalt(MIW815disodiumsalt)⼲扰素因刺激物的激活剂(STING)，具有有效的抗肿瘤和免疫活性[1]。IC50&TargetSTING[1]体外研究ADU-S100showsenhancedtypeIIFNproductionoverCDAinTHP-1humanmonocytes.Incontrast,thedithio,mixed-linkagecyclicdinucleotide(CDN)derivatives(MLRR-CDA,MLRR-S2CDG,andMLRR-S2cGAMP)potentlyactivateallfivehSTINGalleles,includingtherefractoryhSTINGREFandhSTINGQalleles.ADU-S100inducesthehighestexpressionofIFN-βandthepro-inflammatorycytokinesTNF-α,IL-6,andMCP-1onamolarequivalentbasis,ascomparedtoendogenousMLcGAMPandtheTLR3agonistpolyI:C.ADU-S100isalsofoundtoinduceaggregationofSTINGandinducephosphorylationofTBK1andIRF3inmousebonemarrowmacrophage(BMM).ADU-S100inducessignificantlyhigherlevelsofIFN-αwhencomparedtoMLcGAMP[1].体内研究ADU-S100showshigheranti-tumorcontrolthantheendogenousMLcGAMP.AdoseresponseoftheADU-S100compoundisperformedinB16tumor-bearingmice,whichidentifiesanoptimalantitumordoselevelthatalsoelicitesmaximumtumorantigen-specificCD8+Tcellresponses,andimproveslong-termsurvivalto50%[1].PROTOCOLCellAssay[1]CryopreservedhPBMCsarethawedand1×106cellsperwellareplatedina96wellplateinRPMImediasupplementedwith10%FBS,1%non-essentialaminoacids,1%penicillin/streptomycin,L-glutamine,10mMHEPESbuffer,1mMSodiumPyruvate,0.055mMβ-MEat37°Cwith5%CO2.Cellsarestimulatedwith10μMADU-S100orMLcGAMPfor6hoursandsupernatantsareharvested.Supernatantsarediluted1:2andassayedforIFN-αproteinusingCytometricBeadArray(CBA)HumanFlexSet.DataiscollectedusingaFACSVersecytometerandanalyzedbyFCAPArraySoftware[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice[1]Administration[1]WTC57BL/6miceareinoculatedwith5×104B16.F10cellsintheleftflank(n=8).Whentumorvolumesare100mm3micereceivethreeITdosesofeitherMLRR-S2CDG(25μg),ADU-S100(50μg),orHBSSascontrol.WTC57BL/6miceareinoculatedwith5×104B16.F10cellsintheleftflank(n=5).Whentumorvolumesare100mm3theyreceivedthreeITdosesofADU-S100at5,25,50or100μgorHBSSascontrol.WTC57BL/6miceareinoculatedwith5×104B16.F10cellsintheleftflank(n=8).Whentumorvolumesare100mm3theyreceivethreeITdosesof100μgADU-S100orHBSSascontrol.Treatmentsareadministeredondays13,17and20andtumormeasurementsaretakentwiceweekly.ResultsareshownaspercentsurvivalbyLog-rank(Mantel-Cox)test(AandC)[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE户使⽤本产品发表的科研⽂献•NatNanotechnol.2021Sep30.•CancerCell.2020Mar16;37(3):289-307.e9.•Neuron.2022Nov4;S0896-6273(22)00961-8.•NatCommun.2022May31;13(1):3022.•Biomaterials.2018May;163:67-75.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].CorralesL,etal.DirectActivationofSTINGintheTumorMicroenvironmentLeadstoPotentandSystemicTumorRegressionandImmunity.CellRep.2015May19;11(7):1