STING-IN-8-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemESTING-IN-8Cat.No.:HY-163749分子式: C₁₈H₁₄F₃N₃O₅S₂分子量: 473.45作用靶点: STING作用通路: Immunology/Inflammation储存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性STING-IN-8(Compound15b)是一种有效的干扰素基因刺激因子(STING)抑制剂，对人的IC50值为0.121μM，小鼠的IC50值为0.033μM。STING-IN-8抑制MSA-2(HY-136927)或2’,3’-cGAMP(HY-100564)刺激STING信号传导和人、小鼠细胞中的免疫炎症细胞因子水平。STING-IN-8在STING相关炎症和自身免疫性疾病领域的研究前景广阔[1]。体外研究STING-IN-8(0.1,0.3,1,3μM,5h)restrainstheMSA-2(10μM)or2’,3’-cGAMP(10μM)-inducedp-TBK1andp-IRF3upregulationexpressioninbothhumanandmurinecells[1].STING-IN-8showsnegligiblecytotoxicitywithCC50of30μMinTHP1-DualandRAW-Luciacells[1].STING-IN-8(0.3,1,3μMand0.1,1,3μM,9h)effectivelyinhibitsSTINGdownstreamimmune-inflammatorycytokinesinbothhumanandmouseimmunecells[1].WesternBlotAnalysis[1]CellLine:HumanmonocytederivedTHP1-Dualcellline,murinemacrophagecellsandmouseembryonicfibroblastsConcentration:0.1,0.3,1,3μMIncubationTime:5hResult:Significantlydown-regulatethethelevelsofphosphorylatedTBK1andIRF3inducedbyMSA-2(10μM)and2’,3’-cGAMP(10μM)inallcelllineswithbetterpotencythanSN-011(HY-145010).RealTimeqPCR[1]1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemECellLine:THP1-DualcelllineandRAW-LuciacellsConcentration:0.3,1,3μMand0.1,1,3μMIncubationTime:9hResult:SignificantlyinhibitedtheMSA-2(10μM)or2’,3’-cGAMP(10μM)-inducedupregulationofSTINGsignalsexpressioninTHP1-DualcelllineandRAW-Luciacells.体内研究STING-IN-8(10MG/KG,i.p.)effectivelyinhibitsSTINGdownstreamcytokinesinMSA‑2(10MG/KG)‑stimulatedmice[1].STING-IN-8(10MG/KG,i.p.,dailyfortwoweeks)attenuatessustainablyhighlevelsofimmune-inflammatorycytokinesinthemicewithTrex1loss-of-function[1].1.19合并列符号：代表后面的三列被合并：结束是列是行PharmacokineticparametersofSTING-IN-8inmice[1]药代动力学分析[1]AdministrationT1/2(h)Tmax(h)Cmax(ng/mL)AUC0-∞(ng·h/mL)MRT(h)p.o.10mg/kgb1.750.2577.61092.53i.p.5mg/kgc4.860.181371004.73AnimalModel:C57BL/6miceDosage:10MG/KGAdministration:i.p.,asingledoseResult:EffectivelyreducedMSA-2(10MG/KG)-stimulatedserumIL-6,CXCL10levelsandinhibitedtheexpressionofIFNβ,TNFα,ISG15,ISG56,Cxcl10,IL6inkidneytissues[1]AnimalModel:KidneytissuesofTrex1-D18NmiceDosage:10MG/KGAdministration:i.p.dailyfortwoweeksResult:SignificantlyreducedtheISG15,ISG56,CXCL10levelsinkidneyanddemonstratedanti-inflammatoryeffectsintongueandothermuscletissuesofTrex1-D18Nmice[1]REFERENCESJinZ,etal.Design,synthesis,andevaluationofthiazolecarboxamidederivativesasstimulatorofinterferongeneinhibitors[J].MolDivers.2024Apr29,1573-501XMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedi