R-R-VVD-118313-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE(R,R)-VVD-118313Cat.No.:HY-151385ACASNo.:2875046-31-2分⼦式:C₁₉H₂₂Cl₂N₂O₃S分⼦量:429.36作⽤靶点:STAT;InterleukinRelated;IFNAR;JAK作⽤通路:JAK/STATSignaling;StemCell/Wnt;Immunology/Inflammation;Epigenetics;ProteinTyrosineKinase/RTK储存⽅式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(232.90mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3290mL11.6452mL23.2905mL5mM0.4658mL2.3290mL4.6581mL10mM0.2329mL1.1645mL2.3290mL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。BIOLOGICALACTIVITY⽣物活性(R,R)-VVD-118313VVD-118313(HY-151385)的异构体。VVD-118313⼀种选择性JAK1抑制剂，可阻断JAK1依赖的反式磷酸化和细胞因⼦信号。VVD-118313可⽤于癌症的研究。IC50&TargetJAK11/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体外研究VVD-118313(compound5a;0.01-10ꢀμM;3h;primaryhumanPBMCs)inhibitsJAK1byengagementofC817andJAK2byengagementofC838.VVD-118313inhibitscysteinereactivityinadose-dependentmanner[1].VVD-118313(2µM,2h)blocksIFNα-simulatedSTAT1andIL-6-stimulatedSTAT3phosphorylationinWT-orC810A-JAK1-expressing22Rv1cells.VVD-118313alsoblockstheconstitutivephosphorylationofWT-andC810A-JAK1[1].VVD-118313(0.01-10ꢀμM)selectivelyinhibitsJAK1signalinginprimaryhumanimmunecells.VVD-118313inhibitsJAK1-dependentIFNα-pSTAT1,IL-6-pSTAT3,andIL-2-pSTAT5pathwaysinhumanPBMCsinadose-dependentmanner[1].VVD-118313(0.1-0.4μM;24h)inhibitsT-cellactivationinduction.VVD-118313inhibitstheactivationofhumanTcellsco-stimulatedwithαCD3/αCD28byareductionintheproportionofCD25+Tcells.VVD-118313blocksthesecretionoftheTh1-polarizingcytokineIFNγandincreasestheproductionofIL-2[1].VVD-118313(0.1-0.5ꢀμM;2h)inhibitsontheproductionofpro-inflammatorycytokinesandchemokines.VVD-118313suppressestheinductionofseveralpro-inflammatorychemokines,includingCCL2/MCP-1,CXCL10/IP-10,andCCL4/MIP-1β[1].WesternBlotAnalysis[1]CellLine:22Rv1cellsConcentration:0.01,0.1,and1μMIncubationTime:2hoursResult:ShowedlabelingofrecombinantWT-JAK1andC810A-JAK1,butnotC817A-JAK1.InhibitedWT-andC810A-JAK1phosphorylationwithevengreaterpotencythanSTAT1/STAT3phosphorylation.体内研究VVD-118313(compound5a;25-50mg/kg;i.h.;once)inhibitsJAK1signalinginTYK2knockoutmice[1].REFERENCES[1].KavanaghME,et,al.SelectiveinhibitorsofJAK1targetinganisoform-restrictedallostericcysteine.NatChemBiol.2022Sep12.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplica