DGKα-IN-10-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEDGKα-IN-10Cat.No.:HY-178062CASNo.:2980579-79-9分⼦式:C₂₅H₂₅N₅O₄分⼦量:459.5作⽤靶点:DGK;InterleukinRelated作⽤通路:MetabolicEnzyme/Protease;Immunology/Inflammation储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性DGKα-IN-10⼀种具有⼝服活性的强效DGKα抑制剂，其IC50为0.27nM。DGKα-IN-10可诱导IL-2释放和T细胞增殖。DGKα-IN-10可⽤于癌症研究，如结肠癌[1]。IC50&TargetDKGαIL-20.27nM(IC50)体外研究DGKα-IN-10(Compound16)inducesIL-2releaseinhumanperipheralbloodmononuclearcells(PBMCs)withanEC50of0.29μM[1].DGKα-IN-10(12-1000nM,4h)promotesproliferationofCD4+andCD8+TcellsinhumanPBMCs[1].DGKα-IN-10(59.85-163.3nM)enhancespERKactivationinhumanTcells[1].DGKα-IN-10(1μM)exhibits≥100-foldselectivityforDGKαovermostDGKisoforms[1].CellProliferationAssay[1]CellLine:Humanperipheralbloodmononuclearcells(PBMCs)Concentration:12,37,111,333and1000nMIncubationTime:4hResult:IncreasedCD4+andCD8+Tcells.体内研究DGKα-IN-10(Compound16)(0.5-10mg/kg,p.o.,twiceaday)inhibitstumorgrowthcombinedwithanti-PD-1antibodyinMC38/CT26xenograftC57BL/6Jmice[1].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:MC38/CT26xenograftC57BL/6Jmicemodels[1]Dosage:0.5,3and10mg/kg,combinedwithanti-PD-1antibody(3-5mg/kg)Administration:Orallyadministration,twiceadayResult:Reducedtumorvolume.Showedtumorgrowthinhibition(TGI)rateof51.2%-90.3%.Hadnosignificantbodyweightloss.REFERENCES[1].LuH,etal.DiscoveryofNovel,Potent,Selective,andOrallyAvailableDGKαInhibitorsfortheTreatmentofTumors.JMedChem.2025Sep25;68(18):19645-19660.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792