Glutaminase-C-IN-3-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGlutaminaseC-IN-3Cat.No.:HY-180241分⼦式:C₃₁H₃₁F₃N₆O₅S分⼦量:656.68作⽤靶点:Glutaminase;ReactiveOxygenSpecies(ROS)作⽤通路:MetabolicEnzyme/Protease;Immunology/Inflammation;NF-κB储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性GlutaminaseC-IN-3⼀种强效的⾕氨酰胺酶C(GAC)变构抑制剂，EC50值为116nM。GlutaminaseC-IN-3通过阻断⾕氨酰胺代谢来调节细胞代谢物并增加活性氧(ROS)的产⽣。在A549异种移植⼩⿏模型中，GlutaminaseC-IN-3表现出显著的抗肿瘤活性。GlutaminaseC-IN-3可⽤于⾮⼩细胞肺癌(NSCLC)的研究[1]。IC50&TargetGAC116nM(EC50)体外研究GlutaminaseC-IN-3(compound16)(72h)demonstratespotentantiproliferativeactivityinA549cells(IC50=2.45nM),whileshowingselectivityovernormalcells(BEAS-2B)withanIC50of1.12µM[1].GlutaminaseC-IN-3(30-300nM,16h)significantlydisruptsglutaminemetabolism,leadingtoaconcentration-dependentreductionintheglutamate/glutamineratioinA549cells[1].GlutaminaseC-IN-3(300nM-1µM,16h)inducesadose-dependentincreaseinROSlevelsinA549cells,indicatingenhancedROSgenerationandalossofredoxhomeostasis[1].GlutaminaseC-IN-3(5μM,1h)demonstrateshighstabilityinsimulatedgastricfluid(SGF)andsimulatedintestinalfluid(SIF)[1].GlutaminaseC-IN-3(5µM,0.25-2h)exhibitsmoderatemetabolicstabilityinratlivermicrosomes[1].体内研究GlutaminaseC-IN-3(compound16)(10and30mg/kg,i.p.,dailyfor22days)exhibitsantitumorefficacyinanA549xenograftmousemodelwithgoodsafety[1].AnimalModel:MaleBalb/cnudemiceinoculatedwithA549tumorfragments[1]1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEDosage:10and30mg/kgAdministration:i.p.,oncedailyfor22daysResult:ShowedtumorgrowthinhibitionwithaTGIof25.8%at10mg/kg.Didnotsignificantlyenhanceefficacyat30mg/kg.Showednosignificantbodyweightdecrease.REFERENCES[1].SunH,etal.Structure-enableddiscoveryofcarboxylateestersprodrugsaspotentialpotentinhibitorstargetingGlutaminaseC.BioorgChem.PublishedonlineNovember24,2025.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.