VARS1-IN-1-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEVARS1-IN-1Cat.No.:HY-180995CASNo.:428830-84-6分⼦式:C₂₁H₁₅N₅OS分⼦量:385.44作⽤靶点:DNA/RNASynthesis作⽤通路:CellCycle/DNADamage储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性VARS1-IN-1⼀种缬氨酰-tRNA合成酶(VARS1)抑制剂，其Kd值为0.213μM。VARS1-IN-1能抑制VARS1的tRNA氨酰化活性，降低缬氨酸tRNA的荷电⽔平，并减少总蛋⽩合成速率。VARS1-IN-1可抑制PC3前列腺癌异种移植模型中侵袭性肿瘤的⽣长和细胞增殖。VARS1-IN-1可⽤于前列腺癌研究[1]。体外研究VARS1-IN-1(Compound2701)(10µM;2days)interfersVARS1’stRNAaminoacylationactivitybutnotitsexpressionwithareductioninchargedtototaltRNA-Valratioinprostatecancercells[1].VARS1-IN-1(10µM;2days)reduestotalproteinsynthesisrateinPC3cells[1].体内研究VARS1-IN-1(Compound2701)(15mg/kg;i.p.;onceeveryotherdayfor20days)suppressestumorgrowthandcellproliferationinmaleBALB/c-nunudemicePC3prostatecancerxenograft[1].AnimalModel:BALB/c-nunudemicewithPC3xenograft(male,6-7weeksold)[1]Dosage:15mg/kgAdministration:i.p.;onceeveryotherdayfor20daysResult:InhibitedtumorgrowthwithsignificantreductionintumorweightcomparedtoDMSOcontrol.DecreasedcellproliferationindexasshownbyKi-67immunohistochemicalstaining.REFERENCES1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].HeQ,etal.VARS1fuelsprostatecancerevolutionviacodon-selectivetranslationalrewiring[J].bioRxiv,2025:2025.12.09.693333.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792/p>