SCR7-pyrazine-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemESCR7pyrazineCat.No.:HY-107845CASNo.:14892-97-8分⼦式:C₁₈H₁₂N₄OS分⼦量:332.38作⽤靶点:CRISPR/Cas9;DNA/RNASynthesis;Apoptosis作⽤通路:CellCycle/DNADamage;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(300.86mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.0086mL15.0430mL30.0860mL5mM0.6017mL3.0086mL6.0172mL10mM0.3009mL1.5043mL3.0086mL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，并请注意储备液的保存⽅式和期限。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.52mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.52mM);ClearsolutionBIOLOGICALACTIVITY1/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE⽣物活性SCR7pyrazine⼀种DNA连接酶IV(DNAligaseIV)抑制剂，它以连接酶IV依赖的⽅式阻断⾮同末端连接(NHEJ)。SCR7pyrazine也⼀种CRISPR/Cas9的增强⼦，可提⾼Cas9介导的同性定向修复(HDR)的效率。SCR7pyrazine诱导细胞凋亡(apoptosis)并具有抗癌活性。IC50&TargetDNALigaseIV[1]CRISPR/Cas9[2]体外研究SCR7pyrazine(20-100μM;24hours;MCF7cells)treatmentinterfereswithNHEJincells,leadingtoaccumulationofunrepaireddouble-strandbreaks(DSBs)[1].SCR7pyrazinetreatmentshowsadose-dependentdecreaseincellproliferationwithIC50valuesof40μM,34μM,44μM,8.5μM,120μM,10μMand50μMforMCF7,A549,HeLa,T47D,A2780,HT1080andNalm6cells,respectively[1].InMCF7cells,SCR7pyrazine(20,40μM)treatmentincreasesphosphorylationofATMandactivatesp53,decreasesMDM2,BCL2,resultinginactivationofproapoptoticproteins,PUMAandBAX.AndtheshorterfragmentsofMCL1,PARP1,Caspase3,andCaspase9cleavageareupregulatedinadose-dependentmanner[1].WesternBlotAnalysis[1]CellLine:MCF7cellsConcentration:20μM,40μM,100μMIncubationTime:24hoursResult:ShowedanincreaseinlevelsofgH2AXfociandprotein.体内研究SCR7pyrazine(10mg/kg;intraperitonealinjection;sixdoses;BALB/cmice)treatmentsignificantlyreducesbreastadenocarcinoma-inducedtumorandincreaseslifespan[1].AnimalModel:BALB/cmiceinjectedwithbreastadenocarcinomacells[1]Dosage:10mg/kgAdministration:Intraperitonealinjection;onalternatedays(0,2,4,6,8,and10)Result:Significantlyreducedbreastadenocarcinoma-inducedtumorandincreasedlifespan.•EMBORep.2019Mar;20(3):e46821.•JImmunol.2020Feb19.pii:ji1900305.•JMolMed(Berl).2019Aug;97(8):1183-1193.•OncoTargetsTher.2018Aug17;11:4945-4953.Seemorecustomervalidationsonwww.MedChemE2/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].SrivastavaM,etal.Aninhibitorofnonhomologousend-joiningabrogatesdouble-strandbreakrepairandimpedescancerprogression.Cell.2012Dec21;151(7):1474-87.[2].LinC,etal.IncreasingtheEfficiencyofCRISPR/Cas9-mediatedPreciseGenomeEditingofHSV-1VirusinHumanCells.SciRep.2016Oct7;6:34531.McePdfHeightCaution:Producthasnotbeenfullyva