KCC-07-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEKCC-07Cat.No.:HY-131031CASNo.:315702-75-1分⼦式:C₁₄H₁₁N₃OS分⼦量:269.32作⽤靶点:DNAAlkylator/Crosslinker作⽤通路:CellCycle/DNADamage储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:125mg/mL(464.13mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.7131mL18.5653mL37.1306mL5mM0.7426mL3.7131mL7.4261mL10mM0.3713mL1.8565mL3.7131mL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(protectfromlight)。-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。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。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(7.72mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(7.72mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(7.72mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性KCC-07⼀种有效的，选择性的且可透过⾎脑屏障的MBD2(methyl-CpG-bindingdomainprotein2)抑制剂。KCC-07防⽌MBD2与甲化DNA结合，并激活脑特异性⾎管⽣成抑制剂1(BAI1)诱导抗增殖BAI1/p53/p21信号传导。抗癌活性。IC50&TargetMBD2(methyl-CpG-bindingdomainprotein2)[1]体外研究KCC-07(10μM;72hours;MBcells)treatmentclearlyinhibitedMBcellgrowthinvitro,consistentwithinductionofanti-proliferativeBAI1/p53/p21signaling[1].KCC-07(10μM;48hours;MBcells)treatmentlargelyabrogatesMBD2bindingtotheADGRB1promoterandrestoresBAI1mRNAandproteinexpressioninBAI1-silentMBcells[1].CellViabilityAssay[1]CellLine:Medulloblastomas(MB)cellsConcentration:10μMIncubationTime:72hoursResult:ClearlyinhibitedMBcellgrowthinvitro.WesternBlotAnalysis[1]CellLine:Medulloblastomas(MB)cellsConcentration:10μMIncubationTime:48hoursResult:LargelyabrogatedMBD2bindingtotheADGRB1promoterinBAI1-silentMBcells.体内研究KCC-07(100mg/kg;intraperitonealinjection;5days/week;athymicnudemice)treatmentinhibitstumorgrowthandsignificantlyextendsthesurvivalofMBxenograftsinvivo[1].AnimalModel:Outbredathymicnudemice(females;8-10weeksold)injectedwithMBcells[1]Dosage:100mg/kgAdministration:Intraperitonealinjection;5days/weekResult:SignificantlyextendedthesurvivalofMBxenograftsinvivo.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].DanZhu,etal.BAI1SuppressesMedulloblastomaFormationbyProtectingp53FromMdm2-MediatedDegradation.CancerCell.2018Jun11;33(6):1004-1016.e5.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicala