MS37452-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMS37452Cat.No.:HY-119344CASNo.:423748-02-1分⼦式:C₂₂H₂₆N₂O₅分⼦量:398.45作⽤靶点:HistoneMethyltransferase作⽤通路:Epigenetics储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(250.97mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5097mL12.5486mL25.0972mL5mM0.5019mL2.5097mL5.0195mL10mM0.2510mL1.2549mL2.5097mL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。-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:≥2.5mg/mL(6.27mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.27mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性MS37452⼀种有效的CBX7chromodomain与H3K27me3结合的抑制剂，Kd为27.7μM。MS37452可以通过置换CBX7与前列腺癌细胞中INK4A/ARF因座的结合来抑制多梳抑制复合物靶因p16/CDKN2A的转录[1]。IC50&TargetCBX7[1]体外研究MS37452(125-500μM;12hours)significantlyincreasesINK4A/ARFtranscriptlevelsupto25%and60%for250μMand500μM,respectively,ascomparedtotheDMSOcontrol[1].MS37452(250μM;2hours)treatshumanPC3prostatecancercellsfor2hoursreducingCBX7occupancyacrosstheINK4A/ARFlocus[1].MS37452(200µM;5days)combinedwithdoxorubicinresultsinconsistentlydecreasedcellviabilitycomparedtoDMSOtreatedandsingledrugtreatment[2].MS37452(200µM;5days),whichisaCBX7chromodomaininhibitor(CBX7i),incombinationwithdoxorubicinisanoveltherapeuticstrategy[2].RT-PCR[1]CellLine:PC3cellsConcentration:125-500μMIncubationTime:12hoursResult:Up-regulatedINK4A/ARFexpressionupto25%and60%for250μMand500μM,respectively.CellViabilityAssay[2]CellLine:Glioblastomamultiforme(GBM)U118MGcellsConcentration:PRT416540µM,PTC209200nM,DZnep25µM,GSK343400nM,MS37452200µM,Doxorubicin200nM,temozolomide50µM,SAHA1µMIncubationTime:5daysResult:IdentifiedseveralcombinationsthatresultedinconsistentlydecreasedcellviabilitycomparedtoDMSOtreatedandsingledrugtreatment:SAHA/TMZandMS37452/doxorubicin.REFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].RenC,etal.Small-moleculemodulatorsofmethyl-lysinebindingfortheCBX7chromodomain.ChemBiol.2015;22(2):161-168.[2].ConnellyKE,etal.CBXChromodomainInhibitionEnhancesChemotherapyResponseinGlioblastomaMultiforme.YaleJBiolMed.2016;89(4):431-440.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicala