MS37452-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMS37452Cat.No.:HY-119344CASNo.:423748-02-1分?式:C??H??N?O?分?量:398.45作?靶點(diǎn):HistoneMethyltransferase作?通路:Epigenetics儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(250.97mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.5097mL12.5486mL25.0972mL5mM0.5019mL2.5097mL5.0195mL10mM0.2510mL1.2549mL2.5097mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.27mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.27mM);ClearsolutionBIOLOGICALACTIVITY?物活性MS37452?種有效的CBX7chromodomain與H3K27me3結(jié)合的抑制劑，Kd為27.7μM。MS37452可以通過置換CBX7與前列腺癌細(xì)胞中INK4A/ARF因座的結(jié)合來抑制多梳抑制復(fù)合物靶因p16/CDKN2A的轉(zhuǎn)錄[1]。IC50&TargetCBX7[1]體外研究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?邊的抑制劑?師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