GSK591-EPZ015866-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGSK591Cat.No.:HY-100235CASNo.:1616391-87-7Synonyms:EPZ015866;GSK3203591分?式:C??H??N?O?分?量:380.48作?靶點:HistoneMethyltransferase作?通路:Epigenetics儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(262.83mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.6283mL13.1413mL26.2826mL5mM0.5257mL2.6283mL5.2565mL10mM0.2628mL1.3141mL2.6283mL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，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?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：(為保證實驗結(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)實驗的?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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.25mg/mL(5.91mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.25mg/mL(5.91mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.25mg/mL(5.91mM);ClearsolutionBIOLOGICALACTIVITY?物活性GSK591(EPZ015866)?種有效的，選擇性的proteinmethyltransferase5(PRMT5)抑制劑，其IC50值為4nM。IC50&TargetIC50:4nM(PRMT5)[1]體外研究GSK591(5μM;MCF7,T47D,andMCF10Acells)treatmentsuppressesbreastcancerstemcells(BCSCs)proliferationandself-renewal.GSK591reducesBCSCsnumbersinvitro[2].CellProliferationAssay[2]CellLine:MCF7,T47D,andMCF10AcellsConcentration:5μMIncubationTime:Result:SuppressedBCSCsproliferationandself-renewal.戶使?本產(chǎn)品發(fā)表的科研?獻?NatCommun.2019Aug21;10(1):3761.?ProcNatlAcadSciUSA.2019Feb19;116(8):2961-2966.?Theranostics.2021Jan27;11(8):3742-3759.?JBiolChem.2022Aug27;102434.?ExpCellRes.2022Nov16;422(1):113413.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].[1]KennethW.Duncanetal.StructureandPropertyGuidedDesignintheIdentificationofPRMT5ToolCompoundEPZ015666.ACSMed.Chem.Lett.,2016,7(2),pp162-166.[2].ChiangK,etal.PRMT5IsaCriticalRegulatorofBreastCancerStemCellFunctionviaHistoneMethylationandFOXP1Expression.CellRep.2017Dec19;21(12):3498-3513.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forres