Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEA-196Cat.No.:HY-100201CASNo.:1982372-88-2分?式:C??H??Cl?N?分?量:359.25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:≥31mg/mL(86.29mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.7836mL13.9179mL27.8358mL5mM0.5567mL2.7836mL5.5672mL10mM0.2784mL1.3918mL2.7836mL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:≥1mg/mL(2.78mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:1mg/mL(2.78mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥1mg/mL(2.78mM);ClearsolutionBIOLOGICALACTIVITY?物活性A-196?種有效的選擇性的SUV420H1和SUV420H2抑制劑，其IC50值分別為25nM和144nM。A-196以底物競爭性?式抑制SUV4-20，也?種SUV4-20的化學(xué)探針，?于研究組蛋?甲轉(zhuǎn)移酶在因組完整性中的作?。IC50&TargetIC50:25nM(SUV420H1)and144nM(SUV420H2)[1].體外研究A-196(0-5μM;48hours;U2OScells)treatmentresultsinanincreaseinH4K20me1(EC50valueof735nM)andadecreaseinbothH4K20me2andH4K20me3(EC50valuesof262and370nM,respectively)[1].A-196(10μM;72hours;Wild-type,Suv4-20hdoubleknockoutandinhibitortreatedmouseembryonicfibroblastcells)inhibitsbothSUV4-20enzymesincellsinmultipletissuetypeswithoutoverttoxicity[1].WesternBlotAnalysis[1]CellLine:U2OScellsConcentration:0μM,0.075μM,0.15μM,0.3μM,0.6μM,1.25μM,2.5μM,5μMIncubationTime:48hoursResult:IncreasedinH4K20me1anddecreasedinbothH4K20me2andH4K20me3.戶使?本產(chǎn)品發(fā)表的科研?獻?PLoSPathog.2020Mar24;16(3):e1008429.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BrombergKD,etal.TheSUV4-20inhibitorA-196verifiesaroleforepigeneticsingenomicintegrity.NatChemBiol.2017Mar;13(3):317-324.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearc