BioE-1115-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBioE-1115Cat.No.:HY-129571CASNo.:1268863-35-9分?式:C??H??FN?O?分?量:339.36作?靶點:Ser/ThrProtease;CaseinKinase作?通路:MetabolicEnzyme/Protease;CellCycle/DNADamage;StemCell/Wnt儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:62.5mg/mL(184.17mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.9467mL14.7336mL29.4672mL5mM0.5893mL2.9467mL5.8934mL10mM0.2947mL1.4734mL2.9467mL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:2.08mg/mL(6.13mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.13mM);ClearsolutionBIOLOGICALACTIVITY?物活性BioE-1115?種?度選擇性和有效的PAS激酶(PASK)抑制劑，其IC50值約為4nM。BioE-1115還?種有效的酪蛋?激酶2α(caseinkinase2α)抑制劑，IC50值約為10μM。IC50&TargetCK2α10μM(IC50)體外研究InthepresenceofBioE-1115,showsadose-dependentlossofPASKphosphorylation,withanIC50of~1μMinHEK293cells[1].Attheconcentrationsabove10μM,BioE-1115treatmentshowsasignificantreductioninSREBPactivity,withoutanyobservableeffectsoncellmorphologyorgrowthrateinHepG2cells[1].體內(nèi)研究BioE-1115(1-100mg/kg;oralgavage;daily;for7days;maleSprague-Dawleyrats)treatmentshowsadose-dependentsuppressionoftheexpressionofGpat1,FasnandallotherSREBP-1ctargetgenesanalyzed.SREBP-1maturationinliverisalsosuppressedinBioE-1115treatedratsat10,30and100mg/kgdoses.Acalculatedmeasureofinsulinresistance,HOMA-IR,isdecreasedinadose-dependentmannerbyBioE-1115administration.HepaticandserumTAGaredecreasedinadose-dependentmannerbyBioE-1115administration.BioE-1115treatmentcausesasignificantdecreaseinserumglucose.BothSREBP-1candSREBP-1amRNAaremodestlydecreasedatthehighestdoses.NeitherdoseofBioE-1115causesasignificantchangeineitherliverweightorbodyweight[1].AnimalModel:MaleSprague-Dawleyrats(12weeksofage;129.4±0.63g)fedwithhighfructosediet[1]Dosage:1mg/kg,3mg/kg,10mg/kg,30mg/kgand100mg/kgAdministration:Oralgavage;daily;for7daysResult:Treatedwith10,30and100mg/kg,showedadose-dependentsuppressionoftheexpressionofGpat1,FasnandallotherSREBP-1ctargetgenesanalyzed.DecreasedhepaticexpressionoflipogenicSREBP-1ctargetgenes,decreasedserumtriglyceridesandpartiallyreversedinsulinresistance.REFERENCES[1].WuX,etal.PASkinasedriveslipogenesisthroughSREBP-1maturation.CellRep.2014Jul10;8(1):242-55.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidated