Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemE1G244Cat.No.:HY-116304CASNo.:847928-32-9分?式:C??H??F?N?O?分?量:504.57作?靶點:DipeptidylPeptidase;Apoptosis作?通路:MetabolicEnzyme/Protease;Apoptosis儲存?式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性數據體外實驗DMSO:250mg/mL(495.47mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.9819mL9.9094mL19.8189mL5mM0.3964mL1.9819mL3.9638mL10mM0.1982mL0.9909mL1.9819mL請根據產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，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoistureandlight)。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?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：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；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沉淀、析出現象，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:≥2.08mg/mL(4.12mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.12mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性1G244?種有效的DPP8/9抑制劑，IC50分別為12nM和84nM，但不抑制DPPIV和DPPII。1G244可誘導多發性?髓瘤細胞凋亡，并具有抗?髓瘤作?。IC50&TargetIC50:12nM(DPP8),84nM(DPP9)[2]體外研究1G244(0-100μM;72hours;Delta47,U266,KMS-5,RPMI8226,orMM.1?Scells)treatmentdose-dependentlydecreasesviablecellnumberoffivemultiplemyelomacelllines[1].1G244(50μM;0-48hours;MM.1?Scells)treatmentinducesapoptosis,ascleavedformsofbothcaspase-3andPARParedetected[1].CellViabilityAssay[1]CellLine:Delta47,U266,KMS-5,RPMI8226,orMM.1?ScellsConcentration:0μM,1μM,5μM,10μM,50μM,or100μMIncubationTime:72hoursResult:Dose-dependentlydecreasedviablecellnumberoffivemultiplemyelomacelllines.WesternBlotAnalysis[1]CellLine:MM.1?ScellsConcentration:50μMIncubationTime:0hour,3hours,6hours,12hours,24hours,48hoursResult:Decreasedcaspase-3andPARPprotein.體內研究1G244(30mg/kg;subcutaneousinjection;once-a-week;for3weeks;NOGfemalemice)treatmentapparentlysuppressesthesubcutaneousgrowthofMM.1?Scellsinmurinexenograftmodel[1].AnimalModel:NOD/Shi-scidIL-2Rγnull(NOG)femalemice(6-7weeks;19-21?g)injectedwithMM.1?Scells[1]Dosage:30mg/kgAdministration:Subcutaneousinjection;once-a-week;for3weeksResult:ApparentlysuppressedthesubcutaneousgrowthofMM.1?Scellsinmurinexenograftmodel.戶使?本產品發表的科研?獻2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?NatChemBiol.2022Nov10.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SatoT,etal.DPP8isanoveltherapeutictargetformultiplemyeloma.SciRep.2019Dec2;9(1):18094.[2].LeenHeirbaut,etal.Probingforimprovedselectivitywithdipeptidederivedinhibitorsofdipeptidylpeptidases8and9:theimpactofP1-variation.MedChemComm.2016,7.McePdfHeightCaution:Producthasnotbeenfullyvalidated