Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEDKM2-93Cat.No.:HY-101836CASNo.:65836-72-8分?式:C??H??ClNO?分?量:243.69作?靶點:E1/E2/E3Enzyme作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:125mg/mL(512.95mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM4.1036mL20.5179mL41.0357mL5mM0.8207mL4.1036mL8.2071mL10mM0.4104mL2.0518mL4.1036mL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?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，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)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(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:≥2.08mg/mL(8.54mM);Clearsolution1/2MasterofBioactiveMolecules—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:≥2.08mg/mL(8.54mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(8.54mM);ClearsolutionBIOLOGICALACTIVITY?物活性DKM2-93相對選擇性的UBA5抑制劑，IC50值為430μM。IC50&TargetIC50:430μM(UBA5),90μM(PaCa2cells),30μM(Panc1cells)[1]體外研究Ubiquitin-likemodifieractivatingenzyme5(UBA5)isanovelpancreaticcancertherapeutictarget.DKM2-93impairspancreaticcancercellsurvivalthroughcovalentlymodifyingthecatalyticcysteineofUBA5,therebyinhibitingitsactivityasaproteinthatactivatestheubiquitin-likeproteinUFM1toUFMylateproteins.DKM2-93inhibitsPaCa2andPanc1cellssurvivalwithIC50sof90and30μM,respectively[1].體內(nèi)研究DKM2-93dailytreatmentsignificantlyimpairstumorgrowthofPaCa2cellsinvivointumorxenograftstudiesinimmune-deficientmicewithoutcausinganyweightlossoroverttoxicity[1].PROTOCOLCellAssay[1]PaCa2andPanc1cellsaretreatedwith0-1000μMDKM2-93for48hours.CellviabilityisassessedbyHoeschtstain[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:MicearesubcutaneouslyinjectedwithPaCa2cellstoinitiatethetumorxenograftstudyandtreatmentsAdministration[1]ofmiceareinitiatedwithvehicleorDKM2-93(50mg/kgip,onceperday)threedaysafterinjectionofcancercells[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻?CellRep.2019Apr16;27(3):971-986.e9.?CellRep.2019Apr16;27(3):971-986.e9.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].RobertsAM,etal.ChemoproteomicScreeningofCovalentLigandsRevealsUBA5AsaNovelPancreaticCancerTarget.ACSChemBiol.2017Apr21;12(4):899-904.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedi