DKM-2-93-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEDKM2-93Cat.No.:HY-101836CASNo.:65836-72-8分⼦式:C₁₁H₁₄ClNO₃分⼦量:243.69作⽤靶点:E1/E2/E3Enzyme作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(512.95mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM4.1036mL20.5179mL41.0357mL5mM0.8207mL4.1036mL8.2071mL10mM0.4104mL2.0518mL4.1036mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(8.54mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(8.54mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(8.54mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性DKM2-93相对选择性的UBA5抑制剂，IC50值为430μM。IC50&TargetIC50:430μM(UBA5),90μM(PaCa2cells),30μM(Panc1cells)[1]体外研究Ubiquitin-likemodifieractivatingenzyme5(UBA5)isanovelpancreaticcancertherapeutictarget.DKM2-93impairspancreaticcancercellsurvivalthroughcovalentlymodifyingthecatalyticcysteineofUBA5,therebyinhibitingitsactivityasaproteinthatactivatestheubiquitin-likeproteinUFM1toUFMylateproteins.DKM2-93inhibitsPaCa2andPanc1cellssurvivalwithIC50sof90and30μM,respectively[1].体内研究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.户使⽤本产品发表的科研⽂献•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—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedformedi