DMX-5804-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEDMX-5804Cat.No.:HY-111754CASNo.:2306178-56-1分⼦式:C₂₁H₁₉N₃O₃分⼦量:361.39作⽤靶点:MAP4K作⽤通路:MAPK/ERKPathway储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(345.89mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7671mL13.8355mL27.6709mL5mM0.5534mL2.7671mL5.5342mL10mM0.2767mL1.3835mL2.7671mL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(5.76mM);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(5.76mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.76mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性DMX-5804⼀种有效、可⼝服、选择性的MAP4K4抑制剂，对⼈MAP4K4的IC50值为3nM，pIC50值为8.55；对MINK1/MAP4K6(pIC50，8.18)和TNIK/MAP4K7(pIC50，7.96)的作⽤相对较弱。DMX-5804能够增强⼼肌细胞存活率，减少⼩⿏的缺⾎再灌注损伤[1]。IC50&TargetMAP4K4MAP4K4MINK1/MAP4K6TNIK/MAP4K73nM(IC50)8.55(pIC50)8.18(pIC50)7.96(pIC50)GCK/MAP4K2KHS/MAP4K5GLK/MAP4K3MLK1/MAP3K96.50(pIC50)6.36(pIC50)4.95(pIC50)7.19(pIC50)MLK3/MAP3K11NUAKVEGFRABL16.99(pIC50)6.88(pIC50)5.72(pIC50)5.80(pIC50)AuroraBFLT3GSK3β5.49(pIC50)5.31(pIC50)4.66(pIC50)体外研究DMX-5804exhibitsgreatselectivityatMAP4K4overotherkinases,suchasGCK/MAP4K2(pIC50,6.50),GLK/MAP4K3(pIC50,4.95),KHS/MAP4K5(pIC50,6.36),ABL1(pIC50,5.80),AuroraB(pIC50,5.49),FLT3(pIC50,5.31),GSK3β(pIC50,4.66),MLK1/MAP3K9(pIC50,7.19),MLK3/MAP3K11(pIC50,6.99),NUAK(pIC50,6.88)andVEGFR(pIC50,5.72)[1].REFERENCES[1].FiedlerLR,etal.MAP4K4InhibitionPromotesSurvivalofHumanStemCell-DerivedCardiomyocytesandReducesInfarctSizeInVivo.CellStemCell.2019Mar1.pii:S1934-5909(19)30013-X.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuse