UKI-1-UKI-1C-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEUKI-1Cat.No.:HY-100415CASNo.:220355-63-5Synonyms:UKI-1C分⼦式:C₃₂H₄₇N₅O₅S分⼦量:613.81作⽤靶点:PAI-1;Ser/ThrProtease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:100mg/mL(162.92mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.6292mL8.1458mL16.2917mL5mM0.3258mL1.6292mL3.2583mL10mM0.1629mL0.8146mL1.6292mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(4.07mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.07mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.07mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性UKI-1(UKI-1C)⼀种有效的尿激酶型纤溶酶原激活剂(uPA)抑制剂，Ki为0.41μM。UKI-1还⼀种低分⼦量的丝氨酸蛋⽩酶(serineprotease)抑制剂。UKI-1有效的抗转移剂，可抑制癌细胞的侵袭能⼒。IC50&TargetKi:0.41μM(Urokinase-typeplasminogenactivator(uPA))[2]Serineprotease[1]体外研究UKI-1(WX-UK1;0.1-1.0μg/mL)treatmentshowsadecreaseoftumorcellinvasionbyupto50%isachievedinbothmodelswiththeSCCHNlineFaDuandthecervicalcarcinomalineHeLa[1].UKI-1(WX-UK1)interfereswiththeplasminogenactivationsystemat2levels:itinhibitsplasminformationdirectlyandviainhibitionofuPA.InvitroinvasionmodelswithhighlyinvasivefibrosarcomaandbreastcancercellsshowedthatUKI-1effectivelyinhibitsmigrationofthecellsthroughfibrinmatrices[1].体内研究UKI-1(WX-UK1)treatmenthasantimetastaticactivitiesthatsignificantlyreducesthenumberofmetastaticlesionsandtumorgrowthinmetastasizingratpancreaticandmammaryadenocarcinomatumormodels[1].REFERENCES[1].ErtongurSetal.InhibitionoftheinvasioncapacityofcarcinomacellsbyWX-UK1,anovelsyntheticinhibitoroftheurokinase-typeplasminogenactivatorsystem.IntJCancer.2004Jul20;110(6):815-24.[2].EwaZeslawskaetal.Crystalsoftheurokinasetypeplasminogenactivatorvariantβc-uPAincomplexwithsmallmoleculeinhibitorsopenthewaytowardsstructure-baseddrugdesign.JMolBiol.2000Aug11;301(2):465-75.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplication