UKI-1-UKI-1C-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEUKI-1Cat.No.:HY-100415CASNo.:220355-63-5Synonyms:UKI-1C分?式:C??H??N?O?S分?量:613.81作?靶點(diǎn):PAI-1;Ser/ThrProtease作?通路:MetabolicEnzyme/Protease儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(162.92mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.6292mL8.1458mL16.2917mL5mM0.3258mL1.6292mL3.2583mL10mM0.1629mL0.8146mL1.6292mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(4.07mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.07mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.07mM);ClearsolutionBIOLOGICALACTIVITY?物活性UKI-1(UKI-1C)?種有效的尿激酶型纖溶酶原激活劑(uPA)抑制劑，Ki為0.41μM。UKI-1還?種低分?量的絲氨酸蛋?酶(serineprotease)抑制劑。UKI-1有效的抗轉(zhuǎn)移劑，可抑制癌細(xì)胞的侵襲能?。IC50&TargetKi:0.41μM(Urokinase-typeplasminogenactivator(uPA))[2]Serineprotease[1]體外研究UKI-1(WX-UK1;0.1-1.0μg/mL)treatmentshowsadecreaseoftumorcellinvasionbyupto50%isachievedinbothmodelswiththeSCCHNlineFaDuandthecervicalcarcinomalineHeLa[1].UKI-1(WX-UK1)interfereswiththeplasminogenactivationsystemat2levels:itinhibitsplasminformationdirectlyandviainhibitionofuPA.InvitroinvasionmodelswithhighlyinvasivefibrosarcomaandbreastcancercellsshowedthatUKI-1effectivelyinhibitsmigrationofthecellsthroughfibrinmatrices[1].體內(nèi)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