GS-444217-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGS-444217Cat.No.:HY-100844CASNo.:1262041-49-5分⼦式:C₂₃H₂₁N₇O分⼦量:411.46作⽤靶点:MAP3K;Apoptosis作⽤通路:MAPK/ERKPathway;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:15.5mg/mL(37.67mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4304mL12.1518mL24.3037mL5mM0.4861mL2.4304mL4.8607mL10mM0.2430mL1.2152mL2.4304mL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:≥2.5mg/mL(6.08mM);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:≥2.5mg/mL(6.08mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.08mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性GS-444217⼀种有效的，可⼝服的，选择性ATP竞争性凋亡信号调节激酶1(ASK1)抑制剂，IC50为2.87nM[1]。IC50&TargetASK12.87nM(IC50)体外研究TreatmentwithGS-444217reducesASK1phosphorylationandpreventsthephosphorylationofMKK3/6,MKK4,p38,andJNKatconcentrationsof0.3μMandabovewithfullsuppressionofASK1activityat1μM.GS-444217(1μM)reducesASK1activitywithin5minutesofadditiontothecultures,reachingamaximumlevelofinhibitionby30minutes.RemovalofGS-444217fromtheculturesresultsinreactivationofASK1autophosphorylationwithin10minutesandnear-completerecovery2hoursafterdrugwashout[1].体内研究GS-444217reducesoxidativestress(OS)-inducedASK1signalinginkidneyandinhibitsacuterenaltubularinjuryinrats.GS-444217(30mg/kg)inhibitsactivationofASK1,p38,andJNKinratkidney.GS-444217hasaninvivoEC50ofapproximately1.6μMforinhibitingtheASK1pathwayinrodentkidney[1].户使⽤本产品发表的科研⽂献•EMBOJ.2022Feb3;e109386.•EnvironToxicol.2022Feb15.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LilesJT,etal.ASK1contributestofibrosisanddysfunctioninmodelsofkidneydisease.JClinInvest.2018Oct1;128(10):4485-4500.[2].BudasGR,etal.ASK1InhibitionHaltsDiseaseProgressioninPreclinicalModelsofPulmonaryArterialHypertension.AmJRespirCritCareMed.2018Feb1;197(3):373-385.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplication