Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGS-444217Cat.No.:HY-100844CASNo.:1262041-49-5分?式:C??H??N?O分?量:411.46作?靶點:MAP3K;Apoptosis作?通路:MAPK/ERKPathway;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:15.5mg/mL(37.67mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4304mL12.1518mL24.3037mL5mM0.4861mL2.4304mL4.8607mL10mM0.2430mL1.2152mL2.4304mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；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沉淀、析出現象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.08mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.08mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.08mM);ClearsolutionBIOLOGICALACTIVITY?物活性GS-444217?種有效的，可?服的，選擇性ATP競爭性凋亡信號調節激酶1(ASK1)抑制劑，IC50為2.87nM[1]。IC50&TargetASK12.87nM(IC50)體外研究TreatmentwithGS-444217reducesASK1phosphorylationandpreventsthephosphorylationofMKK3/6,MKK4,p38,andJNKatconcentrationsof0.3μMandabovewithfullsuppressionofASK1activityat1μM.GS-444217(1μM)reducesASK1activitywithin5minutesofadditiontothecultures,reachingamaximumlevelofinhibitionby30minutes.RemovalofGS-444217fromtheculturesresultsinreactivationofASK1autophosphorylationwithin10minutesandnear-completerecovery2hoursafterdrugwashout[1].體內研究GS-444217reducesoxidativestress(OS)-inducedASK1signalinginkidneyandinhibitsacuterenaltubularinjuryinrats.GS-444217(30mg/kg)inhibitsactivationofASK1,p38,andJNKinratkidney.GS-444217hasaninvivoEC50ofapproximately1.6μMforinhibitingtheASK1pathwayinrodentkidney[1].戶使?本產品發表的科研?獻?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