GSK3-IN-3-DataSheet-生命科學試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGSK3-IN-3Cat.No.:HY-153089CASNo.:331963-27-0分?式:C??H??N?O?分?量:429.55作?靶點:GSK-3;Mitophagy作?通路:PI3K/Akt/mTOR;StemCell/Wnt;Autophagy儲存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:4.17mg/mL(9.71mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.3280mL11.6401mL23.2802mL5mM0.4656mL2.3280mL4.6560mL10mM---------請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)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(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。BIOLOGICALACTIVITY?物活性GSK3-IN-3?種線粒體?噬(mitophagy)誘導劑，可誘導帕?依賴性線粒體?噬。GSK3-IN-3也?種GSK-3抑制劑，IC50值為3.01μM。GSK3-IN-3具有?ATP和?底物競爭性，對6-OHDA有神經(jīng)保護作?。IC50&TargetIC50:3.01μM(GSK-3)[3]體外研究GSK3-IN-3(VP07)(25μM;24h)inducesmitophagyinParkin-expressingU2OS-iMLScellswithrestricted1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEpotency[1].GSK3-IN-3(1.56-25μM;24h)resultsinmitochondriafissionwithmitochondrialmorphologychangeinU2OS-iMLS-Parkincells[1].GSK3-IN-3(VP0.7)(5μM,10μM;)showsneuroprotectionagainst6-OHDAalbeitinaParkinson'sdiseaseinvitrocellularmodelinSH-SY5Ycells[2].Immunofluorescence[1]CellLine:Parkin-expressingU2OS-iMLScellsConcentration:1.56μM,3.12μM,6.25μM,12.5μM,and25μM;IncubationTime:24hoursResult:Inducedamitochondrialmorphologychangefromafilament-shapednetworktoamoreround-shapednetwork.CellViabilityAssay[2]CellLine:SH-SY5YcellsConcentration:0.5μM,1μM,3μM,5μM,and10μMIncubationTime:16hours;with35μM6-OHDAResult:InhibitedcellgrowthwithanIC50valueof2.57μM.REFERENCES[1].MaestroI,etal.PhenotypicAssayLeadstoDiscoveryofMitophagyInducerswithTherapeuticPotentialforParkinson'sDisease.ACSChemNeurosci.2021Dec15;12(24):4512-4523.[2].Morales-GarcíaJA,etal.Glycogensynthasekinase-3inhibitorsaspotenttherapeuticagentsforthetreatmentofParkinsondisease.ACSChemNeurosci.2013Feb20;4(2):350-60.[3].PalomoV,etal.Exploringthebindingsitesofglycogensynthasekinase3.Identificationandcharacterizationofallostericmodulationcavities.JMedChem.2011Dec22;54(24):8461-70.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch