FMK-9a-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEFMK9aCat.No.:HY-100522CASNo.:1955550-51-2分⼦式:C₂₃H₂₁FN₂O₃分⼦量:392.42作⽤靶点:Autophagy作⽤通路:Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(254.83mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5483mL12.7414mL25.4829mL5mM0.5097mL2.5483mL5.0966mL10mM0.2548mL1.2741mL2.5483mL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(6.37mM);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(6.37mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.37mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性FMK9aautophagin-1的抑制剂，在FRET和LRA试验中测定的IC50值分别为80和73nM。IC50&TargetIC50:80nM(autophagin-1,FRETassay);73nM(autophagin-1,LRAassay)[1]体外研究ATG4Borautophagin-1isacysteineproteasethatcleavesATG8familyproteins.ATG4Bplaysessentialrolesintheautophagosomeformationandtheautophagypathway.FMK9ashowsstronginhibitionofATG4B,withIC50valuesof80and73nMintheTR-FRETandcellular-basedLRAassays,respectively.LC−MS/MSstudyindicatesthatFMK9aformsanirreversiblecovalentbondwiththemorereactivethiolgroupofCys74locatedatthecatalyticsiteofATG4BandthusinactivatesATG4Bproteolyticactivity[1].体内研究FMK9ashowsmoderatesolubility(LYSA:41μg/mL)andhighhumanandmouselivermicrosomeclearancesof13.9and70mL/kgperminute[1].PROTOCOLKinaseAssay[1]FMK9aisdissolvedinDMSO.5μLofserial-dilutedFMK9a(1%DMSO)inassaybufferisaddedinto5μLofpurifiedATG4B(final0.1nM)in384-wellplate,andthesolutionisincubatedatroomtemperature(rt)for30min.Then,5μLofHis-GATE-16-GST(final20nM)isaddedintothewells,andthesolutionisincubatedforanother30min.5μLofdetectionsolution(final2nMofEu-anti-Hisand20nMofUlight-anti-GST)isadded,andtheresultingmixtureisincubatedatrtfor40min[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•Autophagy.2022Mar8;1-18.•ResearchSquarePreprint.2021Jul.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].QiuZ,etal.DiscoveryofFluoromethylketone-BasedPeptidomimeticsasCovalentATG4B(Autophagin-1)Inhibitors.ACSMedChemLett.2016Jun25;7(8):802-6.McePdfHeight2/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedform