AT6-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAT6Cat.No.:HY-112375CASNo.:2098836-50-9分⼦式:C₄₈H₅₈ClN₉O₇S₃分⼦量:1004.68作⽤靶点:PROTACs作⽤通路:PROTAC储存⽅式:-20°C,protectfromlight,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedundernitrogen)溶解性数据体外实验DMSO:100mg/mL(99.53mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM0.9953mL4.9767mL9.9534mL5mM0.1991mL0.9953mL1.9907mL10mM0.0995mL0.4977mL0.9953mL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(protectfromlight,storedundernitrogen)。-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:≥5mg/mL(4.98mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(4.98mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥5mg/mL(4.98mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性AT6⼀种PROTACAT1类似物，PROTACAT1由vonHippel-Lindau配体和BRD4配体相连，⼀种⾼度选择性的溴结构域蛋⽩(Brd4)降解剂。体外研究PROTACs(proteolysis-targetingchimaeras)arebifunctionalmoleculesthatrecruitatargetproteininproximitytoanE3ubiquitinligasetotriggerproteindegradation.Structuralelucidationofthekeyternaryligase:PROTAC:targetspeciesandhowthisimpactstargetdegradationselectivityremainselusive.Theligandfoldsintoitselftoallowformationofspecificintermolecularinteractionsintheternarycomplex.Isothermaltitrationcalorimetrystudies,supportedbysurfacemutagenesisandproximityassays,areconsistentwithpronouncedcooperativeformationofternarycomplexeswithBrd4BD2.Structure-based-designedcompoundAT1exhibitshighlyselectivedepletionofBrd4incells[1].REFERENCES[1].GaddMS,etal.StructuralbasisofPROTACcooperativerecognitionforselectiveproteindegradation.NatChemBiol.2017May;13(5):514-521.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuse