BI8626-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBI8626Cat.No.:HY-120204CASNo.:1875036-75-1分⼦式:C₂₅H₂₈N₈分⼦量:440.54作⽤靶点:E1/E2/E3Enzyme作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:83.33mg/mL(189.15mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2699mL11.3497mL22.6994mL5mM0.4540mL2.2699mL4.5399mL10mM0.2270mL1.1350mL2.2699mL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:≥2.08mg/mL(4.72mM);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%cornoilSolubility:≥2.08mg/mL(4.72mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性BI8626⼀种泛素连接酶HUWE1特异性拮抗剂，IC50为0.9μM[1]。IC50&TargetIC50:0.9μM(HUWE1)[1]体外研究BI8626inducesHUWE1ectopicallyexpressestoabolisheubiquitinationofMCL1inHeLacells[1].BI8626suppressescolonyformationofLs174TcellswithestimatedIC50valueof0.7μM,andBI8622(1-4days)treatmentretardspassageofLs174Tcellsthroughallphasesofthecellcycle,withtheeffectbeingstrongestforG1[1].BI8626(0-50μM;0-6hours)retardsthedegradationofMCL1inresponsetoUVirradiationtothesameextentasdepletionofHUWE1inU2OScells[1].CellCycleAnalysis[1]CellLine:Ls174TcellsConcentration:0μM,5μM,10μM,15μM,20μMIncubationTime:0-4daysResult:RetardedpassageofLs174Tcellsthroughallphasesofthecellcycle,withtheeffectbeingstrongestforG1.WesternBlotAnalysis[1]CellLine:U2OScellsConcentration:0μM,20μM,50μMIncubationTime:0hour,1hour,2hours,4hours,6hoursResult:RetardedthedegradationofMCL1inresponsetoUVirradiationinHeLacellsbyinhibitingHUWE1inU2OScells.REFERENCES[1].PeterS,etal.Tumorcell-specificinhibitionofMYCfunctionusingsmallmoleculeinhibitorsoftheHUWE1ubiquitinligase.EMBOMolMed.2014Dec;6(12):1525-41.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch