Z-4EGI-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE(Z)-4EGI-1Cat.No.:HY-19831ACASNo.:901787-88-0分⼦式:C₁₈H₁₂Cl₂N₄O₄S分⼦量:451.28作⽤靶点:EukaryoticInitiationFactor(eIF)作⽤通路:CellCycle/DNADamage储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(110.80mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2159mL11.0796mL22.1592mL5mM0.4432mL2.2159mL4.4318mL10mM0.2216mL1.1080mL2.2159mL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(5.54mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性(Z)-4EGI-14EGI-1的Z-型异构体，eIF4E/eIF4G相互作⽤和翻译起始的抑制剂。(Z)-4EGI-1有效结合eIF4E，IC50为43.5μM，Kd值为8.74μM。(Z)-4EGI-1具有抗癌活性。IC50&TargeteIF4体外研究(Z)-4EGI-1(15-30µM;6hours;CRL-2813melanomacells)treatmentmarkedlyreducestheexpressionsoftheregulatoryproteins:cyclinD1,cyclinE,andSurvivin,whiletheexpressionsofhousekeepingproteinssuchasβ-Actinandα-Tubulinarenotaffected[1].(Z)-4EGI-1inhibitscancercellsproliferationwithIC50valuesof15.3μMand11.6μMforCRL-2351breastcellsandCRL-2813melanomacells,respectively[2].WesternBlotAnalysis[1]CellLine:CRL-2813melanomacellsConcentration:15µM,30µMIncubationTime:6hoursResult:Markedlyreducedtheexpressionsoftheregulatoryproteins:cyclinD1,cyclinE,andSurvivin.REFERENCES[1].KhuloudTakrouri,etal.Structure-activityRelationshipStudyof4EGI-1,SmallMoleculeeIF4E/eIF4GProtein-ProteinInteractionInhibitors.EurJMedChem.2014Apr22;77:361-77.[2].PoornachandranMahalingam,etal.SynthesisofRigidifiedeIF4E/eIF4Ginhibitor-1(4EGI-1)MimeticandTheirinVitroCharacterizationasInhibitorsofProtein-ProteinInteraction.JMedChem.2014Jun26;57(12):5094-111.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchus