GCN2-IN-6-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGCN2-IN-6Cat.No.:HY-130240CASNo.:2183470-09-7分⼦式:C₁₉H₁₂Cl₂F₂N₄O₃S分⼦量:485.29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:250mg/mL(515.16mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0606mL10.3031mL20.6062mL5mM0.4121mL2.0606mL4.1212mL10mM0.2061mL1.0303mL2.0606mL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(4.29mM);Clearsolution1/3MasterofBioactiveMolecules—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(4.29mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性GCN2-IN-6(Compound6d)⼀种有效的⼝服GCN2抑制剂，通过酶法(IC50为1.8nM)和细胞分析(IC50为9.3nM)证实。GCN2-IN-6还eIF2α激酶PERK抑制剂，IC50为0.26nM(酶法测定)和230nM(细胞测定)。IC50&TargetIC50:1.8nM(GCN2,in-houseenzymatic)and9.3nM(GCN2,cellularassays);0.26nM(PERK,in-houseenzymatic)and230nM(PERK,cellularassays)[1]体外研究ToexaminetheimpactofGCN2inhibitiononcancercellproliferation,acutelymphoblasticleukemia(ALL)CCRFCEMcellsaretreatedwithGCN2-IN-6(Compound6d)inthepresenceofasparaginedepletingagentasparaginase.TreatmentwithGCN2-IN-6greatlysensitizesCCRF-CEMcellstoasparaginase.ThemoderateantiproliferativeeffectsachievedbycombiningasparaginaseandGCN2-IN-6treatmentareobservedinGCN2-wildtype(WT)mouseembryonicfibroblast(MEF)cellsbutnotinGCN2-knockout(KO)MEF.GCN2-IN-6demonstratessuppressiononp-GCN2,p-eIF2α,andATF4activatedbyasparaginase[1].体内研究GCN2-IN-6(Compound6d;0.3-3mg/kg;oraladministration;for8hours;mice)treatmentat3mg/kgsuppressesbothself-phosphorylationofGCN2andthedownstreameffectorATF4tothebasallevelfollowingpretreatmentwithasparaginase[1].AnimalModel:MicebearingCCRF-CEMcellsxenografts[1]Dosage:0.3mg/kg,1mg/kg,and3mg/kgAdministration:Oraladministration;for8hoursResult:Suppressedbothself-phosphorylationofGCN2andthedownstreameffectorATF4tothebasallevelfollowingpretreatmentwithasparaginase.户使⽤本产品发表的科研⽂献•MolCell.2022Mar3;82(5):920-932.e7.•BloodCancerDiscov.December13,2021.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].FujimotoJ,etal.IdentificationofNovel,Potent,andOrallyAvailableGCN2InhibitorswithTypeIHalfBindingMode.ACSMedChemLett.2019Sep19;10(10):1498-1503.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedform