iCRT3-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEiCRT3Cat.No.:HY-103705CASNo.:901751-47-1分⼦式:C₂₃H₂₆N₂O₂S分⼦量:394.53作⽤靶点:Wnt;Apoptosis作⽤通路:StemCell/Wnt;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:150mg/mL(380.20mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5347mL12.6733mL25.3466mL5mM0.5069mL2.5347mL5.0693mL10mM0.2535mL1.2673mL2.5347mL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(6.34mM);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:≥2.5mg/mL(6.34mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性iCRT3Wnt和β-连环蛋⽩应答转录(β-catenin-responsivetranscription)的抑制剂。IC50&TargetWnt[1],β-catenin-responsivetranscription[2]体外研究iCRT3isaninhibitorofbothWntandβ-catenin-responsivetranscription.iCRT3significantlydecreasesTOPFlashactivityandreducesthelevelofNTSR1.Theanti-apoptoticeffectsofNeurotensin(NTS)andWnt3acanbelargelyabrogatedbyiCRT3[1].CellsmaintainedlongtermwithiCRT3showenhancedexpressionofclassicpluripotencygenescomparewiththeDMSOcontrol,whereasexpressionofdifferentiationmarkersandT-cellfactor(TCF)targetgenesisconcomitantlyreduced[2].TreatmentwithiCRT3atdosesof12.5,25,50,and75μMdecreasesTNF-αlevelsby14.7%,18.5%,44.9%and61.3%,respectively.WithiCRT3treatment,IκBlevelsareincreasedinadose-dependentmannercomparetothevehicle[3].体内研究ThetumorgrowthratesaremarkedlyretardedbyiCRT3treatment.Consistently,thetumor-suppressiveroleofiCRT3isaccompaniedwithareductioninKi67index,aproliferationmarker[1].TheIL-6levelsinthe10ꢀmg/kgiCRT3treatmentgroupare82.9%lowerthanthoseinthevehiclegroup.IL-1βlevelsareundetectableintheshambutreach371ꢀpg/mLinsepticmiceandaredownby30.2%and53.2%,respectively,with5and10ꢀmg/kgiCRT3.WithiCRT3treatmentatdosesof5and10ꢀmg/kg,ASTlevelsinthesesepticmiceare15.4%and44.2%lower,respectively,thanthoseinthevehicle-treatedmice.Aftertreatmentwith10ꢀmg/kgiCRT3,lungmorphologyisimprovedwithmuchreducedmicroscopicdeterioration,comparetothevehiclegroup.ThenumberofapoptoticcellsinthelungtissuesoftheiCRT3-treatedmiceissignificantlyreducedby92.7%incomparisonwiththevehiclegroup[3].PROTOCOLCellAssay[1]Cellsareseededinto96-wellplatestoadensityof5×103cellsperwellandincubatedintheculturemediumwithiCRT3foranadditional48h.CellviabilityandcellapoptosisassaysarecarriedoutusingaCellCountingkit-8andaCaspase-Glo3/7assaykitaccordingtothemanufacturer’sinstructions,respectively[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalNOD-SCIDBALB/cmiceareinoculatedsubcutaneouslyintherightbackwith2×106A172cells.ThegrowthAdministration[1]oftheprimarytumorsisrecordedevery4days.iCRT3(5mg/kg)isdilutedinPBSi.p.triweeklywhentumorsgrowto~200mm3.ThecontrolmicearetreatedwithblankPBScontaining5%(v/v)DMSO.Tumorvolumeisevaluatedwiththefollowingformula:volume=tumorlength×width2/2.Themicearesacrificed24daysafterpharmaceuticaltreatment.Thetumorsareresectedandembeddedinparaffin,andtheKi67stainingisanalyzedbyimmunohistochemistry[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE户使⽤本产品发表的科研⽂献•NatCommun.2022Nov2;13(1):6552.•NatCommun.2022Jul28;13(1):4364.•NatCommun.2021Nov24;12(1):6831.•BMCBiol.2020Oct27;18(1):151.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].XiaoH,etal.ANovelPositiveFeedbackLoopBetweenNTSR1andWnt/β-CateninContributestoTumorGrowthofGlioblastoma.CellPhysiolBiochem.2017Oct24;43(5):2133-2142.[2].ChatterjeeSS,etal.Inhibitionofβ-catenin-TCF1interactiondelaysdifferentiationofmouseembryonicstemcells.JCellBiol.2015Oct12;211(1):39-51.[3].SharmaA,etal.Mitigationofsepsis-inducedinflammatoryresponsesandorganinjurythroughtargetingWnt/β-cateninsignaling.doi: