Kinesore-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEKinesoreCat.No.:HY-112777CASNo.:363571-83-9分⼦式:C₂₀H₁₆Br₂N₄O₄分⼦量:536.17作⽤靶点:Others作⽤通路:Others储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(233.14mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8651mL9.3254mL18.6508mL5mM0.3730mL1.8651mL3.7302mL10mM0.1865mL0.9325mL1.8651mL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(3.88mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性KinesoreKLC2-SKIP相互作⽤的抑制剂。IC50&TargetKLC2-SKIP[1].体外研究Remarkably,inkinesore-treatedcells,themicrotubulenetworkisentirelyreorganizedintoaseriesofloopsandbundles.Inaddition,thelysosomalcompartmentaccumulatesinajuxtanuclearposition,wheretherearerelativelyfewmicrotubules.At50μMkinesore,thisphenotypeishighlypenetrant,with95±2.4%(n=3,totalof200cells)ofcellsexhibitingareorganizednonradialmicrotubulenetwork.Intitrationexperiments,incellstreatedfor1h,thisphenotypebecomesapparentataconcentrationof25μMkinesore,withrelativelylittleeffectatorbelowconcentrationsof12.5μM.Theeffectisreversiblebecausea2-hwashoutofkinesorefromcellstreatedfor1hledtothereestablishmentoftheradialmicrotubulearray.Thiskinesore-inducedreorganizationofthemicrotubulenetworkisobservedinapanelofmammaliannormalandcancercelllines.Inwild-typecells,50μMkinesoreinducestheremodelingofthemicrotubulenetworkandtheformationofextensivemicrotubule-richprojections.ThisphenotypeisstronglysuppressedinKif5Bknockoutcells,confirmingthatmicrotubuleremodelinginducedbykinesoreisdependentuponthepresenceofkinesin-1[1].PROTOCOLCellAssay[1]Toexaminetheeffectofkinesoreincells,HeLacellsaretreatedwith50μMkinesoreorvehiclecontrol(0.1%DMSO)for1h[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].RandallTS,etal.Asmall-moleculeactivatorofkinesin-1drivesremodelingofthemicrotubulenetwork.ProcNatlAcadSciUSA.2017Dec26;114(52):13738-13743.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplica