Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEKinesoreCat.No.:HY-112777CASNo.:363571-83-9分?式:C??H??Br?N?O?分?量:536.17作?靶點(diǎn):Others作?通路:Others儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:125mg/mL(233.14mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.8651mL9.3254mL18.6508mL5mM0.3730mL1.8651mL3.7302mL10mM0.1865mL0.9325mL1.8651mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:2.08mg/mL(3.88mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性KinesoreKLC2-SKIP相互作?的抑制劑。IC50&TargetKLC2-SKIP[1].體外研究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