Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMonastrolCat.No.:HY-101071ACASNo.:329689-23-8Synonyms:(±)-Monastrol分?式:C??H??N?O?S分?量:292.35作?靶點:Kinesin;Apoptosis作?通路:CellCycle/DNADamage;Cytoskeleton;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:≥33mg/mL(112.88mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.4206mL17.1028mL34.2056mL5mM0.6841mL3.4206mL6.8411mL10mM0.3421mL1.7103mL3.4206mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(8.55mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(8.55mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(8.55mM);ClearsolutionBIOLOGICALACTIVITY?物活性Monastrol具有?效性和細胞滲透性的有絲分裂驅(qū)動蛋?Eg5的抑制劑，IC50值為14μM。IC50&TargetEg514μM(IC50)體外研究Monastrolisasmall,cell-permeablemoleculethatarrestscellsinmitosisbyspecificallyinhibitingEg5,amemberoftheKinesin-5family.Monastroltreatmentofdividingcellsresultsinspindlecollapseandcellcyclearrestwithamonoastralspindle,whichissimilartothephenotypeobservedwhenEg5isinhibitedbyanti-Eg5antibodies[1].MonastrolisanallostericinhibitorofthemitotickinesinEg5thatexhibitsanantiproliferativeeffectagainstseveralcelllines.MonastroltreatmentcandecreasecellviabilityinMCF-7tumorcells.Real-timecellgrowthkineticanalysisshowedadecreaseintheproliferationofMCF-7cellsexposedtomonastrol[2].PROTOCOLCellAssay[2]ThecytotoxicityassayisperformedwithMTT.Cellsareseededin96-wellcultureplates(5000cells/well)andincubatedfor24hforstabilization.Afterthisperiod,thefollowingtreatmentsareadministeredfor24and48h:vehiclecontrol(0.5%DMSO);1μMdoxorubicinandmonastrolat5,25,50,75,and100μM.Aftereachtimeoftreatment,themediumiswithdrawn,serum-freemediacontaining0.5mg/mLMTTsaltisaddedandincubatedfor4h,andformazancrystalproductsarediluted[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻?IntJBiolSci.2021Jan1;17(2):514-526.?ComputStructBiotechnolJ.1October2021.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].CochranJC,etal.MonastrolinhibitionofthemitotickinesinEg5.JBiolChem.2005Apr1;280(13):12658-67.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[2].MarquesLA,etal.Antiproliferativeactivityofmonastrolinhumanadenocarcinoma(MCF-7)andnon-tumor(HB4a)breastcells.NaunynSchmiedebergsArchPharmacol.2016Dec;389(12):1279-1288.[3].MayerTU,etal.Smallmoleculeinhibitorofmitoticspindlebipolarityidentifiedinaphenotype-basedscreen.Science.1999Oct29;286(5441):971-4.McePdfHeightCaution:Producthasnotbeenfu