Nocodazole-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemENocodazoleCat.No.:HY-13520CASNo.:31430-18-9分?式:C??H??N?O?S分?量:301.32作?靶點:Microtubule/Tubulin;Bcr-Abl;CRISPR/Cas9;Autophagy;Apoptosis作?通路:CellCycle/DNADamage;Cytoskeleton;ProteinTyrosineKinase/RTK;Autophagy;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months

-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:20mg/mL(66.37mM;Needultrasonic)掃描?維碼，運?溶解?案計算器獲得適合您實驗體系的溶解?案MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.3187mL16.5937mL33.1873mL5mM0.6637mL3.3187mL6.6375mL10mM0.3319mL1.6594mL3.3187mL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，并請注意儲備液的保存?式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?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(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?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.請依序添加每種溶劑：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:≥2mg/mL(6.64mM);Clearsolution此?案可獲得≥2mg/mL(6.64mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL20.0mg/mL的澄DMSO儲備液加到900μL20%的SBE-β-CD?理鹽??溶1/3www.MedChemEwww.MedChemE液中，混合均勻。BIOLOGICALACTIVITY?物活性Nocodazole(Oncodazole)快速可逆的microtubule抑制劑。Nocodazole與β-微管蛋?結(jié)合并破壞微管組裝/拆卸動?學(xué)，從?防?有絲分裂并誘導(dǎo)腫瘤細(xì)胞凋亡。Nocodazole抑制Bcr-Abl，增強(qiáng)CRISPR/Cas9的活性。IC50&TargetAblABL(E255K)ABL(T315I)BRAF91nM(Kd)120nM(Kd)170nM(Kd)1.8μM(Kd)BRAF(V600E)c-KITMEK1MEK21.1μM(Kd)1.6μM(Kd)1.7μM(Kd)1.6μM(Kd)METPI3KγMicrotubule/TubulinCRISPR/Cas91.7μM(Kd)1.5μM(Kd)(Kd)(Kd)體外研究Nocodazoleexhibitsgoodaffinitytowardc-KIT,withaKdvalueof1.6μMinhighlymalignanthumancancercells.Nocodazoledisplaysgoodbindingaffinitytowardthecomponentsofthemitogen-activatedproteinkinase(MAPK)pathway,suchasBRAF(Kd=1.8μM),BRAF(V600E)(Kd=1.1μM),MEK1(Kd=1.7μM),andMEK2(Kd=1.6μM)[1].NocodazolehasthehighestaffinityforαβIVandthelowestaffinityforαβIII[2].Nocodazole(1nM)inducesapoptosisofCOLO205cancercells[3].Nocodazole(≥30μg/mL)significantlyincreasesthepercentageofannexin-V-bindingcellswithoutsignificantlymodifyingaverageforwardscatterofhumanerythrocytes[4].體內(nèi)研究Nocodazole(5mg/kg/threetimesperweek,i.p.)hasantitumoreffectsinathymicmicebearingCOLO205tumorxenografts.Nocodazole(1nM)+R-41400dramaticallyincreasethelevelsofp21/CIP1andp27/KIP1proteininthetumortissues[3].PROTOCOLCellAssay[3]Proteinsareloadedat50μg/laneandseparatedby12%(w:v)sodiumdodecylsulfate-polyacrylamidegelelectrophoresis,blotted,andprobedwithantibodiesforcyclinE,p53,p21/CIP1,p27/KIP1,glyceraldehyde3-phosphatedehydrogenase(GAPDH),cyclinA,cyclinD1,cyclinD3,cyclinB,CDK2,CDK4,andcytochromeC.Immunoreactivebandsarevisualizedbyincubatingwiththecolorigenicsubstratesnitrobluetetrazoliumand5-bromo-4-chloro-3-indolyl-phosphate.TheexpressionofGAPDHisusedasthecontrolforequalproteinloading.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalCOLO205cellsaregrowninRPMI1640supplementedwith10%FCS.CellsareharvestedthroughtwoAdministration[3]consecutivetrypsinizations,centrifugedat300×g;for5min,washedtwice,andresuspendedinsterilephosphate-bufferedsaline(PBS).Cells(5×105)in0.1mLareinjectedsubcutaneouslybetweenthescapulaeofeachnudemouse.Aftertransplantation,tumorsizeismeasuredwithcalipers,andthetumorvolumeis2/3www.MedChemEwww.MedChemEestimated.Oncetumorsreachameansizeof200mm3,animalsreceiveintraperitonealinjectionsofDMSO(25μL),R-41400(50mg/kg),nocodazole(5mg/kg),orR-41400+nocodazolethreetimesperweekfor6wk.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?AdvSci(Weinh).2020Jun17;7(15):1903583.?NatCommun.2019Jun28;10(1):2860.?NucleicAcidsRes.2020Dec16;48(22):e127.?Autophagy.2021Mar22;1-17.?Theranostics.2019May31;9(13):3732-3753.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ParkH,etal.Nocodazoleisahigh-affinityligandforthecancer-relatedkinasesABL,c-KIT,BRAF,andMEK.ChemMedChem.2012Jan2;7(1):53-6.[2].KeliangXu,etal.Interactionofnocodazolewithtubulinisotypes.DrugDevelopmentResearch2002[3].WangYJ,etal.R-41400potentiatestheantitumoreffectsofnocodazole:Invivotherapyforhumantumorxenograftsinnudemice.MolCarcinog.2002Aug;34(4):199-210.[4].SignorettoE,etal.NocodazoleInducedSuicidalDeathofHumanErythrocytes.CellPhysiolBiochem.2016;38(1):379-92.[5].ZhangJP,etal.EfficientpreciseknockinwithadoublecutHDRdonorafterCRISPR/Cas9-mediateddouble-strandedDNAcleavage.GenomeBiol.2017Feb20;18(1):35.McePdfHeight關(guān)注MCE中國公眾號，

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