Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEKenpaulloneCat.No.:HY-12302CASNo.:142273-20-9Synonyms:9-Bromopaullone;NSC-664704分?式:C??H??BrN?O分?量:327.18作?靶點(diǎn):CDK;GSK-3作?通路:CellCycle/DNADamage;PI3K/Akt/mTOR;StemCell/Wnt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:≥35mg/mL(106.97mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.0564mL15.2821mL30.5642mL5mM0.6113mL3.0564mL6.1128mL10mM0.3056mL1.5282mL3.0564mL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)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.64mM);SuspendedsolutionBIOLOGICALACTIVITY?物活性Kenpaullone?種有效的CDK1/cyclinB和GSK-3β抑制劑，IC50值分別為0.4μM和23nM，同時(shí)可抑制CDK2/cyclinA，CDK2/cyclinE和CDK5/p25的活性，IC50值分別為0.68μM，7.5μM和0.85μM。Kenpaullone，?種KLF4的?分?抑制劑，在體外降低乳腺癌?細(xì)胞的?我更新和細(xì)胞活?。IC50&TargetCdk1/cyclinBcdk2/cyclinACDK5/p35CDK2/cyclinE0.4μM(IC50)0.68μM(IC50)0.85μM(IC50)7.5μM(IC50)GSK-3βerk1erk2c-raf0.023μM(IC50)20μM(IC50)9μM(IC50)38μM(IC50)體外研究Kenpaulloneshowsmuchlesseffectonc-src(IC50,15μM),caseinkinase2(IC50,20μM),erk1(IC50,20μM),anderk2(IC50,9μM).KenpaulloneactsbycompetitiveinhibitionofATPbinding,andtheapparentKiis2.5μM.Kenpaullonecaninhibitthegrowthoftumorcellsinculture(meanGI50,43μM)andcausesalteredcellcycleprogressionmostclearlyrevealedunderconditionsofrecoveryfromserumstarvation[1].Kenpaullonedemonstratesawiderangeofbiologicalutility,extendingfrommaintenanceofpancreaticβcellsurvivalandproliferationtotheinductionofapoptosisincancercells[2].PROTOCOLKinaseAssay[1]Thekinaseassayisrunfor10minat30°Cwith1mg/mLhistoneH1,inthepresenceof15μM[g-32P]ATP(3000Ci/μmol;1mCi/mL)inafinalvolumeof30ml.Purificationandassaysorinhibitionofotherkinasesareperformed.Inkineticexperiments,thehistoneH1concentrationisloweredto3.5mg/mL;theATPconcentrationrangedfrom50to400μM,andthekenpaulloneconcentrationrangesfrom1to4μM.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?MilMedRes.2020Nov1;7(1):52.?MilMedRes.2020Sep6;7(1):42.?SciAdv.2021Apr14;7(16):eabb2213.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ZaharevitzDW,etal.Discoveryandinitialcharacterizationofthepaullones,anovelclassofsmall-moleculeinhibitorsofcyclin-dependentkinases.CancerRes.1999Jun1;59(11):2566-9.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[2].LyssiotisCA,etal.ReprogrammingofmurinefibroblaststoinducedpluripotentstemcellswithchemicalcomplementationofKlf4.ProcNatlAcadSciUSA.2009Jun2;106(22):8912-7.[3].FYu,etal.Kruppel-likefactor4(KLF4)isrequiredformaintenanceofbreastcancerstemcellsandforcellmigrationandinvasion.Oncogene.2011May5;30(18):2161-72.McePdfHeightCaution:Producthasnotbe