AP-III-a4-hydrochloride-ENOblock-hydrochloride-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAP-III-a4hydrochlorideCat.No.:HY-15858ACASNo.:2070014-95-6Synonyms:ENOblockhydrochloride分?式:C??H??ClFN?O?分?量:631.18作?靶點:Enolase;Apoptosis作?通路:MetabolicEnzyme/Protease;Apoptosis儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數據體外實驗DMSO:≥53mg/mL(83.97mM)H2O:<0.1mg/mL(insoluble)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.5843mL7.9217mL15.8433mL5mM0.3169mL1.5843mL3.1687mL10mM0.1584mL0.7922mL1.5843mL請根據產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品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?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儲存條件，適當保存；體內實驗的?作液，建議您現?現配，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沉淀、析出現象，可以通過加熱和/或超聲的?式助溶)1/4MasterofBioactiveMolecules—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:≥2.08mg/mL(3.30mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.30mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.30mM);ClearsolutionBIOLOGICALACTIVITY?物活性AP-III-a4(ENOblock)hydrochloride?種?底物類似物烯醇酶(enolase)抑制劑，IC50為0.576uM。AP-III-a4hydrochloride可?于癌癥和糖尿病研究。IC50&TargetIC50:0.576uM(enolase)[1]體外研究AP-III-a4(ENOblock)(0-10μM;24h)inhibitsHCT116cellviabilityinadose-dependentmanner[1].AP-III-a4directlybindstoenolaseandinhibitsitsactivity[1].AP-III-a4(0-10μM;24or48h)inhibitscancercellmigrationandinvasion,inducescancercellapoptosis[1].AP-III-a4(10μM;24h)caninduceglucoseuptakeandinhibitphosphoenolpyruvatecarboxykinase(PEPCK)expressioninhepatocytesandkidneycells[1].CellViabilityAssay[1]CellLine:HCT116Concentration:1.25,2.5,5and10μMIncubationTime:24hResult:InducedhigherlevelsofHCT116coloncancercelldeathinhypoxicconditionscomparedtonormoxia.WesternBlotAnalysis[1]CellLine:HCT116Concentration:1.25,2.5,5and10μMIncubationTime:24hforAKT,48hforBcl-XlResult:Boundtoenolaseincelllysateandboundtopurifiedenolase.DecreasedtheexpressionofAKTandBcl-Xl,whicharenegativeregulatorsofapoptosis.CellInvasionAssay[1]CellLine:HCT116Concentration:0.156,0.312,0.625,1.25and2.5μM2/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEIncubationTime:24hResult:Significantlyinhibitscancercellinvasionatatreatmentconcentrationof0.625μM.CellMigrationAssay[1]CellLine:HCT116Concentration:0.625,1.25and2.5μMIncubationTime:24hResult:Inhibitedcellmigrationdose-dependently.RT-PCR[1]CellLine:Huh7andHEKConcentration:10μMIncubationTime:24hResult:InducedglucoseuptakeandinhibitedPEPCKexpression.體內研究AP-III-a4(ENOblock)(10μM;96h)inhibitscancercellmetastasisandsuppressesthegluconeogenesisregulatorPEPCKinzebrafish[1].AnimalModel:ThezebrafishcancercellHCT116xenograftmodel[1]Dosage:10μMAdministration:96hResult:Reducedcancercelldissemination.InhibitedPEPCKexpressionandinducedglucoseuptake.Inhibitedadipogenesisandfoamcellformation.戶使?本產品發(fā)表的科研?獻?CellDiscov.2020Aug18;6:56.?Theranostics.2019Aug12;9(20):5769-5783.?ResearchSquarePrint.November14th,2022Seemorecustomervalidationsonwww.MedChemEREFERENCES3/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].Da-WoonJung,etal.AUniqueSmallMoleculeInhibitorofEnolaseClarifiesItsRoleinFundamentalBiologicalProcesses.ACSChem.Biol.,2013,8(6),pp1271–1282McePdfHeightCaution