Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPKM2-IN-1Cat.No.:HY-103617CASNo.:94164-88-2分?式:C??H??NO?S?分?量:345.48作?靶點:PyruvateKinase作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:320mg/mL(926.25mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.8945mL14.4726mL28.9452mL5mM0.5789mL2.8945mL5.7890mL10mM0.2895mL1.4473mL2.8945mL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(fù)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(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%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:8mg/mL(23.16mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥8mg/mL(23.16mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥8mg/mL(23.16mM);ClearsolutionBIOLOGICALACTIVITY?物活性PKM2-IN-1?種丙酮酸激酶M2(PKM2)抑制劑，其IC50值為2.95μM。IC50&TargetIC50:2.95μM(PKM2)[1]體外研究PKM2-IN-1isapyruvatekinaseM2(PKM2)inhibitorwithanIC50of2.95±0.53μM.ResultsshowthatmostofthetestedcompoundsexhibitsomedegreeofPKM2inhibitionandsomecompounds,suchasPKM2-IN-1(compound3k)and6d,displaymorepotentactivitythanthepositivecontrolshikonin.TherepresentativecompoundsPKM2-IN-1,6ddisplaydose-dependentinhibitionofPKM2withlessinhibitionofPKM1andPKLlikeshikonin.Amongalltestedcompounds,themostpotentcompoundsare3a,PKM2-IN-1and3r,whichexhibitIC50valuesagainstHCT116andHelacellsrangingfrom0.39to0.41μM,0.18to0.29μMand0.18to0.38μM,respectively[1].PROTOCOLCellAssay[1]Celllines(HCT116,Hela,H1299,BEAS-2B)areculturedinRPMI1640containing9%fetalbovineserum(FBS)at37°Cin5%CO2.CellviabilityisdetectedwiththeMTSassayaccordingtothemanufacturer'sinstructions.Briefly,5000cellsinperwellareplatedin96-wellplates.Afterincubatedfor12h,thecellsaretreatedwithdifferentconcentrationoftestedcompound(includingPKM2-IN-1)orDMSO(asnegativecontrol)for48h.Then20μLMTSisaddedinperwellandincubatedat37°Cfor3h.Absorbanceofeachwellisdeterminedbyamicroplatereaderata490nmwavelength.TheIC50valuesarecalculatedusingPrismGraphpadsoftwareofthetriplicateexperiment[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?SciAdv.2022Sep23;8(38):eabo0987.?EBioMedicine.2020Apr;54:102722.?CellRep.2022Mar8;38(10):110468.?JPathol.2022Apr;256(4):414-426.?EurJPharmacol.2019Apr17;854:232-239.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].NingX,etal.DiscoveryofnovelnaphthoquinonederivativesasinhibitorsofthetumorcellspecificM2isoformofpyruvatekinase.EurJMedChem.2017Sep29;138:343-352.McePdfHeightCaution:Producthasnotbeenfully