PI4KIIIbeta-IN-10-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPI4KIIIbeta-IN-10Cat.No.:HY-100198CASNo.:1881233-39-1分⼦式:C₂₂H₂₅N₃O₅S₂分⼦量:475.58作⽤靶点:PI4K作⽤通路:PI3K/Akt/mTOR储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥30mg/mL(63.08mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1027mL10.5135mL21.0270mL5mM0.4205mL2.1027mL4.2054mL10mM0.2103mL1.0513mL2.1027mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(5.26mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.26mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.26mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性PI4KIIIbeta-IN-10⼀种有效的PI4KIIIβ抑制剂，IC50为3.6nM。IC50&TargetPI4KIIIβPI4KIIIαPI3KδPI3KC2γ3.6nM(IC50)3μM(IC50)720nM(IC50)1μM(IC50)PI3KαPI3Kγ10μM(IC50)20μM(IC50)体外研究PI4KIIIbeta-IN-10(Compound10)isapotentPI4KIIIβinhibitorwithveryminoroff-targetinhibitionofPI4KIIIβrelatedlipidkinases.PI4KIIIbeta-IN-10showsweakinhibitionofPI3KC2γ(IC50~1µM),PI3Kα(~10µM),andPI4KIIIα(~3µM),and[1].PROTOCOLKinaseAssay[1]Lipidkinaseassaysarepreformedusingrecombinantenzyme,phosphoinositidesandγ32P-ATPinamembranecaptureassay.Eachinhibitor(e.g.,PI4KIIIbeta-IN-10)isdilutedinto10%DMSOandkinaseassaybuffer.Uponcompletionofthereaction,4µLisspottedonto0.2µmnitrocellulose.Themembraneisdriedfor5minutesunderaheatlampfollowedby1×30secondwashand6×5minwashesin1MNaCl/1%PhosphoricAcid.Themembraneisdriedfor20minutesunderaheatlampfollowedbyovernightexposuretoaphosphorscreenandphosphorimagingfollowedonaTyphoon9500.IntensitiesarequantifiedusingSPOT.Specificationsforeachenzymefollow.L-α-PhosphatidylinositolandDOPS:DOPClipidsaresonicatedinwatertogenerate1mg/mLPI:DOPS:DOPC.Reactionisset-upasfollows1)kinaseassaybuffer,PI:DOPS:DOPC,BSAandPI4KIIIβ,arecombinedinatotalvolumeof10µL(2.5xsolution);2)5µLofinhibitorsolutionisadded(5xsolution)andincubatedwithenzymemixturefor15minutes;3)10µLcoldATPandγ32P-ATPareadded(2.5xsolution)toinitiatethereactionwhichranfor30minutes.Finalconditionsareasfollows:20mMBis-TrisPropanepH7.5,10mMMgCl2,0.075mMTritonX-100,0.5mMEGTA,1mMDTT,100µMPI,500ng/µLBSA,2.5nMPI4KIIIβ,2%DMSO,10µMATPand1uCiγ32P-ATP[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•NatImmunol.2022Nov28.•JExtracellVesicles.2022Jun;11(6):e12233.•NatChemBiol.2022Jul4.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•EMBOJ.2022Nov21;e112677.•Autophagy.2019Jul;15(7):1214-1233.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].RutaganiraFU,etal.DesignandStructuralCharacterizationofPotentandSelectiveInhibitorsofPhosphatidylinositol4KinaseIIIβ.JMedChem.2016Mar10;59(5):1830-9.McePdfHeightCaution:Producthas