Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPI4KIIIbeta-IN-10Cat.No.:HY-100198CASNo.:1881233-39-1分?式:C??H??N?O?S?分?量:475.58作?靶點(diǎn):PI4K作?通路:PI3K/Akt/mTOR儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥30mg/mL(63.08mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1027mL10.5135mL21.0270mL5mM0.4205mL2.1027mL4.2054mL10mM0.2103mL1.0513mL2.1027mL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(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)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(shí)驗(yàn)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(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%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(5.26mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.26mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.26mM);ClearsolutionBIOLOGICALACTIVITY?物活性PI4KIIIbeta-IN-10?種有效的PI4KIIIβ抑制劑，IC50為3.6nM。IC50&TargetPI4KIIIβPI4KIIIαPI3KδPI3KC2γ3.6nM(IC50)3μM(IC50)720nM(IC50)1μM(IC50)PI3KαPI3Kγ10μM(IC50)20μM(IC50)體外研究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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?NatImmunol.2022Nov28.?JExtracellVesicles.2022Jun;11(6):e12233.?NatChemBiol.2022Jul4.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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