Ruboxistaurin-LY333531-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemERuboxistaurinCat.No.:HY-10195CASNo.:169939-94-0Synonyms:LY333531分⼦式:C₂₈H₂₈N₄O₃分⼦量:468.55作⽤靶点:PKC作⽤通路:Epigenetics;TGF-beta/Smad储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(106.71mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1342mL10.6712mL21.3424mL5mM0.4268mL2.1342mL4.2685mL10mM0.2134mL1.0671mL2.1342mL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(5.34mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Ruboxistaurin(LY333531)⼀种具有⼝服活性，选择性PKCbeta抑制剂(Ki=2nM)，Ruboxistaurin表现出ATP依赖的竞争性抑制PKCbetaI，其IC50为4.7nM。Ruboxistaurin对PKCbetaII的IC50为5.9nM[1][2]。IC50&TargetPKC-βIPKC-βIIPKCηPKCδ4.7nM(IC50)5.9nM(IC50)52nM(IC50)250nM(IC50)PKCγPKCαPKCε300nM(IC50)360nM(IC50)600nM(IC50)体外研究RuboxistaurinisaselectiveandATP-competitivePKCβinhibitor,withIC50sof4.7and5.9nMforPKCβIandPKCβII,showslesspotentinhibitiononPKCη(IC50,52nM),PKCα(IC50,360nM),PKCγ(IC50,300nM),PKCδ(IC50,250nM),andhasnoeffectonPKCζ(IC50,>100μM)[1].Ruboxistaurin(10and400nM)dramaticallyinhibitsglucose-inducedmonocyteadherencetolevelsthatarenotdifferentfrombaselineadherenceofmonocytestoendothelialcellsunderNGconditions.Ruboxistaurin(10and400nM)dosenotaltertheendothelialexpressionofadhesionmoleculesormodifyendothelialcellgrowth[2].Ruboxistaurin(LY333531;10nM)reduceshigh-glucose(HG)-inducedhumanrenalglomerularendothelialcells(HRGECs)viability,andinhibitstheincreasesinswiprosin-1inHRGECsincubatedwithHG[3].体内研究Ruboxistaurin(1mg/kg;8weeks)markedlyreducesGECapoptosisaswellasswiprosin-1upregulation,andamelioratesrenalglomerularinjuryinthediabeticmice.RuboxistaurinalsopotentlyattenuatestheexpressionofPARP,cleaved-caspase9,cleaved-caspase3,andtheBax/Bcl-2ratio,indiabeticmice[3].Ruboxistaurin(0.1,1.0,or10.0mg/kg;p.o.)dramaticallyreducesthenumberofleukocytestrappedintheretinalmicrocirculationofdiabeticrats[4].AnimalModel:Rats[4]Dosage:0.1,1.0,or10.0mg/kgAdministration:P.o.Result:Dramaticallyreducedthenumberofleukocytestrappedintheretinalmicrocirculationofdiabeticrats.户使⽤本产品发表的科研⽂献•SciTranslMed.2018Jul18;10(450).pii:eaaq1093.•CellBiosci.2021Feb8;11(1):32.•Endocrinology.2018May1;159(5):2253-2263.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•BiosciRep.2018Sep7;38(5):BSR20171459.•ACSOmega.2020Oct12;5(41):26551-26561.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].JirousekMR,etal.(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16,21-dimetheno-1H,13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-dione(LY333531)andrelatedanalogues:isozymeselectiveinhibitorsofproteinkinaseCbeta.JMedChem.1996;39(14):2664-2671.[2].Ruboxistaurin:LY333531.DrugsRD.2007;8(3):193-199.[3].KuntT,etal.Thebeta-specificproteinkinaseCinhibitorruboxistaurin(LY333531)suppressesglucose-inducedadhesionofhumanmonocytestoendothelialcellsinvitro.JDiabetesSciTechnol.2007Nov;1(6):929-35.[4].NonakaA,etal.PKC-betainhibitor(LY333531)attenuatesleukocyteentrapmentinretinalmicrocirculationofdiabeticrats.InvestOphthalmolVisSci.2000Aug;41(9):2702-6.McePdfHeightCa