Scutellarin-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEScutellarinCat.No.:HY-N0751CASNo.:27740-01-8分⼦式:C₂₁H₁₈O₁₂分⼦量:462.36作⽤靶点:STAT;Akt;HIV作⽤通路:JAK/STATSignaling;StemCell/Wnt;PI3K/Akt/mTOR;Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(216.28mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1628mL10.8141mL21.6282mL5mM0.4326mL2.1628mL4.3256mL10mM0.2163mL1.0814mL2.1628mL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：0.5%CMC-Na/salinewater1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:10mg/mL(21.63mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Scutellarin从芩中分离到的酮类物质，在HCC细胞中，能够下调STAT3/Girdin/Akt信号通路，在破⾻细胞中，能够抑制RANKL介导的MAPK/NF-κB信号通路。Scutellarin具有抗HIV-1IIIB，HIV-1(74V)和HIV-1KM018的活性，EC50分别为26μM，253μM和136μM。IC50&TargetSTAT3HIV-1体外研究ScutellarintreatmentsignificantlyreducesHepG2cellviabilityinadose-dependentmanner,andinhibitsmigrationandinvasionofHCCcellsinvitro.ScutellarintreatmentsignificantlyreducesSTAT3andGirdersofactinfilaments(Girdin)expression,STAT3andAktphosphorylationinHCCcells.IntroductionofSTAT3overexpressionrestoresthescutellarin-downregulatedGirdinexpression,Aktactivation,migrationandinvasionofHCCcells.Furthermore,inductionofGirdinoverexpressioncompletelyabrogatestheinhibitionofscutellarinontheAktphosphorylation,migrationandinvasionofHCCcells.ScutellarincaninhibitHCCcellmetastasisinvivo,andmigrationandinvasioninvitrobydown-regulatingtheSTAT3/Girdin/Aktsignaling[1].ScutellarinselectivelyenhancesAktphosphorylation[2].Scutellarinisaputativetherapeuticagentasithasbeenfoundtonotonlysuppressmicroglialactivationthusamelioratingneuroinflammation,butalsoenhanceastrocyticreaction.Acutellarinamplifiestheastrocyticreactionbyupregulatingtheexpressionofneurotrophicfactorsamongothersthusindicatingitsneuroprotectiverole.Remarkably,theeffectsofscutellarinonreactiveastrocytesaremediatedbyactivatedmicrogliasupportingafunctional"cross-talk"betweenthetwoglialtypes[3].ScutellarincansuppressRANKL-mediatedosteoclastogenesis,thefunctionofosteoclastboneresorption,andtheexpressionlevelsofosteoclast-specificgenes(tartrate-resistantacidphosphatase(TRAP),cathepsinK,c-Fos,NFATc1).FurtherinvestigationindicatesthatScutellarincaninhibitRANKL-mediatedMAPKandNF-κBsignalingpathway,includingJNK1/2,p38,ERK1/2,andIκBαphosphorylation[5].体内研究Scutellarin(50mg/kg/day)significantlymitigatesthelungandintrahepaticmetastasisofHCCtumorsinvivo.Thenumbersofthelungandintrahepaticmetastatictumorsinthescutellarin-treatedgrouparesignificantlylessthanthatinthecontrols[1].TheratstreatedwithScutellarindisplayasignificantalleviationinneurobehavioraldeficitscomparedtotheSAHgroup.ScutellarinenhancedeNOSexpressioncomparedwithSAHrats[4].PROTOCOLCellAssay[1]HepG2cells(1×105/well)areculturedin96-wellplatesandtreatedintriplicatewithscutellarinatconcentrationsof5,10,20,30,and100μMorvehiclealonefor24h.Thecellularviabilityistestedby3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide(MTT)assay,andisexpressedasapercentageofproliferationversuscontrols.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalToestablishanorthotopicliverxenograftmodel,individualmiceareanesthetizedwithisofluraneandasmallAdministration[1]incisionismadeintheirabdomen.Individualmiceareinjectedwith2×106SK-Hep1cellsin30μLMatrigelintotheirleftlobeoftheliver.Twenty-fourhoursafterorthotopicliverimplantation,themicearerandomizedandinjectedintraperitoneallywithscutellarin(50mg/kg/day)orvehicle(0.9%NaCl,normalsaline)dailyfor35consecutivedays(n=10pergroup).Subsequently,themicearesacrificed,andtheirlungsandliversareexcised,fixedin10%bufferedformalinandparaffin-embeddedforhematoxylinandeosinstaining.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•CellDeathDis.2020Nov13;11(11):978.•PhytotherRes.2021Dec2.•CellBiolInt.2022Jun28.•ThoracCancer.2019Mar;10(3):492-500.•Bioengineered.2022Jan;13(1):1013-1024.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].KeY,etal.ScutellarinsuppressesmigrationandinvasionofhumanhepatocellularcarcinomabyinhibitingtheSTAT3/Girdin/Aktactivity.BiochemBiophysResCommun.2016Dec18.pii:S0006-291X(16)32174-X[2].YangLL,etal.DifferentialregulationofbaicalinandscutellarinonAMPKandAktinpromotingadiposecellglucosedisposal.BiochimBiophysActa.2016Nov27;1863(2):598-606.[3].WuCY,etal.Scutellarinattenuatesmicroglia-mediatedneuroinflammationandpromotesastrogliosisincerebralischemia-atherapeuticconsideration.CurrMedChem.2016Nov18.[Epubaheadofprint][4].LiQ,etal.ScutellarinattenuatesvasospasmthroughtheErk5-KLF2-eNOS