Shikonin-C-I-75535-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEShikoninCat.No.:HY-N0822CASNo.:517-89-5Synonyms:C.I.75535;Isoarnebin4分⼦式:C₁₆H₁₆O₅分⼦量:288.3作⽤靶点:ChlorideChannel;PyruvateKinase;NF-κB;TNFReceptor;HIV作⽤通路:MembraneTransporter/IonChannel;MetabolicEnzyme/Protease;NF-κB;Apoptosis;Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:25mg/mL(86.72mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.4686mL17.3430mL34.6861mL5mM0.6937mL3.4686mL6.9372mL10mM0.3469mL1.7343mL3.4686mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：0.5%CMC-Na/salinewaterSolubility:30mg/mL(104.06mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(7.21mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(7.21mM);Clearsolution4.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(7.21mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Shikonin中草药紫草的主成分。Shikonin⼀种有效的TMEM16A氯化物通道(chloridechannel)抑制剂，IC50为6.5μM。Shikonin⼀种特异的丙酮酸激酶M2(PKM2)抑制剂，还可以抑制TNF-α和NF-κB途径。Shikonin通过抑制糖酵解降低外泌体(exosome)的分泌。Shikonin抑制AIM2炎性体活化。IC50&TargetTMEM16AchloridechannelPKM2NF-κB6.5μM(IC50)体外研究ShikoninisaninhibitorofTMEM16AchloridechannelwithanIC50of6.5μM[1].ShikoninisalsoaspecificinhibitorofPKM2[2]andcanalsoinhibittumornecrosisfactor-α(TNF-α)andpreventactivationofnuclearfactor-κB(NF-κB)pathway.Shikoninatconcentrationshigherthan50μMsignificantlyinhibitsormalhumankeratinocytes(NHKs)viability,comparewiththatofcontrol(P[3].TreatmentsofShikoninat5and7.5μMsignificantlyinhibitthecellviabilitystartingfrom12handtheinhibitoryeffectsarepresentedintime-dependentpatternscomparewiththe0hgroupinbothcelllines.Itisfoundthat5μMShikonindisplaysgreaterinhibitioncompareto2.5μMatthetimepointsfrom24to48h.TheinvasivenessofU87andU251cellsissignificantlyattenuatedwhentreatedwithShikoninat2.5,5,and7.5μMcomparewiththecontrolgroupat24and48h(p[4].体内研究ShikoninsignificantlyinhibitstheincreaseinIL-1βandTNF-αexpressionlevelsintheratmodelofosteoarthritis,comparewiththoseintheosteoarthritisgroup(P[5].PROTOCOLCellAssay[4]U87andU251cellsareseededinto96-wellplatesatadensityof1×104cellsperwellinstandardDMEMandincubatedfor24hunderstandardconditions(37°Cand5%CO2).Thenthemediumisreplacedwitheitherblank,serum-freeDMEMorDMEMcontainingShikoninatconcentrationsof2.5,5,and7.5μM.Thetotalvolumeineachwellis200μL.Finally,theplatesareshakensoftlyandtheopticaldensityisrecordedat570nm(OD570)usingaplatereader.Atleastthreeindependentexperimentsareperformed[4].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalHealthymaleSprague-Dawleyrats(n=30;8to10-weeksold,250to300g)areusedinthisstudy.RatsareAdministration[5]randomlyassignedtothreegroups:Sham-operatedgroup(n=10),osteoarthritismodelgroup(n=10)and2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEShikonin-treatedgroup(n=10).Inthesham-operatedgroup,therightkneejointoftheanesthetizedratisonlyexposedundersterileconditions,andtheratsaretreatedwith0.1ml/100gphysiologicalsaline(i.p.).Intheosteoarthritismodelgroup,osteoarthritismodelratsweretreatedwith0.1ml/100gphysiologicalsaline(i.p.).IntheShikonin-treatedgroup,osteoarthritismodelratsaretreatedwith10mg/kgShikonin(i.p.)oncedailyfor4daysafterosteoarthritismodeling[5].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•AdvHealthcMater.2022Jul12;e2200742.•RedoxBiol.10September2022,102458.•EnvironPollut.15February2022,118708.•Hypertension.2022May;79(5):932-945.•IntJOncol.November1,2021.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].JiangYetal.ShikoninInhibitsIntestinalCalcium-ActivatedChlorideChannelsandPreventsRotaviralDiarrhea.FrontPharmacol.2016Aug23;7:270.[2].LiW,etal.ShikoninSuppressesSkinCarcinogenesisviaInhibitingCellProliferation.PLoSOne.2015May11;10(5):e0126459.[3].YanY,etal.ShikoninPromotesSkinCellProliferationandInhibitsNuclearFactor-κBTranslocationviaProteasomeInhibitionInVitro.ChinMedJ(Engl).2015Aug20;128(16):2228-33.[4].ZhangFY,etal.ShikoninInhibitstheMigrationandInvasionofHumanGlioblastomaCellsbyTargetingPhosphorylatedβ-CateninandPhosphorylatedPI3K/Akt:APotentialMechanismfortheAnti-GliomaEfficacyofaTraditionalChineseHerbalMedicine.IntJMolSci.2015Oct9;16(10):23823-48.[5].FuD,etal.Shikonininhibitsinflammationandchondrocyteapoptosisbyregulation