Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEShikoninCat.No.:HY-N0822CASNo.:517-89-5Synonyms:C.I.75535;Isoarnebin4分?式:C??H??O?分?量:288.3作?靶點:ChlorideChannel;PyruvateKinase;NF-κB;TNFReceptor;HIV作?通路:MembraneTransporter/IonChannel;MetabolicEnzyme/Protease;NF-κB;Apoptosis;Anti-infection儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:25mg/mL(86.72mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.4686mL17.3430mL34.6861mL5mM0.6937mL3.4686mL6.9372mL10mM0.3469mL1.7343mL3.4686mL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)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?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：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：0.5%CMC-Na/salinewaterSolubility:30mg/mL(104.06mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(7.21mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(7.21mM);Clearsolution4.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(7.21mM);ClearsolutionBIOLOGICALACTIVITY?物活性Shikonin中草藥紫草的主成分。Shikonin?種有效的TMEM16A氯化物通道(chloridechannel)抑制劑，IC50為6.5μM。Shikonin?種特異的丙酮酸激酶M2(PKM2)抑制劑，還可以抑制TNF-α和NF-κB途徑。Shikonin通過抑制糖酵解降低外泌體(exosome)的分泌。Shikonin抑制AIM2炎性體活化。IC50&TargetTMEM16AchloridechannelPKM2NF-κB6.5μM(IC50)體外研究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].體內(nèi)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?邊的抑制劑?師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.戶使?本產(chǎn)品發(fā)表的科研?獻?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