Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEWogoninCat.No.:HY-N0400CASNo.:632-85-9分?式:C??H??O?分?量:284.26作?靶點(diǎn):CDK;Wnt;Autophagy;Apoptosis作?通路:CellCycle/DNADamage;StemCell/Wnt;Autophagy;Apoptosis儲(chǔ)存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:62.5mg/mL(219.87mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.5179mL17.5895mL35.1791mL5mM0.7036mL3.5179mL7.0358mL10mM0.3518mL1.7590mL3.5179mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)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(chǔ)備液可以根據(jù)儲(chǔ)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：0.5%CMC-Na/salinewaterSolubility:24mg/mL(84.43mM);Suspendedsolution;Needultrasonic2.請(qǐng)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:2.08mg/mL(7.32mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Wogonin?種天然酮類(lèi)物質(zhì)，能夠抑制CDK8和Wnt的活性，具有抗炎、抗腫瘤等功效。IC50&TargetCDK8體外研究Wogonin(0-200μM)exhibitsadose-andtime-dependentreducesincellviabilityofcaco-2,SW1116andHCT116cells.Wogonin(10-40μM)inducesG1phasearrestinHCT-116cells.WogoninalsosupressesWntsignalingpathwayinHCT116cells.WogonininterfersintheactivityoftranscriptionfactorTCF/Leffamily.Moreover,Wogonininhibitsβ-catenin-mediatedtranscriptionthroughsuppressingtheactivityofCDK8[1].WogoninshowscytotoxicandantiproliferativeeffectsonHeLacells.Wogonin(90μM)inducescellcyclearrestatG0-G1phase,andsuppressesthelevelsofcyclinD1andCdk4markedlyinHeLacells[2].Wogonin(1.25,2.5,5,10,20μg/ml)suppressesEtOH-inducedinflammatoryresponseinRAW264.7cells[3].體內(nèi)研究Wogonin(30,60mg/kg)reducestumorgrowthofHCT116cellsinaxenograftmodel[1].Wogonin(25,50,100mg/kg)protectsagainstliverinjuryandpathologicalcharacteristicsofALDinmice.WogoninactivatesPPAR-γexpressioninmicewithALDandEtOHinducedRAW264.7cells[3].PROTOCOLCellAssay[1]HCT116cellsareplantedona96-wellplate(1×105cellsperwell).Differentconcentrationsofwogoninareaddedandincubatedfor24h.Subsequently,20μLofMTTsolution(5mg/mL)istransferredtoeachwellandtheplatesareincubatedfor4hat37°Cand5%CO2.Thesupernatantisaspiratedoffand100μLDMSOisaddedtodissolvetheformazancrystal.Themixtureisshakenandmeasuredat570nmusingauniversalmicroplatereader.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalC57BL/6mice,male,6-8weeksold,weighing18-22gmicearehousedatcomfortableenvironmentandareAdministration[3]acclimatizedfor3daysbeforetheexperiment.Atotalof48micearerandomLydividedintosixgroupsof8animals,respectivelycontroldiet(CD)-fedmice,EtOH-fedmice,wogonin-treatedmiceatthedoseof25,50,100mg/kg/dayandthepositive(dexamethasone,1mg/kg/day)-treatedmice.Modelingprocesshasatotalof16daysincludingaliquiddietadaptationperiodfor3daysandmodelingfor13days.TheEtOH-fedmicearefedcontaining5%v/vethanolliquiddietsaddingcertainvitaminandcholinefor16days,andmicearegavagedwithasinglebingeethanoladministration(5g/kg,bodyweight,20%ethanol)atlastday.Atthesametime,thewogonin-treatedmiceandthepositive-treatedmicearenotonlyplustheethanoladministration,butalsoplusthemedicinesbygavagedaily,whereastheCD-fedmicearefedwithcontrolliquiddietsandgavagedwithisocaloricmaltose-dextrinatlastday.Alldietsarepreparedfreshdaily.9hafterthelastgavagealcohol,micearesacrificedunderanaesthesia,thelivertissuesandbloodarecollectedforfurtheranalysis.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE戶(hù)使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?PharmacolRes.2020May;155:104751.?OxidMedCellLongev.22Jun2021.?TranslStrokeRes.2020Sep12.?FoodChemToxicol.2022Oct5;113450.?JCellMolMed.2021Jun;25(12):5782-5798.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HeL,etal.WogonininducedG1cellcyclearrestbyregulatingWnt/β-cateninsignalingpathwayandinactivatingCDK8inhumancolorectalcancercarcinomacells.Toxicology.2013Oct4;312:36-47.[2].YangL,etal.WogonininducesG1phasearrestthroughinhibitingCdk4andcyclinD1concomitantwithanelevationinp21Cip1inhumancervicalcarcinomaHeLacells.BiochemCellBiol.2009Dec;87(6):933-42.[3].LiHD,etal.WogoninattenuatesinflammationbyactivatingPPAR-γinalcoholicliverdisease.