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Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemE(-)-EpigallocatechinGallateCat.No.:HY-13653CASNo.:989-51-5Synonyms:EGCG;EpigallocatecholGallate分?式:C??H??O??分?量:458.37作?靶點(diǎn):EndogenousMetabolite;Apoptosis作?通路:MetabolicEnzyme/Protease;Apoptosis儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥30mg/mL(65.45mM)H2O:20mg/mL(43.63mM;Needultrasonic)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.1816mL10.9082mL21.8164mL5mM0.4363mL2.1816mL4.3633mL10mM0.2182mL1.0908mL2.1816mL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。-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1/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE、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:10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.54mM);Clearsolution2.請(qǐng)依序添加每種溶劑:10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.54mM);Clearsolution3.請(qǐng)依序添加每種溶劑:10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.54mM);Clearsolution4.請(qǐng)依序添加每種溶劑:PBSSolubility:9.09mg/mL(19.83mM);Clearsolution;Needultrasonicandwarmingandheatto60°CBIOLOGICALACTIVITY?物活性(-)-EpigallocatechinGallatesulfate(EGCG)綠茶中的?種主多酚,可抑制細(xì)胞增殖并誘導(dǎo)細(xì)胞凋亡。(-)-EpigallocatechinGallatesulfate可抑制?氨酸脫氫酶1/2(GDH1/2,GLUD1/2)的活性。(-)-EpigallocatechinGallatesulfate對(duì)結(jié)直腸癌、髓性??病、甲狀腺癌等多種癌癥具有有效的抗癌、抗氧化和抗炎特性[1][2][3][4]。IC50&TargetEGFRHER2HER3體外研究(-)-EpigallocatechinGallate(EGCG,10-60μM)inhibitsthegrowthofFB-2andWROcellsinadose-dependentmanner[1].(-)-EpigallocatechinGallate(10-60μM,0-24h)reducescyclinD1andphosphorylationofAKTandERK1/2,andincreasesp21andp53expression[1].(-)-EpigallocatechinGallate(10-60μM,12h)reducescellmotilityandmigration[1].(-)-EpigallocatechinGallate(0-20μM,0-20minapproximately)inhibitsGLUD1/2andIDH1activityinaconcentrationandtime-dependentway(biochemicalassays)[2].(-)-EpigallocatechinGallate(0-35μg/mL,24-72h)inhibitstheproliferationofcolorectalcancercells(LoVo,SW480,HT-29,HCT-8cells),increasescellapoptosisandblockscellsattheG0/G1phase[3].(-)-EpigallocatechinGallate(30μM,3-24h)suppressestheexpressionofCOX-2andmPGES-1mRNAs,prostaglandinE2productioninLPS-inducedosteoblasts[4].CellProliferationAssay[1]CellLine:FB-2andWROcells(serum-starvedfor48h)Concentration:10,40,60μM.IncubationTime:4daysResult:Inhibitedbasalcellproliferation(40%inFB-2and35%inWRO)at10μM,inhibitedcellnumber(by68%to73%)at40and60μM).WesternBlotAnalysis[1]CellLine:FB-2cellsConcentration:10,40,60μM.2/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEIncubationTime:24hResult:ReducedcyclinD1level,phosphorylationofAKTandERK1/2.Inducedtheexpressionofp21andp53,andE-cadherin,N-cadherin,Vimentinandα5-integrin.CellMigrationAssay[1]CellLine:FB-2andWROcells(serum-starvedfor48h)Concentration:10,40,60μM.IncubationTime:12hResult:ReducedmigrationactivityinFB-2andWROcells.RT-PCR[4]CellLine:Mouseprimaryosteoblasts(1ng/mlLPS-treated)Concentration:30μMIncubationTime:3,6,12,24hResult:SuppressedtheLPS-inducedexpressionofCOX-2andmPGES-1mRNAs,prostaglandinE2production.體內(nèi)研究(-)-EpigallocatechinGallate(Intragastricaladministration,5-20mg/kg,oncedailyfor14days,orthotopictransplantmodel)decreasestumorsgrowth[3].(-)-EpigallocatechinGallate(Injectedintothemouselowergingiva,asingledoseof0.5mg/mouse,experimentalperiodontitismodel)decreasesinhibitstheLPS-inducedlossofbonemineraldensity(BMD)[3].AnimalModel:OrthotopictransplantBALB/cnudemicemodel[3]Dosage:5,10,and20mg/kg,oncedailyfor14days.Administration:Intragastricaladministration.Result:Inhibitedtumorsgrowthwithnoliverorlungmetastases.AnimalModel:Modelofexperimentalperiodontitis,LPS(25μg/mouse)[4]Dosage:0.5mg/mouse,asingledose.Administration:InjectedintothemouselowergingivaResult:InhibitedtheLPS-inducedlossofbonemineraldensity(BMD)inmice.3/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE戶(hù)使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?Biomaterials.2021,120952.?CancerRes.2022Jul27;CAN-22-0042.?AgingCell.2020Oct;19(10):e13217.?AntiviralRes.2022Jun;202:105325.?BrJCancer.2021Jan;124(2):425-436.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].DeAmicisF,etal.EpigallocatechingallateinhibitsgrowthandEpithelial-to-MesenchymalTransitioninhumanthyroidcarcinomacelllines.JCellPhysiol.2013Apr1.[2].PeetersTH,etal.Isocitratedehydrogenase1-mutatedcancersaresensitivetothegreenteapolyphenolepigallocatechin-3-gallate.CancerMetab.2019May20;7:4.[3].JinH,etal.EpigallocatechingallateinhibitstheproliferationofcolorectalcancercellsbyregulatingNotchsignaling.OncoTargetsTher.2013;6:145-53.[4].TsukasaTominari;Epigallocatechingallate(EGCG)suppresseslipopolysaccharide-inducedinflammatoryboneresorption,andprotectsagainstal

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