Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGYY4137(GMP)Cat.No.:HY-107632GCASNo.:106740-09-4分?式:C??H??N?O?PS?分?量:376.47作?靶點:Apoptosis;STAT;NF-κB;TNFReceptor;NOSynthase;InterleukinRelated;COX作?通路:Apoptosis;JAK/STATSignaling;StemCell/Wnt;NF-κB;Immunology/Inflammation儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性GYY4137(GMP)GMP級別的GYY4137(HY-107632)。GMP級別的?分?可?做細胞療法中的輔助試劑。GYY4137(GMP)?種緩釋H2S供體，具有?管擴張、抗??壓活性和抗炎活性。GYY4137(GMP)能通過阻斷STAT3通路，從?抑制細胞?長、誘導了細胞凋亡(apoptosis)和細胞周期停滯，表現出強效的抗癌活性[1][2][3][4][5][6]。IC50&TargetStat-3體外研究GYY4137(GMP)(400-800μM)causesconcentration-dependentkillingofsevendifferenthumancancercelllines(HeLa,HCT-116,HepG2,HL-60,MCF-7,MV4-11andU2OS)butdidnotaffectsurvivalofnormalhumanlungfibroblasts(IMR90,WI-38)[2].GYY4137(GMP)(0.1-0.5mM)decreasesLPS-inducedproductionofnitrite(NO2),PGE2,TNF-αandIL-6fromhumansynoviocytes(HFLS)andarticularchondrocytes(HAC),reducesthelevelsandcatalyticactivityofinduciblenitricoxidesynthase(iNOS)andcyclooxygenase-2(COX-2)andreducedLPS-inducedNF-κBactivation[3].CellViabilityAssay[2]CellLine:HeLa,HCT-116,HepG2,HL-60,MCF-7,MV4-11andU2OSConcentration:400or800μMIncubationTime:5days1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:Significantlyaffectedcancercellsurvivability.體內研究GYY4137(GMP)(100-300mg/kg;i.p.;dailyfor14days)significantlyreducesthetumorvolumeinbothanimalmodels,inadose-dependentmanner[2].InthecompleteFreund'sadjuvant(CFA)-treatedmouse,GYY4137(GMP)(50mg/kg,i.p.)injected1hrpriortoCFAincreasedkneejointswellingwhileananti-inflammatoryeffect,asdemonstratedbyreducedsynovialfluidmyeloperoxidase(MPO)andN-acetyl-β-D-glucosaminidase(NAG)activityanddecreasedTNF-α,IL-1β,IL-6andIL-8concentration,wasapparentwhenGYY4137(GMP)wasinjected6hrsafterCFA[3].GYY4137(GMP)significantlyinhibitedtumorgrowthinthesubcutaneousHepG2xenograftmodelbyinhibitingSTAT3activationanditstargetgeneexpression[4].GYY4137(GMP)preventsnitrativestressandα-synucleinnitrationinanMPTPmousemodelofparkinson’sdisease[5].AnimalModel:Female,severecombinedimmunodeficiency(SCID)mice(bearingHL-60orMV4-11cells)[2]Dosage:100,200and300mg/kgAdministration:i.p.;dailyfor14daysResult:Reducedtumorvolumeby52.5%and55.3%inHL-60andMV4–11injectedanimals.戶使?本產品發表的科研?獻?CellCommunSignal.2024Jan12;22(1):33.?AntioxidRedoxSignal.2024Jun15.?Molecules.2023Jun14,28(12),4770.?NitricOxide.8October2022.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LiL,etal.Characterizationofanovel,water-solublehydrogensulfide-releasingmolecule(GYY4137):newinsightsintothebiologyofhydrogensulfide.Circulation.2008;117(18):2351-2360.[2].LeeZW,etal.Theslow-releasinghydrogensulfidedonor,GYY4137,exhibitsnovelanti-cancereffectsinvitroandinvivo.PLoSOne.2011;6(6):e21077.[3].LiL,etal.Thecomplexeffectsoftheslow-releasinghydrogensulfidedonorGYY4137inamodelofacutejointinflammationandinhumancartilagecells.JCellMolMed.2013;17(3):365-376.[4].LuS,GaoY,etal.GYY4137,ahydrogensulfide(H?S)donor,showspotentanti-hepatocellularcarcinomaactivitythroughblockingtheSTAT3pathway.IntJOncol.2014;44(4):1259-1267.[5].HouX,etal.GYY4137,anH2SSlow-ReleasingDonor,PreventsNitrativeStressandα-SynucleinNitrationinanMPTPMouseModelof2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEParkinson'sDisease.FrontPharmacol.2017;8:741.Published2017Oct30.[6].LuS,etal.GYY4137,ahydrogensulfide(H2S)donor,showspotentanti-hepatocellularcarcinomaactivitythroughblockingtheSTAT3pathway[J].Internationaljournalofoncology,2014,44(4):1259-1267.McePdfHeigh