Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemESTAT3/NF-κB-IN-1Cat.No.:HY-175227分子式: C??H??N?O?S分子量: 542.61作用靶點: STAT;NF-κB;Apoptosis;Caspase;Bcl-2Family作用通路: JAK/STATSignaling;StemCell/Wnt;NF-κB;Apoptosis儲存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性 STAT3/NF-κB-IN-1是一種強效的STAT3和NF-κB抑制劑，其在4T1細(xì)胞中的IC50值分別為5.86(STAT3)和4.22μM(NF-κB)。STAT3/NF-κB-IN-1能夠通過上調(diào)關(guān)鍵的凋亡調(diào)節(jié)因子(caspases-3、9、Bax)以及下調(diào)Bcl-2的表達(dá)來誘導(dǎo)細(xì)胞凋亡(apoptosis)。STAT3/NF-κB-IN-1對乳腺癌細(xì)胞系具有顯著的抗癌活性，并能在體內(nèi)減少腫瘤體積。STAT3/NF-κB-IN-1可用于乳腺癌的研究[1]。IC50&TargetNF-κBSTAT3Caspase-3Caspase-94.22μM(IC50)5.86μM(IC50)Bcl-2Bax體外研究STAT3/NF-κB-IN-1(Compound12a)(72h)exhibitscytotoxicityagainst4T1,MDA-MB-231,MDA-MB-468andMCF-7cellswithIC50sof7.68,1.53,7.00and6.14μM,respectively[1].STAT3/NF-κB-IN-1(10μM,24h)significantlyinhibitscellmigrationandinvasionin4T1andMDA-MB-231cells[1].STAT3/NF-κB-IN-1(1-10μM,24-72h)significantlyinducesearlyMDA-MB-231cellapoptosiswithincreasementactivityofcaspase3/9andincreasementofBax/Bcl-2[1].STAT3/NF-κB-IN-1(1-5μM,48-96h)significantlyinhibitstheexpressionsofp-STAT3andNF-κB[1].CellMigrationAssay[1]CellLine:4T1andMDA-MB-231cellsConcentration:10μMIncubationTime:24h1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEResult:Showedthepercentageofscratchclosurecorrespondingtocellmigrationof15%.ApoptosisAnalysis[1]CellLine:MDA-MB-231Concentration:1,2.8,6and10μMIncubationTime:24,48and72hResult:Considerablyraisedthe%ofapoptoticcellspositivetoannexinVFITC.Increasedearly(rangingfrom0.55%to22.51%)andlateapoptosis(rangingfrom0.18%to16.07%).Haddose-dependent(1,2.8and6μMfor48h)andtimedependent(2.8μMfor24,48and72h)effectsoncaspase-9expression.WesternBlotAnalysis[1]CellLine:MDA-MB-231cellsConcentration:1,1.5,2and5μMIncubationTime:48,72and96hResult:Inhibitedthephosphorylationofp-STAT3Y705proteinaswellasslightlydownregulatetheexpressionleveloftotalSTAT3.ClearlysuppressedNF-κBproteinlevels.Haddose-dependent(1,2and5μMfor72h)andtime-dependenteffects(2μMfor48,72and96h)p-SAT3andNF-kBexpression.體內(nèi)研究STAT3/NF-κB-IN-1(Compound12a)(40mg/kg,s.c.,oncedailyfor12days)hassignificantantitumoractivityinehrlichsolidcarcinomamicemodel[1].AnimalModel:EhrlichsolidcarcinomamodelestablishedinBALB/cmice[1]Dosage:40mg/kgAdministration:Subcutaneousinjection(s.c.),oncedailyfor12daysResult:Decreasedthetumorvolumeby70-80%,andtherewasnosignificanttoxicity.REFERENCESAfifiOS,etal.Revisitingmulti-pathwaymodulationwiththeophyllinederivatives:TargetingSTAT3,NF-κB,andapoptoticsignalinginbreastcancer.BioorgChem.2025Jun30;163:108708.2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedform