CIGB-552-TFA-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECIGB-552TFACat.No.:HY-P11115A分⼦式:C₁₃₁H₁₉₈N₃₈O₂₄·xC₂HF₃O₂Sequence:Ac-His-Ala-Arg-Ile-Lys-{d-Pro}-Thr-Phe-Arg-Arg-{d-Leu}-Lys-Trp-Lys-Tyr-Lys-Gly-Lys-Phe-TrpSequenceShortening:Ac-HARIK-{d-Pro}-TFRR-{d-Leu}-KWKYKGKFW作⽤靶点:Apoptosis;NF-κB;ReactiveOxygenSpecies(ROS)作⽤通路:Apoptosis;NF-κB;Immunology/Inflammation;MetabolicEnzyme/Protease储存⽅式:Sealedstorage,awayfrommoisturePowder-80°C2years-20°C1yearInsolvent-80°C6months-20°C1monthBIOLOGICALACTIVITY⽣物活性CIGB-552TFA⼀种具有抗肿瘤特性的细胞穿透肽，在H460细胞中的IC50为23μM。CIGB-552TFA可以增加COMMD1蛋⽩的⽔平。CIGB-552TFA显著抑制NF-κB信号通路。CIGB-552TFA可以促进肿瘤细胞的凋亡(apoptosis)。CIGB-552TFA可以诱导肿瘤细胞中活性氧(ROS)的积累。CIGB-552TFA具有抗炎和抗⾎管⽣成作⽤。CIGB-552TFA可⽤于肺癌和结肠癌的研究[1][2][3][4]。体外研究CIGB-552TFA(20-60μM,5h)canincreasetheproteincontentoftheanti-tumorrelatedproteinCOMMD1[1].CIGB-552TFA(25μM,0-12h)promotestheubiquitinationdegradationofRelAandinhibitsNF-κBsignalinginH460cells[1].CIGB-552TFA(25μM,0-24h)canincreasethelevelofproapoptoticproteinsandreducethelevelofantiapoptoticproteinsinH460cells[1].CIGB-552TFA(25μM,24-48h)caninduceapoptosisinlungcancercells[1].CIGB-552TFA(25μM,8h)reducescellularantioxidantcapacity,leadingtoproteinandlipidoxidativedamageinH460cells[1].CIGB-552TFA(37.5μM,1h)inducestheaccumulationofreactiveoxygenspecies(ROS)byinhibitingSOD1activity,selectivelykillingtumorcells[2].CIGB-552TFA(75-150μM,24h)cansignificantlyinhibitTNF-α-inducedNF-κBactivation[3].CIGB-552TFA(2.5-25μM,24h)exertsantiangiogeniceffectsbyinhibitinghypoxiainducedHIF-1activationthroughCOMMD1[3].CellViabilityAssay[1]CellLine:H460,H-125,H-82,LS174T,MDA-231andPBMCcells1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEConcentration:0-200μMIncubationTime:48hResult:HadbettercytotoxicityagainstH460(IC50=23μM,H-125(IC50=42μM),H-82(IC50=15μM),LS174T(IC50=22μM),MDA-231(IC50=40μM)andPBMC(IC50=249μM)cellscomparedtothecontrolgroup.WesternBlotAnalysis[1]CellLine:H460cellsConcentration:25μMIncubationTime:24hResult:IncreasedthelevelofproteinBax,decreasedtheamountofproteinBcl-2,andactivatedCaspase-3andPARPcleavage.WesternBlotAnalysis[1]CellLine:H460,MCF7,andHT29cellsConcentration:20-60μM,MG132(HY-13259)asacontrolgroupIncubationTime:20-60μM,MG132(HY-13259)asacontrolgroupResult:IncreasedtheproteinlevelofCOMMD1inthreetypesofcancercells.ApoptosisAnalysis[1]CellLine:H460cellsConcentration:25μMIncubationTime:24,48hResult:Significantlyincreasedtheapoptosisrateofcellscomparedtothecontrolgroup.体内研究CIGB-552TFA(1mg/kg;s.c.;threetimesaweek;forthreeweeks)significantlyinhibitstumorgrowthinthelungcancermiceandprolongssurvivalwithoutcausingsignificanttoxicity[2].CIGB-552TFA(0.2-1.4mg/kg;s.c.;twotimesaweek;fortwoweeks)significantlyinhibitstumorgrowthinmicewithcoloncancerandhasantiangiogeniceffects[4].AnimalModel:5×104TC-1cellsinjectedtheC57/BL6femalemice(8weeks,18-20g)[2]Dosage:1mg/kg,combinationwith0.4mg/kgCisplatin(HY-17394)2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAdministration:Subcutaneousinjection(s.c.);threetimesaweekforthreeweeksResult:Significantlyreducedtumorvolumeofthecancermice.Improvedthesurvivalrateofthecancermice.AnimalModel:7×104CT-26cellsinjectedtheBALB/cmice[4]Dosage:0.2or0.7mg/kgAdministration:Subcutaneousinjection(s.c.);twotimesaweekfortwoweeksResult:Inhibitedthetumorvolumeoftumormiceandcausedapoptosisofcellsatthetumorsite.AnimalModel:1×107HT-29cellsinjectedthefemaleathymicnu/nu(nude)mice[4]Dosage:0.7or1.4mg/kgAdministration:Subcutaneousinjection(s.c.);twotimesaweekfortwoweeksResult:Inhibitedthetumorvolumeoftumormiceandreducedtumormicrovasculardensity.REFERENCES[1].FernándezMassóJR,etal.TheAntitumorPeptideCIGB-552IncreasesCOMMD1andInhibitsGrowthofHumanLungCancerCells.JAminoAcids.2013;2013:251398.[2].GomezRodriguezY,etal.SynergiceffectofanticancerpeptideCIGB-552andCisplatininlungcancermodels.MolBiolRep.2022Apr;49(4):3197-3212.[3].DagheroH,etal.TheAnticancerPeptideCIGB-552ExertsAnti-InflammatoryandAnti-AngiogenicEffectsthroughCOMMD1.Molecules.2020Dec31;26(1):152.[4].VallespíMG,etal.Antitumorefficacy,pharmacokineticandbiodistributionstudiesoftheanticancerpeptideCIGB-552inmousemodels.JPeptSc