RSL3-1S-3R-RSL3-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemERSL3Cat.No.:HY-100218ACASNo.:1219810-16-8Synonyms:(1S,3R)-RSL3分⼦式:C₂₃H₂₁ClN₂O₅分⼦量:440.88作⽤靶点:GlutathionePeroxidase;Ferroptosis作⽤通路:MetabolicEnzyme/Protease;Apoptosis储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:100mg/mL(226.82mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2682mL11.3410mL22.6819mL5mM0.4536mL2.2682mL4.5364mL10mM0.2268mL1.1341mL2.2682mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMF>>90%cornoilSolubility:≥0.56mg/mL(1.27mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.72mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:5mg/mL(11.34mM);Suspendedsolution;Needultrasonic4.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.67mM);Clearsolution5.请依序添加每种溶剂：50%PEG300>>50%salineSolubility:20mg/mL(45.36mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性RSL3((1S,3R)-RSL3)⼀种⾕胱⽢肽过氧化物酶4(GPX4)的抑制剂(ferroptosis激动剂)，可降低GPX4的表达，诱导头颈部癌细胞的肥⼤性死亡。在HN3耐受细胞中，可增加p62和Nrf2的蛋⽩⽔平，使Keap1灭活[1]。IC50&TargetGlutathioneperoxidase4[1]体外研究RSL3(0-8μM,72hours)potentlyreducestheviabilityofHN3cells,withIC50sof0.48µMinHN3and5.8µMinHN3-rslRcells,respectively[1].RSL3(0-8μM,24hours)reducestheexpressionofGPX4protein,increasestheexpressionofp62andNrf2andinactivatesKeap1inHN3-rslRcells[1].CellViabilityAssay[1]CellLine:HN3cells,HN3-rslRcellsConcentration:0-8μMIncubationTime:72hoursResult:ShowedIC50sof0.48µMinHN3and5.8µMinHN3-rslRcells,respectively[1].WesternBlotAnalysis[1]CellLine:HN3-rslRcellsConcentration:0-8μMIncubationTime:24hoursResult:InhibitedGPX4expression,increasedp62andNrf2levels,anddecreasedKeap1levels.体内研究RSL3(100mg/kg,Intratumorallytwiceperweekfor20days)significantlyinhibitsthegrowthoftumorincombinationwithtrigonellineinmicebearingHN3Rcells.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:Ten-week-oldathymicBALB/cmalenudemice(nu/nu)bearingHN3Rcells[1]Dosage:100mg/kgincombinationwithtrigonelline(50mg/kg)Administration:Intratumorallytwiceperweekfor20daysResult:Significantlyreducedthevolumeoftumorcombinedwithtrigonellineinmice.户使⽤本产品发表的科研⽂献•CellDiscov.2022May3;8(1):40.•NatCancer.2022Apr;3(4):471-485.•AdvSci(Weinh).2022Nov29;e2203718.•ChemEngJ.15October2022,137110.•Small.2021Aug;17(32):e2101368.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ShinD,etal.Nrf2inhibitionreversesresistancetoGPX4inhibitor-inducedferroptosisinheadandneckcancer.FreeRadicBiolMed.2018Dec;129:454-462.McePdfHeightCaution:Producthasnotbeenf