Eprenetapopt-APR-246-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEprenetapoptCat.No.:HY-19980CASNo.:5291-32-7Synonyms:APR-246;PRIMA-1Met分⼦式:C₁₀H₁₇NO₃分⼦量:199.25作⽤靶点:MDM-2/p53;Autophagy;Apoptosis;Ferroptosis作⽤通路:Apoptosis;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(501.88mM;Needultrasonic)H2O:50mg/mL(250.94mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM5.0188mL25.0941mL50.1882mL5mM1.0038mL5.0188mL10.0376mL10mM0.5019mL2.5094mL5.0188mL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。-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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(12.55mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(12.55mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(12.55mM);Clearsolution4.请依序添加每种溶剂：PBSSolubility:100mg/mL(501.88mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Eprenetapopt(APR-246)⾸创的在TP53突变细胞中恢复野⽣型p53功能的⼩分⼦。Eprenetapopt引发肿瘤细胞凋亡。Eprenetapopt还抑制硒蛋⽩硫氧还蛋⽩还原酶1(TrxR1)。IC50&Targetp53activator[1]TrxR1inhibitor[1]体外研究EprenetapoptinhibitsbothrecombinantTrxR1invitroandTrxR1incells.CellularTrxR1activityisinhibitedbyEprenetapoptirrespectiveofp53status.EprenetapoptcandirectlyaffectcellularredoxstatusviatargetingofTrxR1.Severalsmallmoleculeshavebeenshowntorestorewild-typeactivitytomutantp53,includingCP-31398,PRIMA-1andEprenetapopt,MIRA,STIMA,PhiKan-083andNSC319726.PRIMA-1anditsmethylatedanalogEprenetapoptpromotecorrectfoldingofmutantp53,inducecelldeathbyapoptosis,andinhibittumorgrowthinmice.Eprenetapopthasalsobeenshowntoreactivatemutantformsofthep63andp73proteinsthatsharehighstructuralhomologywithp53[1].Eprenetapoptisapowerfulapoptosis-inducingagent.Eprenetapoptcanenhanceapoptosisinmutantp53carryingcells,comparedtothep53nullparentalcells.Mostp53mutantsareincomplexwithHsp70proteins.EprenetapopttreatmentincreasesHsp70expressionandnucleolartranslocation,inparallelwiththeinductionofnucleolaraccumulationofmutantp53.SeverallinesofevidencesuggestthatEprenetapoptcanalsoactindependentlyofthep53statusofthecell.Itcanradiosensitizeprostatecarcinomacelllineswithmutantorwildtypep53andp53-/-cellsaswell.Introductionofmutantp53(p53ser249orp53gln248)intop53-/-hepatocarcinomacellsincreasessensitivitytoEprenetapoptwithouttheinductionofp53targetgenes.Eprenetapoptregularlyinducesapoptosisinmutantp53expressingcells[2].户使⽤本产品发表的科研⽂献•SciAdv.2022Sep16;8(37):eabm9427.•CellBiosci.2022Feb25;12(1):20.•Cancers.2021Feb2;13(3):581.•ResearchSquarePreprint.2021Jan.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].PengX,etal.APR-246/PRIMA-1METinhibitsthioredoxinreductase1andconvertstheenzymetoadedicatedNADPHoxidase.CellDeathDis.2013Oct24;4:e881.[2].StuberG,etal.PRIMA-1METinducesnucleolartranslocationofEpstein-Barrvirus-encodedEBNA-5protein.MolCancer.2009Mar26;8:23.[3].SallmanDA,etal.Eprenetapopt(APR-246)andAzacitidineinTP53-MutantMyelodysplasticSyndromes.JClinOncol.2021;39(14):1584-1594.McePdfHeightCaution:P