Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEEprenetapoptCat.No.:HY-19980CASNo.:5291-32-7Synonyms:APR-246;PRIMA-1Met分?式:C??H??NO?分?量:199.25作?靶點(diǎn):MDM-2/p53;Autophagy;Apoptosis;Ferroptosis作?通路:Apoptosis;Autophagy儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(501.88mM;Needultrasonic)H2O:50mg/mL(250.94mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM5.0188mL25.0941mL50.1882mL5mM1.0038mL5.0188mL10.0376mL10mM0.5019mL2.5094mL5.0188mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(12.55mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(12.55mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(12.55mM);Clearsolution4.請(qǐng)依序添加每種溶劑：PBSSolubility:100mg/mL(501.88mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Eprenetapopt(APR-246)?創(chuàng)的在TP53突變細(xì)胞中恢復(fù)野?型p53功能的?分?。Eprenetapopt引發(fā)腫瘤細(xì)胞凋亡。Eprenetapopt還抑制硒蛋?硫氧還蛋?還原酶1(TrxR1)。IC50&Targetp53activator[1]TrxR1inhibitor[1]體外研究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].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?SciAdv.2022Sep16;8(37):eabm9427.?CellBiosci.2022Feb25;12(1):20.?Cancers.2021Feb2;13(3):581.?ResearchSquarePreprint.2021Jan.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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