TMPyP4-tosylate-TMP-1363-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETMPyP4tosylateCat.No.:HY-108477CASNo.:36951-72-1Synonyms:TMP1363分⼦式:C₇₂H₆₆N₈O₁₂S₄分⼦量:1363.6作⽤靶点:G-quadruplex;Telomerase;Cholinesterase(ChE);SARS-CoV作⽤通路:CellCycle/DNADamage;NeuronalSignaling;Anti-infection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H2O:25mg/mL(18.33mM;Needultrasonic)DMSO:10mg/mL(7.33mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM0.7334mL3.6668mL7.3335mL5mM0.1467mL0.7334mL1.4667mL10mM0.0733mL0.3667mL0.7334mL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%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥1mg/mL(0.73mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1mg/mL(0.73mM);Clearsolution3.请依序添加每种溶剂：PBSSolubility:7.14mg/mL(5.24mM);Clearsolution;Needultrasonicandwarmingandheatto60°CBIOLOGICALACTIVITY⽣物活性TMPyP4tosylate(TMP1363)⼀种四链体(G-quadruplex)特异性配体，可抑制G-四链体和IGF-1之间的相互作⽤。TMPyP4tosylate⼀种端粒酶(telomerase)抑制剂，且抑制肿瘤细胞增殖。TMPyP4tosylate也是核酸⼆级结构的稳定剂和⼄酰胆碱酯酶抑制剂。除此之外，TMPyP4tosylate对SARS-CoV-2有抗病毒活性。IC50&TargetAChEG-quadruplexTelomeraseSARS-CoV-2体外研究TMPyP4tosylate(50ꢀµM,96h)inhibitstelomeraseactivityintelomerasepositiveHOScells[2].TMPyP4tosylate(50ꢀµM,48or96h)inhibitsthegrowthofHOScells[2].TMPyP4tosylate(50ꢀµM,96h)inducescellapoptosisinHOS,Saos-2,MG-63,andU2OScelllines[2].TMPyP4tosylate(100ꢀµM,24or48h)increasescellcycleregulatoryproteinsandMAPKsinK562cells[4].CellViabilityAssay[2]CellLine:HOScellsConcentration:50ꢀµMIncubationTime:48or96hResult:Time-dependentlyinhibitedcellviability.WesternBlotAnalysis[4]CellLine:K562cellsConcentration:100ꢀµMIncubationTime:24or48hResult:Increasedtheexpressionofp21CIP1proteinandp57KIP2protein.体内研究TMPyP4tosylate(10and20mg/kg,i.p.,twotimesweekly)inhibitstumorgrowthinMX-1tumormodel[5].TMPyP4tosylate(15ꢀmg/kgor30ꢀmg/kg,i.n.)decreasesthemeanviralloadsinSARS-CoV-2-infectedhamster[6].TMPyP4tosylate(30ꢀmg/kg,i.n.,hamsters)showsaCmaxof17.88ꢀμg/mLat1h,andahalf-life(T1/2)of6.36ꢀh[6].2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:MX-1mammarychemoadjuvantmodel[5]Dosage:10and20mg/kgAdministration:Intraperitonealinjection(i.p.),twiceweekly.Result:Inhibitedtumorgrowthandprolongedmicesurvival.AnimalModel:SARS-CoV-2-infectedhamster[6]Dosage:15ꢀmg/kgor30ꢀmg/kgAdministration:i.n.,startingat1ꢀhpriortovirusinoculationandcontinuinguntil3dayspostinfectionResult:Decreasedthemeanviralloadsinthenasalwash,nasalturbinateandlungtissues.户使⽤本产品发表的科研⽂献•MicrobiolSpectr.2022Apr21;e0046022.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].FujiwaraN,etal.aStabilizerofNucleicAcidSecondaryStructure,IsaNovelAcetylcholinesteraseInhibitor.PLoSOne.2015Sep24;10(9):e0139167.[2].Mikami-TeraoY,etal.AntitumoractivityofG-quadruplex-interactiveagentTMPyP4inK562leukemiccells.CancerLett.2008Mar18;261(2):226-34.[3].GrandCL,etal.ThecationicporphyrinTMPyP4down-regulatesc-MYCandhumantelomerasereversetranscriptaseexpressionandinhibitstumorgrowthinvivo.MolCancerTher.2002Jun;1(8):565-73.Erratumin:MolCancerTher.2003Feb;2(2):208.[4].QinG,etal.RNAG-quadruplexformedinSARS-CoV-2usedforCOVID-19treatmentinanimalmodels.CellDiscov.2022Sep6;8(1):86.[5].ChenH,etal.Insuline-likegrowthfactortypeIselectivelybindstoG-quadruplexstructures.BiochimBiophysActaGenSubj.2019Jan;1863(1):31-38.[6].FujimoriJ,etal.AntitumoreffectsoftelomeraseinhibitorTMPyP4inosteosarcomacelllines.JOrthopRes.2011Nov;29(11):1