TPI-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETPI-1Cat.No.:HY-100463CASNo.:79756-69-7分⼦式:C₁₂H₆Cl₂O₂分⼦量:253.08作⽤靶点:Phosphatase作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(197.57mM;Needultrasonic)H2O:<0.1mg/mL(ultrasonic;warming;heatto60°C)(insoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.9513mL19.7566mL39.5132mL5mM0.7903mL3.9513mL7.9026mL10mM0.3951mL1.9757mL3.9513mL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.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:≥2.5mg/mL(9.88mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(9.88mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(9.88mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性TPI-1SHP-1的抑制剂；抑制重组SHP-1的IC50值为40nM。IC50&TargetIC50:40nM(recombinantSHP-1)[1]体外研究SHP-1hasbeenimplicatedasapotentialcancertherapeutictarget.TPI-1iseffectivestartingat10ng/mLinincreasingSHP-1phospho-substratespLck-pY394.TPI-1selectivelyincreasesSHP-1phospho-substrates(pLck-pY394,pZap70andpSlp76)inJurkatTcellsbuthaslittleeffectsonpERK1/2orpLck-pY505.TPI-1inducesmousesplenic-IFNγ+cellsandinducesIFNγ+cellsinhumanperipheralblood[1].体内研究TPI-1inhibitsthegrowthofB16melanomatumorsinmiceatatoleratedoraldoseinaTcell-dependentmannerbuthaslittleeffectsonB16cellgrowthinculture.TPI-1thusalsoincreasespLck-pY394andIFNγ+cellsinmice.TPI-1alsoinhibitsB16tumorgrowthandprolongstumormicesurvivalasatolerateds.c.agent[1].PROTOCOLAnimalMice:ForinvivoinductionofpLck-pY394andIFNγ+cellsinmice,C57BL/6JmicearetreatedwithPBSorAdministration[1]TPI-1(1or3mg/kg,s.c.)for4days.Spleensareharvestedonehourpost-treatmentonday4andprocessedintosplenocytes,whichareusedforassessingpLck-pY394levelsbySDS/WesternblottingandforquantificationofIFNγ+cellsbyELISPOTassays.MicearealsotreatedwithTPI-1(10mg/kg,daily,s.c.)toevaluatethetoxicityofthecompoundsinvivo[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•CancerRes.(2022)82(10):1991-2002.•JAllergyClinImmunol.2021Jun15;S0091-6749(21)00936-2.•JNeuroinflammation.2020Mar9;17(1):81.•FrontImmunol.21January2021.•IntImmunopharmacol.2022Jul16;110:109063.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].KunduS,etal.NovelSHP-1inhibitorstyrosinephosphataseinhibitor-1andanalogswithpreclinicalanti-tumoractivitiesastoleratedoralagents.JImmunol.2010Jun1;184(11):6529-36.McePdfHeightCaution:Producthasnotbeenfullyv