TPCA-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETPCA-1Cat.No.:HY-10074CASNo.:507475-17-4分⼦式:C₁₂H₁₀FN₃O₂S分⼦量:279.29作⽤靶点:IKK;STAT;Apoptosis作⽤通路:NF-κB;JAK/STATSignaling;StemCell/Wnt;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥100mg/mL(358.05mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.5805mL17.9025mL35.8051mL5mM0.7161mL3.5805mL7.1610mL10mM0.3581mL1.7903mL3.5805mL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%saline1/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥7.5mg/mL(26.85mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥7.5mg/mL(26.85mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥7.5mg/mL(26.85mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性TPCA-1⼀种有效，选择性的IKK-2抑制剂，IC50值为17.9nM。TPCA-1也STAT3磷酸化、DNA结合以及反式激活的有效抑制剂。IC50&TargetIKK-2STAT317.9nM(IC50)体外研究TPCA-1inhibitslipopolysaccharide-inducedhumanmonocyteproductionofTNF-α,IL-6,andIL-8withanIC50of170to320nM[1][2].TPCA-1(0-2μM)inhibitsSTAT3phosphorylationandtransactivationinducedbycytokinesandnonreceptortyrosinekinaseindose-andtime-dependentmanner.TPCA-1completelyinhibitsSTAT3phosphorylationwithoutchangingtotalSTAT3levels[3].TPCA-1increasedsensitivitytoZD1839inbothTKIsensitivecellsandinsensitivecells[3].CellViabilityAssay[2]CellLine:humanperipheralbloodmonocytesstimulatedwithLPS.Concentration:0-10μM.IncubationTime:~24hours.Result:TPCA-1InhibitsLPS-InducedTNF-α,IL-6,andIL-8productionbyhumanmonocytes.CellViabilityAssay[3]CellLine:HCC827andH1975cells.Concentration:0-10μM.IncubationTime:0.5-2hours.Result:SuppressedproliferationofHCC827andH1975cells.LedtoaG2-Mcell-cyclearrestinHCC827butnotA549.WesternBlotAnalysis[3]CellLine:HEK-293Tcelllines.Concentration:0-2μM(beforeIL-2orIFN-αtreatment).2/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIncubationTime:0.5-2hours.Result:InhibitedSTAT3phosphorylationandtransactivationinducedbycytokinesandnonreceptortyrosinekinaseindose-andtime-dependentmanner.体内研究TPCA-1(3,10,or20mg/kg,i.p.)resultsinadose-dependentreductionintheseverityofmurinecollagen-inducedarthritis(CIA)[2].TPCA-1(10mg/kg,i.p.daily)inhibitsgrowthofNSCLCwithEGFRmutationandpotentiatesantitumoreffectofZD1839inxenograftmodels[3].AnimalModel:10-12weeksoldmaleDBA/1OlaHsdmice[2].Dosage:3,10,or20mg/kg.Administration:I.P.,b.i.d,fromdays1to47.Result:ReducedtheseverityanddelaystheonsetofCIA.Attenuatedexvivoantigen-inducedTcellproliferationinCIA.AnimalModel:Six-week-oldBALB/cfemalenudemiceinjectedsubcutaneouslywithHCC827cells(5×106)[3].Dosage:10mg/kg.Administration:Intraperitoneallydaily.Result:ThetumorweightinhibitionrateofTPCA-1,ZD1839,andtheircombinationare0.419(ETPCA-1),0.680(EZD1839),and0.837(Eobserved),respectively.户使⽤本产品发表的科研⽂献•SignalTransductTargetTher.2021Apr24;6(1):167.•SciTranslMed.2018Jul18;10(450).pii:eaaq1093.•ACSNano.2015Dec22;9(12):11800-11.•ProcNatlAcadSciUSA.2019Feb19;116(8):2996-3005.•PharmacolRes.2020Jul;157:104800.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SachseF,etal.IKK-2inhibitorTPCA-1repressesnasalepithelialinflammationinvitro.Rhinology.2011Jun;49(2):168-73.[2].PodolinPL,etal.Attenuationofmurinecollagen-inducedarthritisbyanovel,potent,selectivesmallmoleculeinhibitorofIkappaB3/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEKinase2,TPCA-1(2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide),occursviareductionofproinflamm[3].NanJ,etal.TPCA-1isadirectdualinhibitorofSTAT3andNF-κBandregressesmutantEGFR-associatedhumannon-smallcelllungcancers.MolCancerTher.2014Mar;13