WEHI-345-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEWEHI-345Cat.No.:HY-18937CASNo.:1354825-58-3分⼦式:C₂₂H₂₃N₇O分⼦量:401.46作⽤靶点:RIPkinase作⽤通路:Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:25mg/mL(62.27mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4909mL12.4545mL24.9091mL5mM0.4982mL2.4909mL4.9818mL10mM0.2491mL1.2455mL2.4909mL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>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.23mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.23mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性WEHI-345⼀种有效的选择性RIPK2激酶抑制剂，IC50值为0.13μM。WEHI-345在寡聚化结构域(NOD)刺激下可延迟RIPK2的泛素化和NF-κB的活化。IC50&TargetIC50:0.13μM(RIPK2kinase)[1]体外研究WEHI-345(500nM;Raw267.4cells)isabletoinhibitMDP-inducedautophosphorylationactivityofRIPK2incells[1].WEHI-345(500nM;0hour,2hours,4hours,8hours;BMDMsorTHP-1cells)potentlyblocksMDP-inducedtranscriptionoftheinflammatorymediatorsTNFandinterleukin-6(IL-6)inbonemarrow-derivedmacrophages(BMDMs).InTHP-1cells,WEHI-345reducesmRNAlevelsofNF-kBtargetssuchasTNF,IL-8,IL-1bandA20[1].WesternBlotAnalysis[1]CellLine:Raw267.4cellsConcentration:500nMIncubationTime:Result:InhibitedMDP-inducedautophosphorylationactivityofRIPK2incells.RT-PCR[1]CellLine:BMDMsorTHP-1cellsConcentration:500nMIncubationTime:0hour,2hours,4hours,8hoursResult:BlockedMDP-inducedtranscriptionoftheinflammatorymediatorsTNFandinterleukin-6(IL-6)inBMDMs.AndreducedmRNAlevelsofNF-kBtargetsinTHP-1cells.体内研究WEHI-345(20mg/kg;intraperitonealinjection;twicedaily;for6days;C57BL/6malemice)treatmentreducesdiseasescore,inflammatoryinfiltrate,histologicalscoreandrecruitmentofdendriticcellstothesiteofinflammation.Andimprovesbodyweightandreducescytokineandchemokinelevels,indicatinganoverallimprovementoftheconditioninexperimentalautoimmuneencephalomyelitis(EAE)-inducedwild-typeC57Bl/6mice[1].AnimalModel:C57BL/6malemice(8-week-old)[1]2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEDosage:20mg/kgAdministration:Intraperitonealinjection;twicedaily;for6daysResult:Reduceddiseasescore,inflammatoryinfiltrate,histologicalscoreandrecruitmentofdendriticcellstothesiteofinflammation.Andimprovedbodyweightandreducedcytokineandchemokinelevels.户使⽤本产品发表的科研⽂献•MolCell.2018Feb15;69(4):551-565.e7.•JImmunol.2017May1;198(9):3729-3736.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].NachburU,etal.ARIPK2inhibitordelaysNODsignallingeventsyetpreventsinflammatorycytokineproduction.NatCommun.2015Mar17;6:6442.McePdfHeightCaution:Producthasnotbeenfullyv