IWP-2-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEIWP-2Cat.No.:HY-13912CASNo.:686770-61-6分⼦式:C₂₂H₁₈N₄O₂S₃分⼦量:466.6作⽤靶点:Wnt;Porcupine;CaseinKinase作⽤通路:StemCell/Wnt;CellCycle/DNADamage储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:2mg/mL(4.29mM;Needultrasonic)扫描⼆维码，H2O:<0.1mg/mL(insoluble)运⽤溶解⽅案计算器获得适合您实验体系的溶解⽅案MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1432mL10.7158mL21.4316mL5mM---------10mM---------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，并请注意储备液的保存⽅式和期限。BIOLOGICALACTIVITY⽣物活性IWP-2Wnt加⼯和分泌的抑制剂，其IC50为27nM。IWP-2靶向膜结合的O-酰转移酶porcupine(Porcn)，从⽽阻⽌关键的Wnt配体棕榈糖化。IWP-2还⼀种具有ATP竞争能⼒的CK1δ抑制剂，对于M82FCK1δ的IC50为40nM。IC50&TargetWntCK1δ27nM(IC50)40nM(IC50)体外研究IWP-2inhibitstheproliferationoftheinvestigatedcelllineswithinthesingledigitμMrange.IWP-2inhibits1/3www.MedChemEwww.MedChemEcellproliferationinA818-6,MiaPaCa2,Panc-1,Panc-89,HT29,HEK293,SW620andCapancellwithEC50sof8.96μM,1.90μM,2.33μM,3.86μM,4.67μM,2.76μM,1.90μMand2.05μM,respectively[2].Panc-1cellsareeitheruntreatedortreatedwith2.33μMIWP-2for48h.InIWP-2treatedcells,theCK1δkinasepeakactivityisreducedtoapproximately66%residualactivitycomparedtotheactivityinuntreatedcells,respectively.IWP-2reducestheactivityofCK1δinPanc1cells[2].体内研究ToevaluatetheefficacyofIWP-2invivo,200μLeachofIWP-2-liposomeorfreeliposomeiseparatelyinjectedintoC57BL/6miceintraperitoneallyabout2hbeforeinjectionofasimilarvolumeofeitherblue-dye-filledlatexbeadsorE.coliDH5α.IWP-2causessignificantreductionintheuptakeofbluebeadsaswellasE.coliasassessedbyCFUsinperitoneallavagecellswithin2h.Inaddition,thelevelsofTNF-αandIL-6inthelavagefluidofthecorrespondingmicearereducedby2-4-foldcomparedwithcontrolvalues.Interestingly,IWP-2eveninducesaconsiderableincreaseinsecretionoftheanti-inflammatorycytokineIL-10[3].PROTOCOLCellAssay[2]ThehumanRCCcelllines786OandCaki-2(5×103)areseededinto96-wellplates.CellviabilityisestimatedbyMSTassayafterCaki-2acellsareincubatedwithncreasingconcentrationsofLEFtogetherwith20μMIWP-2for48h.Aftertreatment,10μLMTSisaddedintoeachwellfor2hincubation.TheabsorbanceismeasuredusingamodelELX800MicroPlateReaderat490nm.Forcolonyformationassay,Caki-2cellsaretrypsinizedtosinglecellsuspensionsandseededintofresh6-wellplatesat1000cells/well.ThencellsareincubatedwithLEFatdepictedconcentrationsfor7days.Coloniesarefixedwithabsolutemethanolfor15minandthenstainedwith0.1%crystalvioletfor20min.AfterwashingwithPBSthreetimes,thecolonieswithadiameterover2mmarevisualizedbyadigitalcamera[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•DevCell.2020Nov10;S1534-5807(20)30835-2.•StemCellsTranslMed.2021May;10(5):743-755.•JCellPhysiol.2020Jul;235(7-8):5811-5822.•BiochemPharmacol.2019Nov;169:113608.•ACSCombSci.2019Dec9;21(12):805-816.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ChenB,etal.Smallmolecule-mediateddisruptionofWnt-dependentsignalingintissueregenerationandcancer.NatChemBiol.2009Feb;5(2):100-7.[2].MaitiG,etal.TheWinglesshomologWnt5astimulatesphagocytosisbutnotbacterialkilling.ProcNatlAcadSciUSA.2012Oct9;109(41):16600-5.[3].García-ReyesB,etal.DiscoveryofInhibitorofWntProduction2(IWP-2)andRelatedCompoundsAsSelectiveATP-Competitive2/3www.MedChemEwww.MedChemEInhibitorsofCaseinKinase1(CK1)δ/ε.JMedChem.2018May10;61(9):4087-4102.McePdfHeight关注MCE中国公众号，

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