FR900359-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEFR900359Cat.No.:HY-117037CASNo.:107530-18-7分子式:C₄₉H₇₅N₇O₁₅分子量:1002.16作用靶点:Others;Apoptosis;ERK作用通路:Others;Apoptosis;MAPK/ERKPathway;StemCell/Wnt储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性FR900359是一种酯肽，是哺乳动物Gαq/11/14的选择性抑制剂，能抑制ERK通路，能抑制黑色素瘤细胞增殖，降低血压。在Ovalbumins(HY-W250978)诱导的过敏性小鼠哮喘模型中，FR900359也能防止气道过度反应。FR900359可用于癌症和心血管疾病研究。体外研究FR900359(1.0μM,1hours)inhibitsGαq,Gα11andGα/14,butnotGα16oranyothermammalianGαisoforminHEK293cells[1].FR900359(0-10μM,24hours)effectivelyreducesgrowthofB16cellsandsuppressedcellproliferationandinhibitsmigrationinaconcentration-dependentmanner[1].FR900359(10nM,72hours)inducesG1cellcyclearrestinmelanomacellswithGqtoneandforcesmelanomacells(B16cells)intodifferentiation[1].FR900359(1.0μM,5min)interdictstheactivationofextracellularsignal-regulatedkinases1and2(ERK1/2)thatbelargelyGq-mediated28[1].FR900359(1μM,24hours)significantlyinducesmore92.1cellsundergoingapoptosiscomparedtountreated[3].FR900359(30nM,60min)inducesdose-dependentrelaxationofmurine,porcine,andhumanairwaysexvivo[4].CellProliferationAssay[1]CellLine:B16cellsConcentration:0-10μMIncubationTime:24hours1/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEResult:EffectivelyreducedgrowthofB16cellsinaconcentration-dependentmannerandsuppressedcellproliferationandmigration.CellDifferentiationAssay[1]CellLine:B16cellsConcentration:10nMIncubationTime:72hoursResult:InducedG1cellcyclearrestinmelanomacellswithGqtone.Treatedcellsappearedflattened,ratherdark,andpackedwithmelaninvesicles,attributesconsistentwiththeadoptionofamoredifferentiatedstate.Mademelanocytedifferentiationmarkergp100wasupregulatedconsiderablyonFRtreatment.WesternBlotAnalysis[1]CellLine:HEK293cellsConcentration:1.0μMIncubationTime:5minResult:FRinterdictsGq-dependentERK1/2activationApoptosisAnalysis[3]CellLine:92.1cellsConcentration:1.0μMIncubationTime:24hoursResult:Significantlyinducedmore92.1cellsundergoingapoptosiscomparedtountreatedcells体内研究FR900359(0.2or1mg/ml,12μLpermouse,i.v.)stronglyreducesvasculartoneinmousetailartery[1].FR900359(0.1mg/ml,2.5mg/mouse,intratracheally)abolishesairwayhyperreactivityafterOvalbumin(HY-W250978)-inducedsensitizationinmice[4].AnimalModel:Isometricforcemeasurementsinmousetailartery[1]Dosage:1.0μMAdministration:Washed2/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEResult:StronglyreducedvasculartoneAnimalModel:Ovalbumins–inducedsensitizationmodelofasthma.[4]Dosage:0.1mg/ml,2.5mgpermouseAdministration:IntratracheallyResult:Abolishedairwayhyperreactivityafterovalbumin-inducedsensitizationinmiceREFERENCESSchrageR,et.al.TheexperimentalpowerofFR900359tostudyGq-regulatedbiologicalprocesses.NatCommun.2015Dec14;6:10156.Fujioka,M,et.al.StructureofFR900359,acyclicdepsipeptidefromArdisiacrenatasimsJ.Org.Chem.1988,53(12),2820−2825.LapadulaD,et.al.EffectsofOncogenicGαqandGα11InhibitionbyFR900359inUvealMelanoma.MolCancerRes.2019Apr;17(4):963-973.MattheyM,et.al.TargetedinhibitionofGqsignalinginducesairwayrelaxationinmousemodelsofasthma.SciTranslMed.2017Sep13;9(407):eaag2288.McePdfHeightCaution:Producthasno