Zunsemetinib-ATI-450-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEZunsemetinibCat.No.:HY-139553CASNo.:1640282-42-3Synonyms:ATI-450;CDD-450分⼦式:C₂₅H₂₂ClF₂N₅O₃分⼦量:513.92作⽤靶点:MAPKAPK2(MK2)作⽤通路:MAPK/ERKPathway储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(194.58mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9458mL9.7291mL19.4583mL5mM0.3892mL1.9458mL3.8917mL10mM0.1946mL0.9729mL1.9458mL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。BIOLOGICALACTIVITY⽣物活性Zunsemetinib(CDD-450)⼀种具有⼝服活性的p38α丝裂原激活蛋⽩激酶激活蛋⽩激酶2(MK2)通路抑制剂。Zunsemetinib可⽤于免疫炎症性疾病的研究[1]。IC50&TargetMK2[1]1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体外研究Zunsemetinib(1and10μM;1hour;WTandNOMIDBMMs)hasnoeffectonNLRP3expression,butdecreasesIL-1βexpressionbypromotingIL-1βmRNAdegradation[1].Zunsemetinib(0.4nM~1μM;16hours;PBMC)reducesIL-1βsecretionandpromotesIL-1βmRNAinstability[1].Zunsemetinibselectivelyblocksp38αMAPKactivationoftheproinflammatorykinaseMK2whilesparingp38αactivationofothereffectorssuchasPRAKandATF2.ZunsemetinibinhibitsinvitroosteoclastformationinducedbyRANKL[1].RT-PCR[1]CellLine:WTandNOMIDBMMsConcentration:1and10μMIncubationTime:1hourResult:HadnoeffectonNLRP3expression,butdecreasedIL-1βexpressionbypromotingIL-1βmRNAdegradation.体内研究Zunsemetinib(1,000ppm;p.o.)blocksLPS-inducedTNF-αexpressionpersistedforupto4weeksafterdosing[1].Zunsemetinib(10and20mg/kg;p.o.)increasesbonedensity[1].ZunsemetinibpreventsosteopeniainNOMIDcmicethroughinhibitionofosteoclastogenesis[1].AnimalModel:8-week-oldWTfemalemice[1]Dosage:1,000ppmAdministration:P.o.Result:BlockedLPS-inducedTNF-αexpressionpersistedforupto4weeksafterdosing.AnimalModel:Rats[1]Dosage:10and20mg/kgAdministration:P.o.Result:Increasedbonedensity.REFERENCES[1].Zunsemetinib(ATI-450)–InvestigationaloralMK2pathwayinhibitor[2].AclarisTherapeuticsAnnouncesATI-450(MK2pathwayInhibitor)publicationinJournalofExperimentalMedicine[3].WangC,etal.Selectiveinhibitionofthep38αMAPK-MK2axisinhibitsinflammatorycuesincludinginflammasomeprimingsignals.JExpMed.2018;215(5):1315-1325.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Fo