PROTAC-BRAF-V600E-degrader-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPROTACBRAF-V600Edegrader-1Cat.No.:HY-137487CASNo.:2417296-84-3分⼦式:C₄₈H₅₄F₂N₁₀O₁₀S分⼦量:1001.07作⽤靶点:PROTACs;Raf作⽤通路:PROTAC;MAPK/ERKPathway储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性PROTACBRAF-V600Edegrader-1⼀种有效的PROTACBRAF-V600E降解剂，对BRAF和BRAF-V600E的Kd分别为2.4nM和2nM。PROTACBRAF-V600Edegrader-1通过泛素-蛋⽩酶体系统(UPS)降解BRAF-V600E。PROTACBRAF-V600Edegrader-1可抑制⿊⾊素瘤细胞的⽣长。IC50&TargetBRAF-V600EBraf2nM(Kd)2.4nM(Kd)体外研究PROTACBRAF-V600Edegrader-1(compound23)(1nM-10μM;72h)inhibitsthecellviabilityofA375andHT-29[1].PROTACBRAF-V600Edegrader-1(1-1000nM;16hor0-24h)inhibitsp-ERKandBRAF-V600EproteininA375cells[1].CellViabilityAssay[1]CellLine:A375andHT-29Concentration:1nM-10μMIncubationTime:72hResult:InhibitedthecellviabilityofA375andHT-29withIC50sof46.5nMand51nM.WesternBlotAnalysis[1]CellLine:A3751/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEConcentration:1,4,12,37,111,333and1000nMIncubationTime:16hor0-24hResult:InducedthereductioninthephosphorylationofERK.Inhibitedp-ERKandBRAF-V600Einadose-andtime-dependentmanner.REFERENCES[1].HanXR,etal.DiscoveryofSelectiveSmallMoleculeDegradersofBRAF-V600E.JMedChem.2020Apr23;63(8):4069-4080.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792