PROTAC-BRAF-V600E-degrader-1-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPROTACBRAF-V600Edegrader-1Cat.No.:HY-137487CASNo.:2417296-84-3分?式:C??H??F?N??O??S分?量:1001.07作?靶點(diǎn):PROTACs;Raf作?通路:PROTAC;MAPK/ERKPathway儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性PROTACBRAF-V600Edegrader-1?種有效的PROTACBRAF-V600E降解劑，對(duì)BRAF和BRAF-V600E的Kd分別為2.4nM和2nM。PROTACBRAF-V600Edegrader-1通過(guò)泛素-蛋?酶體系統(tǒng)(UPS)降解BRAF-V600E。PROTACBRAF-V600Edegrader-1可抑制??素瘤細(xì)胞的?長(zhǎng)。IC50&TargetBRAF-V600EBraf2nM(Kd)2.4nM(Kd)體外研究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?邊的抑制劑?師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