DU-14-PTP1B-TC-PTP-PROTAC-生命科学试剂-MCE.pdf

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Inhibitors•ScreeningLibraries•Proteins

www.MedChemE

DU-14(PTP1B/TC-PTPPROTAC)

Cat.No.:HY-164864

CASNo.:3053413-58-1

分⼦式:C₇₄H₈₅BrF₂N₉O₁₄PS

分⼦量:1505.46

作⽤靶点:PROTACs;STAT

作⽤通路:PROTAC;JAK/STATSignaling;StemCell/Wnt

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性DU-14(PTP1B/TC-PTPPROTAC)是⼀种有效的和选择性的PTP1B和TC-PTP双重PROTAC降解剂，对PTP1B

和TC-PTP磷酸酶活性的IC50分别为24.2nM和30.1nM。DU-14(PTP1B/TC-PTPPROTAC)可以增强IFN-γ

信号传导、促进T细胞活化，具有抗肿瘤的活性。(粉⾊:PTP1B/TC-PTP抑制剂(HY-171027);⿊⾊:连接⼦(

HY-W340290);蓝⾊:E3连接酶配体(HY-112078))

IC50TargetIC50:24.2nM(PTP1B);30.1nM(TC-PTP)[1]

体外研究DU-14(PTP1B/TC-PTPPROTAC)(0-1000nM;16h)causesPTP1B/TC-PTPdegradationandpromotes

STAT1phosphorylationinIFN-γ-treatedMC38cells[1].

DU-14(PTP1B/TC-PTPPROTAC)(48h)effectivelydegradesTC-PTPandPTP1BinTcellsandpromotes

theactivationofTcells[1].

WesternBlotAnalysis[1]

CellLine:IFN-γtreatedMC38cells

Concentration:0,5,25,125,250,500and1000nM

IncubationTime:16h

Result:InhibitedthelevelsofPTP1BandTC-PTPinadose-