PROTAC-PARP1-degrader-4-生命科学试剂-MCE.pdf

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Inhibitors•ScreeningLibraries•Proteins

www.MedChemE

PROTACPARP1degrader-4

Cat.No.:HY-170620

分⼦式:C₅₁H₆₂FN₇O₆S

分⼦量:920.14

作⽤靶点:PROTACs;PARP

作⽤通路:PROTAC;CellCycle/DNADamage;Epigenetics

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性PROTACPARP1degrader-4(Compound180055)是⼀种选择性的PARP1PROTAC降解剂(在T47D和MDA-

MB-231细胞系中的DC50分别为180nM和240nM)。PROTACPARP1degrader-4可促进PARP1的泛素化和

降解，并抑制PARP1酶的活性，但不会产⽣明显的DNA诱捕效应。PROTACPARP1degrader-4能抑制携带

BRCA基因突变肿瘤，同时对正常细胞的⽣长影响较⼩(粉红⾊：PARP1ligand(HY-10617A);蓝⾊：E3ligase

VHLligand(HY-125845);⿊⾊：linker(HY-W014787))[1]。

IC50TargetPARP1

体外研究PROTACPARP1degrader-4(1-10μM,24-48h)protectsT47DandMOLT4cellsfromgenetoxicity-induced

celldeath[1].

PROTACPARP1degrader-4(10μM,3-6days)inducessubstantialcytotoxiceffectsinMOLT4cellswith

BRCA1mutation[1].

CellViabilityAssay[1]

CellLine:CardiomyocytecelllineslackingBRCA1mutationsandMOLT4cells

Concentration:1,5,10μM

IncubationTime:144h

Result:Showedminimalcytotoxicityincardiomyocytecell