A PROTAC that drives the selective proteasomal degradation of BRD4; also causes the removal of BRD2 and BRD3 when used at higher concentrations

MZ1 – 500 µg

Brand:
Cayman
CAS:
1797406-69-9
Storage:
-20
UN-No:
Non-Hazardous - /

MZ1 is a hybrid compound that drives the selective proteasomal degradation of bromodomain-containing protein 4 (BRD4).{33482} It is characterized as a proteolysis-targeting chimera (PROTAC) and contains JQ-1, which binds bromo- and extra-terminal (BET) proteins, linked to a ligand for the E3 ubiquitin ligase VHL. MZ1 induces the selective degradation of BRD4 in HeLa cells when used at 0.1-0.5 µM.{33482} At concentrations of 2-10 µM, MZ1 causes the removal of BRD2, BRD3, and BRD4.{33482} BRD protein removal is evident within four hours of adding MZ1 and persists for at least 48 hours, unless MZ1 is removed.{33482}  

 

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Description

A PROTAC that drives the selective proteasomal degradation of BRD4; also causes the removal of BRD2 and BRD3 when used at higher concentrations

Formal name: (4R)-N-[14-[(6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]-1,13-dioxo-3,6,9-trioxa-12-azatetradec-1-yl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-L-prolinamide

Synonyms: 

Molecular weight: 1,002.60

CAS: 1797406-69-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|PROTACs||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System||Research Area|Epigenetics, Transcription, & Translation|Readers|Bromodomains

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