MZ1 |
カタログ番号GC18729 |
MZ1 は、von Hippel-Lindau および BRD4 のリガンドによって接続された PROTAC です。 MZ1 は、BRD2 および BRD3 よりも、BRD4 の可逆的かつ長期的な選択的除去を強力かつ迅速に誘導します。 BRD4 BD1/2、BRD3 BD1/2、BRD2 BD1/2 の Kds はそれぞれ 382/120、119/115、307/228 nM。
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Cas No.: 1797406-69-9
Sample solution is provided at 25 µL, 10mM.
MZ1 is a hybrid compound that drives the selective proteasomal degradation of bromodomain-containing protein 4 (BRD4). 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 uM. At concentrations of 2-10 uM, MZ1 causes the removal of BRD2, BRD3, and BRD4. BRD protein removal is evident within four hours of adding MZ1 and persists for at least 48 hours, unless MZ1 is removed.
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Average Rating: 5
(Based on Reviews and 40 reference(s) in Google Scholar.)Review for MZ1
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