MZ 1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. MZ 1 potently and rapidly induces reversible, long-lasting, and selective removal of BRD4 over BRD2 and BRD3. K d s of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively.
MZ 1 conjugates the pan-BET inhibitor JQ1 to VH032, a potent and specific VHL ligand, via a 3-unit PEG linker.MZ 1 (100 and 250 nM; 24 hours) induces BRD4 degradation in LS174t cells 24?h. MZ 1 leads to complete degradation of BRD4 protein, whereas the expression of BRD4 mRNA is not reduced. has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献
[1]. Zengerle M, et al. Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4. ACS Chem Biol. 2015 Aug 21;10(8):1770-7.[2]. Gadd MS, et al. Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017 May;13(5):514-521.[3]. Otto C, et al. Tar
溶解度数据
In Vitro: DMSO : 100 mg/mL (99.74 mM; Need ultrasonic)配制储备液