• 生物活性

靶点及简介 ：MZ1 is a hybrid compound that drives the selective proteasomal degradation of bromodomain-containing protein 4 (BRD4).

MZ-1 是一种 bromodomain-containing protein 4 (BRD4) 的PROTAC降解剂。MZ-1 可结合到Brd结构域Brd2^BD1、Brd2^BD2、Brd3^BD1、Brd3^BD2、Brd4^BD1和Brd4^BD2，对应的Kd值分别为62 nM、60 nM、21 nM、13 nM、39 nM和15 nM。

MZ 1是一种PROTAC BRD4降解剂，对BRD4 BD1/2，BRD3 BD1/2和BRD2 BD1/2的Kd值分别为382/120，119/115和307/228 nM。MZ 1迅速地诱导BRD4降解，选择性高于BRD2和BRD3。MZ 1通过一个3-unit PEG连接子将pan-BET抑制剂JQ1与VH032结合，VH032是一种有效且特异性的VHL配体。

• 验证及参考文献

验证：

参考文献：

[1] C Otto, et al. Neoplasia. Targeting bromodomain-containing protein 4 (BRD4) inhibits MYC expression in colorectal cancer cells

[2] Morgan S Gadd, et al. Nat Chem Biol. Structural basis of PROTAC cooperative recognition for selective protein degradation

[3] Michael Zengerle, et al. ACS Chem Biol. Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

• 溶解度及制备方案
  

  DMSO	100 mg/mL  (99.74 mM)
  Ethanol	100 mg/mL  (99.74 mM)
  Water	Insoluble

制备储备液

浓度   溶剂体积   质量	1 mg	5 mg	10 mg
1 mM	0.9974 mL	4.9868 mL	9.9737 mL
5 mM	0.1995 mL	0.9974 mL	1.9947 mL
10 mM	0.0997 mL	0.4987 mL	0.9974 mL
50 mM	0.0199 mL	0.0997 mL	0.1995 mL

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  关键词：MZ 1, MZ1, MZ 1供应商, PROTAC抑制剂, 购买MZ 1, MZ 1溶解度, MZ 1结构式