产品说明书
MZP-55
 |
同义名 : | - |
| CAS号 : | 2010159-48-3 | |
| 货号 : | A176034 | |
| 分子式 : | C57H70ClN7O10S | |
| 纯度 : | 98% | |
| 分子量 : | 1080.725 | |
| MDL号 : | N/A | |
| 存储条件： |
粉末 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 50 mg/mL(46.27 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
|
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | MZP-55 is a VHL-based PROTAC targeting on BET with pDC50/Dmax (%) values of 8.1/95, 7.5/93, 7.7/92, −/26 for Brd4 short, Brd4 long, Brd3 and Brd2 in HeLa cells, consist of I-BET726 as a warhead ligand linked to VHL ligand VH032. MZP-55 at concentration ranging in 30-1000nM led a dose-dependent degradation of BRD3,4, as well as slight degradation of BRD2, in HeLa cells post 24-hour treatment. MZP-55 at concentration of 50nM achieved a depletion of BRD4 by 81% and downregulation of c-MYC, the target of BRD4, by 60% in MV4;11 cells treated for 4h. Also it exhibited anti-proliferation of MV4;11 and HL60 cells with pEC50/Emax (%) values of 7.08/96.4 and 6.37/98.3, respectively, post 48h[1]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
0.93mL 0.19mL 0.09mL |
4.63mL 0.93mL 0.46mL |
9.25mL 1.85mL 0.93mL |
| 参考文献 |
|---|