产品说明书
MZP-54
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同义名 : | - |
| CAS号 : | 2010159-47-2 | |
| 货号 : | A376159 | |
| 分子式 : | C55H66ClN7O9S | |
| 纯度 : | 98% | |
| 分子量 : | 1036.672 | |
| MDL号 : | MFCD31807304 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
无水乙醇: 50 mg/mL(48.23 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | MZP-54 is a PROTAC targeting on BET, consist of a warhead I-BET726 (BET bromodomain inhibitor) linked to a VHL ligand VH032. It exhibited affinity to the Brd4BD2 and VHL-EloC-EloB protein with Kd values of 4nM and 105nM, respectively. Treatment with 50nM MZP-54 for 4h led to degradation of Brd4 by 87%, accompanied with the downregulation of c-MYC by 73% in MV4;11 cells. A dose-dependent antiproliferative effect on MV4;11 treated with MZP-54 at various concentration could be observed post 48h. A further assay showed that MZP-54 exhibited potency to depletion of Brd4 short, Brd4 long, Brd3 and Brd2 with pDC50/Dmax (%) values of 8.1/98, 7.6/95, 7.3/91 and −/43, respectively, in HeLa cells post 24-hour treatment. It exhibited anti-proliferative potency against MV4;11 cells and HL60 cells with pEC50/ Emax(%) values of 7.31/94.2 and 6.57 and 98.3, respectively, post 48h[1]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
0.96mL 0.19mL 0.10mL |
4.82mL 0.96mL 0.48mL |
9.65mL 1.93mL 0.96mL |
| 参考文献 |
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