|(2S,4R)-1-((S)-1-(4-((2S,4R)-1-乙酰基-4-((4-氯苯基)氨基)-2-甲基-1,2,3, 4-四氢喹啉-6-基)苯基)-15-(叔丁基)-1,13-二氧代-5,8,11-三氧杂-2,14-二氮杂十六烷-16-酰基)-4-羟基-N-(4-(4-甲基噻唑-5-基)苄基)吡咯烷-2-甲酰胺|CsnPharm

CAS No.: 2010159-47-2

Synonyms: MZP-54

MZP-54 is a PROTAC targeting on BET, consist of a warhead I-BET726 (BET bromodomain inhibitor) linked to a VHL ligand VH032.

规格	价格	促销价格	库存	数量

400-920-2911

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400-920-2911

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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 Brd4^BD2 and VHL-EloC-EloB protein with K_d 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/ E_max(%) values of 7.31/94.2 and 6.57 and 98.3, respectively, post 48h^[1].
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CAS号	2010159-47-2	储存条件	粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C55H66ClN7O9S	运输	蓝冰
分子量	1036.67	别名	MZP-54

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