MZ 1
目录号: PL10630 纯度: ≥99%
CAS No. :1797406-69-9
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中文名称
MZ 1
英文名称
MZ 1
英文别名
MZ 1;GTPL10728;MZ1; MZ-1;BCP31482;MZ 1( MZ-1);BDBM50459880;s8889;(2S,4R)-1-((S)-2-(Tert-butyl)-17-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]tria
Cas No.
1797406-69-9
分子式
C49H60ClN9O8S2
分子量
1002.64
包装储存
-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
产品详情
MZ 1 是由 von Hippel-Lindau 配体和 BRD4 配体相连的 PROTAC。MZ 1 强效迅速地诱导 BRD4 降解,选择性高于 BRD2 和 BRD3。对 BRD4 BD1/2,
生物活性
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.
性状
Solid
IC50 & Target[1][2]
Kd: 382/120 nM (BRD4 BD1/2), 119/115 nM (BRD3 BD1/2), 307/228 nM (BRD2 BD1/2).
体外研究(In Vitro)
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
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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