|(2S,4R)-N-((S)-2-(叔丁基)-17-((S)-4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-f][1,2,4]三唑并[4,3-a][1,4]二氮杂卓-6-基)-4,16-二氧代-6,9,12-三氧杂-3,15-二氮杂庚-1-酰基)-4-羟基-1-(4-(4-甲基噻唑-5-基)苄基)吡咯烷-2-羧酰胺|CsnPharm

CAS No.: 1797406-69-9

MZ1 Catalog No. CSN22292

MZ1 is a PROTAC with VHL-ligand and targeting on BRD protein, with preferential selectivity to BRD4 (Kd=149nM) over BRD2 and BRD3.

规格	价格	促销价格	库存	数量

400-920-2911

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tech@csnpharm.cn

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述MZ1 is a PROTAC with VHL-ligand and targeting on BRD protein, with preferential selectivity to BRD4 (Kd=149nM) over BRD2 and BRD3. MZ1 at concentration of 1μM led to a significant degradation of BRD2,3 and almost complete degradation of BRD4 in HeLa cells post 24-hour treatment. MZ1 exhibited higher selectivity to BRD4 than BRD2,3, for MZ1 led an almost complete degradation of BRD4 (long) at concentration>0.1μM but the completed degradation of BRD2,3 could be observed at concentration at least higher than 2μM. Treatment with MZ1 resulted upregulation of P21 and AREG on RNA level and showed more subtle and less significant effects on genes relative to VHL-1, including FAS, TYRO3 and FGFR1 due to the preferential degradation of BRD4 over the other two BET proteins. The cis-MZ1 works as a negative control of MZ1^[1].
动物研究
剂量
Mice: 10 mg/kg^[2] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 10 mg/kg^[2] (i.p.)
给药途径	i.p.

[1] Zengerle M, Chan KH, et al. Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4. ACS Chem Biol. 2015 Aug 21;10(8):1770-7.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 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

技术信息

CAS号

1797406-69-9

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C49H60ClN9O8S2

运输

蓝冰

分子量

1002.64

别名

溶解度

DMSO	100.0 mg/mL (99.7 mM)
Water	Insoluble
Ethanol	100.0 mg/mL (99.7 mM)

动物实验配方

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