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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-MS417
MS417

Chemical Structure : MS417

CAS No.: 916489-36-6

MS417 (GTPL-7512, MS-417)

货号: PC-62474Not For Human Use, Lab Use Only.

MS417 (GTPL-7512) is a highly specific BET bromodomain inhibitor that binds to BRD4-BD1 and BRD4 BD2 with Kd of 36.1 uM and 25.4 uM respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MS417 (GTPL-7512) is a highly specific BET bromodomain inhibitor that binds to BRD4-BD1 and BRD4 BD2 with Kd of 36.1 uM and 25.4 uM respectively.
MS417 shows 100-200-fold weaker affinity for CBP, BRD7, or BPTF, and no binding affinity for many other bromodomains.
MS417 blocks BRD4 binding to the acetylated NF-κB, effectively attenuates NF-κB transcriptional activation of proinflammatory genes in kidney cells treated with TNFα or infected by HIV.
MS417 ameliorates inflammation and kidney injury in HIV-1 transgenic mice.

物理化学性质&存储条件

分子量 414.908
分子式 C20H19ClN4O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Methyl 2-[(6S,Z)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]acetate

参考文献

1. Zhang G, et al. J Biol Chem. 2012 Aug 17;287(34):28840-51.

2. Boehm D, et al. Cell Cycle. 2013 Feb 1;12(3):452-62.

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