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CAS No.: 1699750-95-2

EOAI3402143 Catalog No. CSN25574

Synonyms: EOAI 402143;G9 free base

EOAI3402143 is a deubiquitinase (DUB) inhibitor, which dose-dependently inhibits Usp9x/Usp24 and Usp5.

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技术信息

生物活性

描述Ubiquitination plays an essential role in human cancers. EOAI3402143 is a deubiquitinase inhibitor that reduces the activity of deubiquitinase Usp5 and Usp9x in both vemurafenib sensitive and resistant A375 melanoma cells. Incubation of A375R cells with 2μM EOAI3402143 for 8 hours reduced the levels of pERK, pStat3, and increased the concentration of NOXA.^[1] Treatment of pancreatic cancer patient-derived cell lines (UM-2, UM-6, UM-16, and UM-76) with EOAI3402143 (1-5μM) suppressed cell survival in a dose-dependently manner. EOAI3402143 at a concentration of 600nM completely suppressed UM-2 3D colony growth compared with the vehicle-treated controls. Treatment with 600nM EOAI3402143 also promoted the 3D colony growth of 8041 cells by two folds. In both human MIAPACA2 xenografts and mouse 8041 xenografts, administration with EOAI3402143 at 15mg/kg for 12 days effectively inhibited the activity of Usp9x in tumors. However, tumor suppression was only observed in human MIAPACA2 xenografts. ^[2] In NSH mice inoculated with A375 cells, treatment with EOAI3402143 at both 7.5 and 15mg/kg completely suppressed tumor growth.^[1]
作用机制EOAI3402143 is a small molecule deubiquitinase inhibitor that retains potent inhibitory activity against Usp5 and Usp9x.^[1]
参考文献

[1] Potu H, Peterson LF, Pal A, Verhaegen M, Cao J, Talpaz M, Donato NJ. Usp5 links suppression of p53 and FAS levels in melanoma to the BRAF pathway. Oncotarget. 2014 Jul 30;5(14):5559-69. doi: 10.18632/oncotarget.2140
[2] Pal A, Dziubinski M, Di Magliano MP, Simeone DM, Owens S, Thomas D, Peterson L, Potu H, Talpaz M, Donato NJ. Usp9x Promotes Survival in Human Pancreatic Cancer and Its Inhibition Suppresses Pancreatic Ductal Adenocarcinoma In Vivo Tumor Growth. Neoplasia. 2018 Feb;20(2):152-164. doi: 10.1016/j.neo.2017.11.007

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
- 1.9864 mL
- 9.9320 mL
- 19.8641 mL
- 5 mM
- 0.3973 mL
- 1.9864 mL
- 3.9728 mL
- 10 mM
- 0.1986 mL
- 0.9932 mL
- 1.9864 mL

技术信息

CAS号

1699750-95-2

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H28Cl2N4O3

运输

蓝冰

分子量

503.42

别名

EOAI 402143;G9 free base

溶解度

DMSO	100.0 mg/mL (198.6 mM)
Water	Insoluble
Ethanol	Insoluble

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