Home>>Signaling Pathways>> DNA Damage/DNA Repair>> Deubiquitinase>>DUBs-IN-2

DUBs-IN-2 Sale

(Synonyms: 9-乙氧基亚氨基-9H-茚并[1,2-B]吡嗪-2,3-二甲腈) 目录号 : GC17125

DUBs-IN-2 是一种有效的去泛素酶抑制剂,IC50 为 0.28 μM for USP8。

DUBs-IN-2 Chemical Structure

Cas No.:924296-19-5

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥2,957.00
现货
2mg
¥1,953.00
现货
5mg
¥2,930.00
现货
10mg
¥4,185.00
现货
50mg
¥12,555.00
现货
100mg
¥17,577.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

产品描述

IC50s: 7.2 M/0.93 M for USP7/USP8, respectively.

DUBs-IN-2 is a potent deubiquitinase enzyme inhibitor.

USP7 (or HAUSP) associated with the protein Mdm2 (an E3 ubiquitin ligase) recognizes the N-terminal transactivation domain of the p53 tumor suppressor and elicites its degradation by ubiquitination. USP7 also interacts with directly essential viral proteins (p53, FOXO4, PTEN) and oncogenic pathways. In addition, phenotypes connected with USP7 silencing strongly reveal that targeting USP7 by small-molecule inhibitors may be an potential direction for antiviral and anticancer therapies. USP8 (or UBPY) interacts with many substrates, such as the epidermal growth factor receptor (EGFR), an essential for the regulating cell survival, proliferation, and differentiation pathways), and is a critical regulator of receptor endocytosis and trafficking [1].

In vitro: Human USP7 and USP8 enzymes in baculovirus-infected insect cells were overexpressed in their full-length forms, then purified by the His-tag affinity chromatography procedure. using ubiquitin C-terminal 7-amido-4-methylcoumarin (Ub–AMC) evaluates inhibition of USP7 and USP8 deubiquitinating activity. Ub–AMC is hydrolyzed by deubiquitinating enzymes, thus releasing AMC. IC50 values were calculated based on dose–response curve after dilution of this compound in eight final concentrations, ranging from 100 mm to 10 nm [1].

DUBs-IN-2 as potent inhibitors of USP7 and USP8 deubiquitinating enzymes was identified functionalized cyanopyrazines by high-throughput screening of 65092 chemically diverse compounds for activity toward full-length USP7 cysteine protease in a fluorescence-based biochemical assay [1].

In vivo: So far, no study in vivo has been conducted.

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Colombo M, Vallese S, Peretto I, Jacq X, Rain JC, Colland F, Guedat P.  Synthesis and biological evaluation of 9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile analogues as potential inhibitors of deubiquitinating enzymes. ChemMedChem. 2010 Apr 6;5(4):552-8.

Chemical Properties

Cas No. 924296-19-5 SDF
别名 9-乙氧基亚氨基-9H-茚并[1,2-B]吡嗪-2,3-二甲腈
化学名 (E)-9-(ethoxyimino)-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile
Canonical SMILES CCO/N=C1C2=CC=CC=C2C3=C\1N=C(C(C#N)=N3)C#N
分子式 C15H9N5O 分子量 275.26
溶解度 Soluble in DMSO 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 3.6329 mL 18.1646 mL 36.3293 mL
5 mM 0.7266 mL 3.6329 mL 7.2659 mL
10 mM 0.3633 mL 1.8165 mL 3.6329 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置