DUBs-IN-2
(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。
Cas No.:924296-19-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
| 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。 |
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| 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。 | ||
| 制备储备液 | |||
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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 |
| 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 | 只 |
| 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 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。