DUBs-IN-2
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50值:对USP7/USP8分别为7.2 M/0.93 M.
DUBs-IN-2是一种有效的去泛素化酶抑制剂.
USP7(或HAUSP)与蛋白Mdm2(一种E3泛素连接酶)共同识别p53肿瘤抑制子的N端转录激活结构域,通过泛素化引起其降解.USP7也可与直接必不可少的病毒蛋白(p53\FOXO4\PTEN)和致癌通路相互作用.另外,与USP7沉默相关的表型强烈表明,靶向USP7的小分子抑制剂可能是抗病毒和抗癌疗法的潜在方向.USP8(或UBPY)可与多种底物相互作用,如表皮生长因子受体(EGPR),其是调控细胞存活\增殖和分化途径所必需的.USP8也是受体内吞和转运的关键调节子[1].
体外:在杆状病毒感染的昆虫细胞中过表达人类USP7和USP8酶的全长形式,然后用His标记亲和层析手段纯化.用泛素C端7-氨基-4-甲基香豆素(Ub–AMC)评估对USP7和USP8去泛素化活性的抑制能力.Ub–AMC被去泛素化酶水解,而后释放AMC.以该物质稀释为100 mM到10 nM不等的八个终浓度后,基于剂量反应曲线计算IC50值[1].
DUBs-IN-2是USP7和USP8去泛素化酶的有效抑制剂,是在基于荧光的生化实验中,对65902种化学结构不同的物质针对全长USP7半胱氨酸蛋白酶活性的高通量筛选中鉴定得到的功能化氰基吡啶[1]..
体内:迄今为止,无体内实验进行.
临床试验:迄今为止,无临床试验进行.
参考文献：
[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.
| Storage | Store at -20°C |
| M.Wt | 275.26 |
| Cas No. | 924296-19-5 |
| Formula | C15H9N5O |
| Solubility | ≥17.03 mg/mL in DMSO with ultrasonic; ≥2.27 mg/mL in EtOH with gentle warming and ultrasonic; insoluble in H2O |
| Chemical Name | (E)-9-(ethoxyimino)-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile |
| SDF | Download SDF |
| Canonical SMILES | CCO/N=C1C2=CC=CC=C2C3=C\1N=C(C(C#N)=N3)C#N |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
质量控制和MSDS
- 批次:
化学结构
