P 22077
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.
描述:IC 50:8.6 nM(singleplexed),7.8 nM(multiplexed)
USP7,也被称为HAUSP,因其对肿瘤抑制基因p53稳定性的影响而在癌症发展过程中发挥着至关重要的作用。P 022077抑制泛素特异性蛋白酶(USP)7及紧密相关的去泛素化酶(DUB)USP4。
体外实验:P 022077在所测试的浓度范围内,对DEN1和SENP2core显现出极低的活性,但抑制USP7,IC50值为8 μM[1]。在另一项研究中,以小分子抑制剂P 22077抑制USP7可使Tip60不稳定,从而减弱p53依赖性的细胞凋亡通路。然而,P 22077具有细胞毒性,部分原因是Tip60的不稳定[2]。
体内实验:P 022077目前处于体外研究阶段,没有进行动物体内研究。
临床试验:P 022077目前处于临床前开发阶段,没有进行中的临床试验。
参考文献:
[1] Tian X, Isamiddinova NS, Peroutka RJ, Goldenberg SJ, Mattern MR, Nicholson B, Leach C. Characterization of selective ubiquitin and ubiquitin-like protease inhibitors using a fluorescence-based multiplex assay format. Assay Drug Dev Technol. 2011;9(2):165-73.
[2] Dar A, Shibata E, Dutta A. Deubiquitination of Tip60 by USP7 determines the activity of the p53-dependent apoptotic pathway. Mol Cell Biol. 2013; 33(16):3309-20.
Physical Appearance | A solid |
Storage | Store at 4°C |
M.Wt | 315.32 |
Cas No. | 1247819-59-5 |
Formula | C12H7F2NO3S2 |
Solubility | insoluble in H2O; insoluble in EtOH; ≥14.6 mg/mL in DMSO |
Chemical Name | 1-[5-(2,4-difluorophenyl)sulfanyl-4-nitrothiophen-2-yl]ethanone |
SDF | Download SDF |
Canonical SMILES | CC(=O)C1=CC(=C(S1)SC2=C(C=C(C=C2)F)F)[N+](=O)[O-] |
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。 |
描述 | P 22077是泛素特异性蛋白酶(USP)7的强效抑制剂,其EC50值为8.6 ?M。 | |||||
靶点 | USP 7 | |||||
IC50 | 8.6 ?M (EC50) |