
- PR-619
- Vialinin A
- P005091
- WP1130
- NSC 687852 (b-AP15)
- NSC 632839 hydrochloride
P 22077USP7/(DUB)USP47 inhibitor |
Sample solution is provided at 25 µL, 10mM.
































Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure

Description | P 22077 is a potent inhibitor of ubiquitin-specific protease (USP) 7 with EC50 value of 8.6 µM. | |||||
Targets | USP 7 | |||||
IC50 | 8.6 µM (EC50) |

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Cas No. | 1247819-59-5 | SDF | Download SDF |
Chemical Name | 1-[5-(2,4-difluorophenyl)sulfanyl-4-nitrothiophen-2-yl]ethanone | ||
Canonical SMILES | CC(=O)C1=CC(=C(S1)SC2=C(C=C(C=C2)F)F)[N+](=O)[O-] | ||
Formula | C12H7F2NO3S2 | M.Wt | 315.32 |
Solubility | ≥14.6mg/mL in DMSO | Storage | Store at 4°C |
Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
Description:IC50: 8.6 nM (singleplexed); 7.8 nM (multiplexed)USP7, also known as HAUSP, has been found to be critical in cancer progression due to its influence on the stability of the tumor suppressor p53. P022077 Inhibits ubiquitin-specific protease (USP) 7 and also inhibits the closely related deubiquitinase (DUB) USP4. In vitro: P022077 had negligible activity versus DEN1 and SENP2core over the concentration range tested, but inhibited USP7 with an IC50 of 8 μM [1]. In another study Inhibiting, USP7 with the small-molecule inhibitor P22077 attenuates the p53-dependent apoptotic pathway by destabilizing Tip60. P22077, however, is still cytotoxic, and this is partly due to destabilization of Tip60 [2]. In vivo: P022077 is currently in in-vitro investigation and no animal in vivo study is ongoing. Clinical trial: P022077 is currently in the preclinical development and no clinical trial is ongoing.References:[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.
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1、直接竞争,标记抗原,与检测样品中的抗原竞争抗体。
2、间接竞争,标记抗体,固相抗原与液相抗原(样品)竞争标记抗体。
3、定义
间接竞争法的模型:包被抗原,用HRP-抗体与样本一起加入。样本中的Ag与Solid-Ag竞争HRP-Ab,固相吸附的HRP-Ab与样本中的Ag浓度成反比。
直接竞争法的模型:包被抗体,用HRP-抗原与样本一起加入。样本中的Ag与HRP-Ag竞争Solid-Ab,固相吸附的HRP-Ag与样本中的Ag浓度成反比。
4、竞争法的理论基础:是限量抗体。只有在限量抗体基础上,两种抗原才会形成竞争关系。
5、、间接竞争法具备较高灵敏度原因。
直接竞争法里,标记抗原与待测抗原均是液相,与抗体的结合机会是一样的,例如有1份标记抗原与1份待测抗原竞争1份抗体,那么有50%的标记抗原能与抗体结合,所以标记抗原的相对结合率为50%。间接法里,固相抗原与抗体的接触面积较小,固相抗原与待测抗原的结合抗体机会是不平等的,接近顺序饱和法,即只有与待测抗原结合剩余的抗体才会与固相抗原结合,同样有1份固相抗原与1份待测抗原竞争1份抗体时,基本上抗体会被待测抗原中和掉,与固相抗原结合的抗体非常少。固相抗原的相对结合率为0%。因此,间接法的抑制曲线斜率会大于竞争法。
因为抑制率越大则斜率越大,从而灵敏度越大。(假设零管变异5%,以两倍SD为灵敏度限,则为90%相对结合率,则间接法可以在较低的待测抗原浓度达到这一相对结合率,因此灵敏度要高。)
在进行系统放大时,间接法一般可以使用酶标二抗。因为二抗可以针对抗体的多个部位,所以存在放大效应,从而能提高间接法的灵敏度。直接法一般难以进行放大,常用的有生物 素化抗原与酶标亲和素,但模式上似乎不存在放大效应。
6、间接法的高灵敏度难以实现的原因:
双抗体 夹心的免放(IRMA)模式刚出现时,也被模型证明灵敏度优于竞争法的放免(RIA),原因也是较大的斜率,但是IRMA的高灵敏度一直到单抗发展后才得以实现。
采用抗-HBe抗体包被反应板,加入校准品及被测样本,同时加入定量HBeAg中和抗原,经过振荡孵育,洗板后再加入铕标记的抗-HBe,若标本中抗-HBe浓度高,HBeAg将被大量中和,使最后形成的抗-HBe-HBeAg-铕标记抗-HBe复合物减少。增强液(β-NTA)将标记在抗体上的Eu3+解离到溶液中,Eu3+和增强液中的有效成分形成高荧光强度的螯合物,荧光强度和样本中的抗-HBe浓度成反比。

