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Merck
CN

I1911

Sigma-Aldrich

IU1

≥98% (HPLC)

别名:

1-[1-(4-氟-苯基)-2,5-二甲基-1H-吡咯-3-基]-2-吡咯烷-1-基-乙酮

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About This Item

经验公式(希尔记法):
C18H21FN2O
分子量:
300.37
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

质量水平

方案

≥98% (HPLC)

表单

powder

颜色

off-white to light brown

溶解性

DMSO: >10 mg/mL

储存温度

2-8°C

SMILES字符串

FC1=CC=C(N2C(C)=CC(C(CN3CCCC3)=O)=C2C)C=C1

InChI

1S/C18H21FN2O/c1-13-11-17(18(22)12-20-9-3-4-10-20)14(2)21(13)16-7-5-15(19)6-8-16/h5-8,11H,3-4,9-10,12H2,1-2H3

InChI key

JUWDSDKJBMFLHE-UHFFFAOYSA-N

应用

IU1已用于抑制人神经母细胞瘤细胞(SH-SY5Y)中的泛素特异性肽酶14(USP14)并用于泛素-若丹明水解板测定。

生化/生理作用

IU1是USP14的抑制剂,USP14是与蛋白酶体相关的去泛素化酶。
IU1是USP14的抑制剂,USP14是与蛋白酶体相关的去泛素化酶。 蛋白酶体介导氧化、损伤和错误折叠的蛋白质的细胞降解,如果不去除,这些蛋白质会积聚并对细胞产生毒性。 首先将靶向蛋白酶体降解的蛋白质泛素化,较长长度的泛素链与蛋白酶体的相互作用更强。 去泛素化酶(DUB)(例如USP14)会干扰降解过程。 IU1抑制USP14介导的泛素“链修剪”,从而增强蛋白酶体对底物的降解。 该化合物可以通过增强其降解来帮助更有效地消除有毒蛋白质。

储存分类代码

11 - Combustible Solids

WGK

WGK 3


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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Inactive USP14 and inactive UCHL5 cause accumulation of distinct ubiquitinated proteins in mammalian cells.
Chadchankar J, et al.
bioRxiv, 10(11), 479758-479758 (2018)
Liu Xu et al.
International journal of biological sciences, 16(15), 2951-2963 (2020-10-17)
Previous studies have demonstrated that the antitumor potential of IU1 (a pharmacological compound), which was mediated by selective inhibition of proteasome-associated deubiquitinase ubiquitin-specific protease 14 (USP14). However, the underlying molecular mechanisms remain elusive. It has been well established that mdm2
Di Yun et al.
Neuropharmacology, 133, 354-365 (2018-02-07)
Posttranslational modification and degradation of proteins by the ubiquitin-proteasome system (UPS) is crucial to synaptic transmission. It is well established that 19S proteasome associated deubiquitinases (DUBs) reverse the process of ubiquitination by removing ubiquitin from their substrates. However, their potential
USP14 inhibition corrects an in vivo model of impaired mitophagy.
Chakraborty J, et al.
EMBO Molecular Medicine, 10(11), e9014-e9014 (2018)
Ningning Liu et al.
Molecular and cellular biochemistry, 431(1-2), 87-96 (2017-04-02)
Persistent activation of nuclear factor B (NF-κB) is very important in the modulation of macrophages cellular response to microbial infections. The deubiquitinase USP14, which is critical for ubiquitin-mediated proteasomal degradation of proteins, is known to be involved in cancer, neurological

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