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质量水平
检测方案
≥98% (HPLC)
形式
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。 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。
WGK
WGK 3
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
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
Inactive USP14 and inactive UCHL5 cause accumulation of distinct ubiquitinated proteins in mammalian cells.
Chadchankar J, et al.
bioRxiv, 10(11), 479758-479758 (2018)
Kapil Sareen-Khanna et al.
American journal of physiology. Renal physiology, 311(5), F1035-F1046 (2016-09-16)
Kidney cell injury may be associated with protein misfolding and induction of endoplasmic reticulum (ER) stress. Examples include complement-induced glomerular epithelial cell (GEC)/podocyte injury in membranous nephropathy and ischemia-reperfusion injury. Renal cell injury can also result from mutations in integral
Yuning Liao et al.
Cell death & disease, 8(2), e2585-e2585 (2017-02-06)
Androgen receptor (AR) is frequently over-expressed and plays a critical role in the growth and progression of human prostate cancer. The therapy attempting to target AR signalling was established in decades ago but the treatment of prostate cancer is far
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