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I1911

Sigma-Aldrich

IU1

≥98% (HPLC)

Sinonimo/i:

1-[1-(4-Fluoro-phenyl)-2,5-dimethyl-1H-pyrrol-3-yl]-2-pyrrolidin-1-yl-ethanone

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5 MG
131,00 €
25 MG
254,00 €

131,00 €

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5 MG
131,00 €
25 MG
254,00 €

About This Item

Formula empirica (notazione di Hill):
C18H21FN2O
Numero CAS:
314245-33-5
Peso molecolare:
300.37
Numero MDL:
MFCD01917473
Codice UNSPSC:
12352200
ID PubChem:
329815361
NACRES:
NA.77

131,00 €

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Livello qualitativo

100

Saggio

≥98% (HPLC)

Stato

powder

Colore

off-white to light brown

Solubilità

DMSO: >10 mg/mL

Temperatura di conservazione

2-8°C

Stringa SMILE

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
JUWDSDKJBMFLHE-UHFFFAOYSA-N

Applicazioni

IU1 has been used for the inhibition of Ubiquitin Specific Peptidase 14 (USP14) in human neuroblastoma cells (SH-SY5Y)[1] and in ubiquitin-rhodamine hydrolysis plate assay.[2]

Azioni biochim/fisiol

IU1 is an inhibitor of USP14, a deubiquitinating enzyme associated with the proteasome.
IU1 is an inhibitor of USP14, a deubiquitinating enzyme associated with the proteasome. The proteasome mediates the cellular degradation of oxidized, damaged and misfolded proteins which, if not removed, accumulate and become toxic to cells. Proteins targeted for proteasomal degradation are first ubiquitinated, with longer length ubiquitin chains interacting more strongly with the proteasome. Deubiquitinating enzymes (DUBs) such as USP14 interfere with the degradation process. IU1 inhibits USP14-mediated ubiquitin "chain-trimming" thereby enhancing substrate degradation by the proteasome. The compound may help to eliminate toxic proteins more effectively by enhancing their degradation.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

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Certificati d'analisi (COA)

Lot/Batch Number
0000289208
0000230419
0000230419
0000289208
0000103525

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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)
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
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
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