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1-[1-(4-Fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl]-2-(1-pyrrolidinyl)ethanone

1-[1-(4-Fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl]-2-(1-pyrrolidinyl)ethanone ??? ???
?? ??:
314245-33-5
???:
1-[1-(4-Fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl]-2-(1-pyrrolidinyl)ethanone
???(??):
IU1;CS-1901;IU1; IU-1; IU 1;IU-1 (USP14 inhibitor IU1);1-[1-(4-Fluorophenyl)-2,5-dimethyl-3-pyrrolyl]-2-(1-pyrrolidinyl)ethanone;1-[1-(4-Fluorophenyl)-2,5-dimethylpyrrol-3-yl]-2-(pyrrolidin-1-yl)ethanone;1-[1-(4-Fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl]-2-(1-pyrrolidinyl)ethanone;1-(1-(4-fluorophenyl)-2,5-diMethyl-1H-pyrrol-3-yl)-2-(pyrrolidin-1-yl)ethanone;Ethanone, 1-[1-(4-fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl]-2-(1-pyrrolidinyl)-;1-[1-(4-FLUOROPHENYL)-2,5-DIMETHYL-1H-PYRROL-3-YL]-2-(1-PYRROLIDINYL)ETHANONE;IU1
CBNumber:
CB42518875
???:
C18H21FN2O
??? ??:
300.37
MOL ??:
314245-33-5.mol
MSDS ??:
SDS

1-[1-(4-Fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl]-2-(1-pyrrolidinyl)ethanone ??

?? ?
437.0±45.0 °C(Predicted)
??
1.16±0.1 g/cm3(Predicted)
?? ??
2-8°C
???
DMSO: >10mg/mL
?? ?? (pKa)
8.20±0.20(Predicted)
??? ??
??
??
????? ?? ????
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??? ?? ?????? 2? ?? ??????. DMSO ?? ??? ??? -20°C?? ?? 1?? ?? ??? ? ????.
??
  • ?? ? ?? ??
  • ?? ? ???? ?? (GHS)
??? ?? Xi
?? ???? ?? 41
????? 61
WGK ?? 3
????(GHS): GHS hazard pictograms
?? ?: Danger
??·?? ??:
?? ??·?? ?? ?? ?? ?? ?? ? ?? ?? P- ??
H318 ?? ?? ??? ??? ?? ? ?? ?? ??? ?? ?? 1 ?? GHS hazard pictograms P280, P305+P351+P338, P310
??????:
P280 ????/???/???/?????? ?????.
P305+P351+P338 ?? ??? ? ?? ?? ???? ????. ???? ?????? ?????. ?? ????.
NFPA 704
0
3 0

1-[1-(4-Fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl]-2-(1-pyrrolidinyl)ethanone C??? ??, ??, ??

??

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

Biochem/physiol Actions

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.

1-[1-(4-Fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl]-2-(1-pyrrolidinyl)ethanone ?? ?? ? ???

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1-[1-(4-Fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl]-2-(1-pyrrolidinyl)ethanone ?? ??

???( 88)?? ??
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1-[1-(4-Fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl]-2-(1-pyrrolidinyl)ethanone ?? ??:

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