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IU1, Proteasome USP14  Inhibitor

IU1, Proteasome USP14 Inhibitor

$49.00
A cell-permeable, reversible and selective inhibitor of human proteasome USP14.
Catalog No. Unit Price Qty
M60203-2s 2mg solid $49.00

Details

Product Information
Molecular Weight: 300.37
Formula: C18H21FN2O
Purity: ≥98%
CAS#: 314245-33-5
Solubility: DMSO up to 100 mM
Chemical Name: 1-(1-(4-fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl)-2-(pyrrolidin-1-yl)ethanone
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

IU1 is a cell-permeable, reversible and selective inhibitor of human USP14 with an IC50 of 4.7 μM. It selectively stimulates ubiquitin-dependent protein degradation in vitro at 34 μM and in MEF cells at 50 μM. At 75 μM, IU1 reduces accumulation of oxidized proteins in HEK293 cells, alleviating cytotoxicity induced by oxidative stress. Usp14 inhibition accelerated the degradation of oxidized proteins and enhanced resistance to oxidative stress. Enhancement of proteasome activity through inhibition of Usp14 may offer a strategy to reduce the levels of aberrant proteins in cells under proteotoxic stress.

 

How to Use:

  • In vitro:  IU1 was used at 10-75 µM final concentration in various in vitro assays.
  • In vivo:  n/a

 

Reference:

  • 1. Byung-Hoon L, et al. Enhancement of Proteasome Activity by a Small-Molecule Inhibitor of Usp14. (2010) Nature, 467(7312), 179-184.
  •  

 

Products are for research use only. Not for human use.

Description

Details

Product Information
Molecular Weight: 300.37
Formula: C18H21FN2O
Purity: ≥98%
CAS#: 314245-33-5
Solubility: DMSO up to 100 mM
Chemical Name: 1-(1-(4-fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl)-2-(pyrrolidin-1-yl)ethanone
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

IU1 is a cell-permeable, reversible and selective inhibitor of human USP14 with an IC50 of 4.7 μM. It selectively stimulates ubiquitin-dependent protein degradation in vitro at 34 μM and in MEF cells at 50 μM. At 75 μM, IU1 reduces accumulation of oxidized proteins in HEK293 cells, alleviating cytotoxicity induced by oxidative stress. Usp14 inhibition accelerated the degradation of oxidized proteins and enhanced resistance to oxidative stress. Enhancement of proteasome activity through inhibition of Usp14 may offer a strategy to reduce the levels of aberrant proteins in cells under proteotoxic stress.

 

How to Use:

  • In vitro:  IU1 was used at 10-75 µM final concentration in various in vitro assays.
  • In vivo:  n/a

 

Reference:

  • 1. Byung-Hoon L, et al. Enhancement of Proteasome Activity by a Small-Molecule Inhibitor of Usp14. (2010) Nature, 467(7312), 179-184.
  •  

 

Products are for research use only. Not for human use.

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