IU1, Proteasome USP14 Inhibitor


Catalog No. size PriceQuantity
M60203-2S 2 mg solid $79
M60203-10S 10mg solid $320

Description

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.

Product information

CAS Number: 314245-33-5

Molecular Weight: 300.37

Formula: C18H21FN2O

Chemical Name: 1-(1-(4-fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl)-2-(pyrrolidin-1-yl)ethanone

Smiles: CC1=CC(C(=O)CN2CCCC2)=C(C)N1C1C=CC(F)=CC=1

InChiKey: JUWDSDKJBMFLHE-UHFFFAOYSA-N

InChi: 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

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

IU1 was used at 10-75 µM final concentration in various in vitro assays.

References:

  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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