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Merck
CN

662210

USP14 Inhibitor, IU1

The USP14 Inhibitor, IU1 controls the biological activity of USP14. This small molecule/inhibitor is primarily used for Cell Structure applications.

Synonym(s):

USP14 Inhibitor, IU1, 1-(1-(4-Fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl)-2-(pyrrolidin-1-yl)ethanone, 1-(1-(4-Fluorophenyl)-2,5-dimethylpyrrol-3-yl)-2-pyrrolidin-1-ylethanone, Ubiquitin Specific Protease 14 Inhibitor, DUB Inhibitor IX

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About This Item

Empirical Formula (Hill Notation):
C18H21FN2O
Molecular Weight:
300.37
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥90% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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Quality Segment

assay

≥90% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

beige

solubility

DMSO: 50 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

Fc1ccc(cc1)[n]2c(c(cc2C)C(=O)CN3CCCC3)C

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

General description

A cell-permeable pyrrolylpyrrolidinyl-ethanone that inhibits the proteasome association-dependent USP14 deubiquitinase (DUB) activity in a reversible manner (IC50 = 4.7 µM against Ub-AMC hydrolysis), exhibiting little or no activity toward 8 other DUBs. Shown to downregulate tau, TDP-43, ATXN3, GFAP, and free Ub levels in MEF cultures in a dose- (25 to 100 µM), time-, and USP14-dependent manner. USP14-catalyzed trimming of protein surface polyubiquitin chains rescues proteasome-bound proteins from proteolytic degradation and thereby prevents the depletion of free ubiquitin pool in cells. Comparing to b-AP15 (Cat. No. 662140), IU1 does not inhibit UCH37/UCH-L5 (IC50 = 700 µM).

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Lee, B.H., et al. 2010. Nature467, 179.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Regulatory Review (Z)


Storage Class

11 - Combustible Solids

wgk

WGK 3



Certificates of Analysis (COA)

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