For research use only.

Catalog No.S7134

18 publications

IU1 Chemical Structure

CAS No. 314245-33-5

IU1 is a cell-permeable, reversible and selective proteasome inhibitor of human USP14 with IC50 of 4.7 μ M, 25-fold selective to IsoT. IU1 induces autophagy.

Selleck's IU1 has been cited by 18 publications

2 Customer Reviews

  • IU1 treatment increased levels of peIF2a in both WT and S63del L. Sciatic nerves were treated ex vivo with 200 lM IU1 for 16 hr and the levels of p-eIF2a and eIF2a were analyzed by western blot. A Student’s t-test was performed between treated and untreated conditions of the same genotype

    Glia, 2018, 66(2):379-395. IU1 purchased from Selleck.

  • ELISA analyzed the concentrations of IFN‐β in serum from IU1- or DMSO-treated mice.

    Eur J Immunol, 2018, doi:10.1002/eji.201847603. IU1 purchased from Selleck.

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Biological Activity

Description IU1 is a cell-permeable, reversible and selective proteasome inhibitor of human USP14 with IC50 of 4.7 μ M, 25-fold selective to IsoT. IU1 induces autophagy.
USP14 [1]
(cell-free assay)
4.7 μM
In vitro

IU1 binds specifically to the activated form of USP14. IU1 can potentially inhibit USP14 by preventing its docking on the proteasome, exhibiting little or no activity toward 8 other DUBs, IsoT, UCH37, BAP1, UCH-L1, UCH-L3, USP15, USP2, USP7. USP14 inhibition is rapidly established upon addition of IU1 and rapidly reversed upon its removal. IU1 inhibits USP14 induced chain trimming and decreases electrophoretic mobility of Ub-CCNB species. IU1 enhances proteasomal degradation of Ub-CCNB in the presence of USP14. IU1 promots degradation of tau and depletes TDP-43, ATXN3, and glial fibrillary acidic protein (GFAP) in proteotoxic mechanisms. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293T MW\GeY5kfGmxbjDhd5NigQ>? M3j6NVMxKHWP NETiZ5gzKGi{cx?= NHfJbFJKdmirYnn0bY9vKG:oIHTleYJqeXWrdHnuZZNmKGmwIFjFT|I6O1RiY3XscJMh\XiycnXzd4lv\yCQLYTldo1qdmGuIFjBMZRi\2enZDD1ZolyfWm2aX6gZZN{\XO|ZXSgZZMhe3SjYnnsbZpifGmxbjDv[kBJVVdvVXKgdJJwfGWrboOgZZQhOzBidV2gZYZ1\XJiMjDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz NVnOWFBJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C1NlgyPjhpPkOwOVI5OTZ6PD;hQi=>

... Click to View More Cell Line Experimental Data


Kinase Assay:[1]
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High-throughput screening:

Screening is conducted at the ICCB-Longwood screening facility. 10 μL of recombinant USP14 protein are dispensed into each well of a 384-well low volume plate in duplicate, using a Wellmate plate dispenser. 33.3 nL of compound from the library are pin-transferred into the wells using a Seiko pin transfer robotic system, followed by pre-incubation for about 30 min. The last two columns of each plate are used for positive and negative controls for the assay. To initiate the enzyme reaction, 10 μL of VS-proteasome plus Ub-AMC mixture are added to each well, using a Wellmate dispenser. Samples are then incubated for another 45 min. Ub-AMC hydrolysis is measured at Ex355/Em460 using an Envision plate reader. The final concentrations of USP14, VS-proteasome and Ub-AMC are 15 nM, 1 nM and 0.8 μM, respectively. The final concentration of test compound is approximately 17 μM. Enzymes and substrates are prepared in Ub-AMC assay buffer (50 mM Tris-HCl (pH 7.5), 1 mM EDTA, 1 mM ATP, 5 mM MgCl2, 1 mM DTT, and 1 mg/Ml ovalbumin).
Cell Research:[1]
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  • Cell lines: MEF cells
  • Concentrations: ~1.5 mM
  • Incubation Time: 48 hours
  • Method: MTT
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 60 mg/mL (199.75 mM)
Ethanol 60 mg/mL (199.75 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 300.37


CAS No. 314245-33-5
Storage powder
in solvent
Synonyms N/A
Smiles CC1=CC(=C(N1C2=CC=C(C=C2)F)C)C(=O)CN3CCCC3

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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O

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DUB Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID