IU1

Catalog No.S7134

For research use only.

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.

IU1 Chemical Structure

CAS No. 314245-33-5

Selleck's IU1 has been cited by 18 publications

Purity & Quality Control

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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.
Targets
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 MonTSpVv[3Srb36gZZN{[Xl? NHnGVmw{OCC3TR?= Mn\INkBpenN? MVXJcohq[mm2aX;uJI9nKGSndXLpdZVqfGmwYYPlJIlvKEiHS{K5N3Qh[2WubIOg[ZhxemW|c3nu[{BPNXSncn3pcoFtKEiDLYTh[4dm\CC3YnnxeYl1cW5iYYPz[ZN{\WRiYYOgd5Ri[mmuaYrheIlwdiCxZjDIUXcuXWJicILveIVqdnNiYYSgN|AhfU1iYX\0[ZIhOiCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| NGjjNWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEWyPFE3QCd-M{C1NlgyPjh:L3G+

Protocol (from reference)

Kinase Assay:[1]
  • 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]
  • Cell lines: MEF cells
  • Concentrations: ~1.5 mM
  • Incubation Time: 48 hours
  • Method: MTT

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.

5mg/mL

Chemical Information

Molecular Weight 300.37
Formula

C18H21FN2O

CAS No. 314245-33-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=C(N1C2=CC=C(C=C2)F)C)C(=O)CN3CCCC3

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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