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IU1

Catalog No. T6107 CAS 314245-33-5

IU1(IC50=4.7 μ M), a reversible, specific human USP14 proteasome inhibitor, can penetrate the cell.

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IU1, CAS 314245-33-5

Pack Size	Availability	Price/USD
5 mg	In stock	$ 54.00
10 mg	In stock	$ 76.00
25 mg	In stock	$ 146.00
50 mg	In stock	$ 252.00
100 mg	In stock	$ 448.00
1 mL * 10 mM (in DMSO)	In stock	$ 59.00

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Purity: 99.11%

Purity: 98.77%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	IU1(IC50=4.7 μ M), a reversible, specific human USP14 proteasome inhibitor, can penetrate the cell.
Targets&IC50	USP14:4.7 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]
Kinase Assay	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	MTT(Only for Reference)

Molecular Weight	300.37
Formula	C18H21FN2O
CAS No.	314245-33-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL (100 mM)

Ethanol: 15 mg/mL (50 mM)

References and Literature

1. Byung-Hoon L, et al. Nature, 2010, 467(7312), 179-184.

Citations

1. Wu W, Xu H, Liao C, et al. Blockade of USP14 potentiates type I interferon signaling and radiation-induced antitumor immunity via preventing IRF3 deubiquitination. Cellular Oncology. 2022: 1-15 2. Yue X, Liu T, Wang X, et al.Pharmacological inhibition of BAP1 recruits HERC2 to competitively dissociate BRCA1–BARD1, suppresses DNA repair and sensitizes CRC to radiotherapy.Acta Pharmaceutica Sinica B.2023

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Ubiquitination Compound Library Anti-Aging Compound Library DNA Damage & Repair Compound Library Fluorochemical Library Anti-Cancer Compound Library Bioactive Compound Library HIF-1 Signaling Pathway Compound Library Cell Cycle Compound Library Autophagy Compound Library

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FT671 IU1-248 USP28-IN-3 USP28-IN-4 B-AP15 USP8-IN-2 USP7/USP47 inhibitor RA-9

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

IU1 314245-33-5 Autophagy Cell Cycle/Checkpoint DNA Damage/DNA Repair Ubiquitination DUB inhibit DUBs IU 1 Inhibitor Deubiquitinase IU-1 inhibitor

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