USP22 Inhibitor Screening Assay Kit

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Application: Study enzyme kinetics and screening small molecule inhibitors for drug discovery and high-throughput screening (HTS) applications.

Background: USP22 (ubiquitin-specific peptidase 22) is a member of the USP DUBs (deubiquitinases) protein group. Deubiquitinases play a role in several cellular processes including transcriptional regulation, cell cycle progression or innate immunity. In humans, USP22 is ubiquitously expressed. Overexpression of this protein has been linked to cancer, diabetes, neurological disorders and male infertility. In the context of cancer, USP22 overexpression levels correlate with patient prognosis. In prostate cancer, USP22 promotes the activity of AR (androgen receptor). In addition, as part of the transcription regulatory histone acetylation (HAT) complex SAGA (Spt-Ada-Gcn5 acetyl transferase complex) it catalyzes the deubiquitination of both histones H2A and H2B. It can also induce cell cycle progression by stabilizing cyclin B and TRF1 (telomeric repeat binding factor 1) and inhibit apoptosis. In view of all its role as a tumor promoter, targeting USP22 has become an attractive cancer therapeutic option, with the discovery of highly selective USP22 small molecule inhibitors being one of the main challenges.

Description: The USP22 Inhibitor Screening Assay Kit is a fluorogenic assay kit designed to measure the activity of the deubiquitinating (DUB) enzyme USP22 (ubiquitin specific peptidase 22) for screening and profiling applications. The kit contains enough purified USP22, Ubiquitinated-AMC substrate, and assay buffer for 100 reactions.To determine the effect of an inhibitor on USP22 activity, the enzyme should be preincubated with or without the test inhibitor prior to adding the Ub-AMC substrate to the reaction. The assay was functionally validated using Ub-Aldehyde, a potent inhibitor of the DUB subfamilies Ubiquitin C-terminal Hydrolases (UCHs), Ubiquitin-Specific Proteases (USPs), Ovarian Tumor Proteases (OTU), and Machado-Josephin Domain (MJD) proteases.Figure 1: Illustration of the assay principle.
Ubiquitin-AMC (Ub-AMC) is a fluorogenic substrate for ubiquitin hydrolases, based on the C-terminus derivatization of ubiquitin with 7-amido-4-methylcoumarin (AMC). In the conjugated form the energy emitted from the fluorochrome AMC is quenched. Upon release from Ub, AMC emissions are no longer quenched fluorescence with λexcitation/λemission maxima of 350/460 nm is emitted. The increase in fluorescence is proportional to the DUB activity.

Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.

Uniprot: Q9UPT9

Warnings: Avoid freeze/thaw cycles

Biosafety Level: Not applicable (BSL-1)

References: Melo-Cardenas J., et al., 2016 Oncotarget 7(28):44848-44856.

• Artikelnummer: BPS82742
• Hersteller: BPS Bioscience
• Hersteller Artikelnummer: 82742
• Verpackungseinheit: 96 reactions
• Mengeneinheit: PAK