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Application: Enzyme kinetics studies and screening small molecule inhibitors for drug discovery and high-throughput screening (HTS) applications.
Background: Ubiquitin specific peptidase 21 (USP21), also known as USP23, belongs to a large group of ubiquitin-specific proteases capable of cleaving ubiquitin from other proteins. These enzymes are also referred to as deubiquitinating peptidases, deubiquitinases (DUBs), ubiquitin proteases, ubiquitin hydrolases or ubiquitin isopeptidases. They contribute to the ubiquitin signaling pathway by countering the signal induced by ubiquitin conjugating enzymes and ligases. USP21 has several substrates, including RIP (ribosome-inactivating protein), MEK2 (dual specificity mitogen-activated protein kinase kinase 2) and GATA3 (GATA binding protein 3), and thus contributes to multiple pathways related to cellular homeostasis and diseases, such as cancer, auto-immune disorders and obesity. The use of USP21 inhibitors may open new avenues of treatment for these diseases.
Description: The USP21 Inhibitor Screening Assay Kit is a 96-well format fluorogenic assay designed to measure the activity of the deubiquitinating (DUB) enzyme USP21 (ubiquitin specific peptidase 21) for screening and profiling applications. The kit contains enough purified USP21 protein, Ubiquitinated-AMC substrate, and assay buffer for 100 reactions. To determine the effect of an inhibitor on USP21 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 DUB subfamilies ubiquitin C-terminal hydrolases (UCHs), ubiquitin-specific proteases (USPs), Ovarian Tumor Proteases (OTU), and Machado-Josephin domain proteases (MJD). Figure 1: Illustration of the assay principle. Ubiquitin-AMC is a fluorogenic substrate for ubiquitin hydrolases based on the C-terminus derivatization of ubiquitin with 7-amido-4-methylcoumarin (AMC). In conjugated form, the energy emitted from fluorochrome AMC is quenched. Upon proteolysis, AMC is no longer quenched and emits fluorescence with excitation/emission maxima of 350/460 nm. The increase in fluorescence is proportional to the DUB activity. Need us to run inhibitor screens or profile your compounds against USP21? Check out our Protease Screening Services or Ubiquitination Screening Services.
Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.
Target: USP21
Uniprot: Q9UK80
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: An T., et al., 2022 Front Pharmacol. 13:944989.
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