SPRINTer™ IKZF2 Protein Turnover Biosensor Cell Line (Jurkat)
The SPRINTer™ IKZF2 Protein Turnover Biosensor Cell Line (Jurkat) is a stable clonal cell line used for monitoring drug-induced protein turnover of IKZF2.
Catalog #: 91-1010C19
Size: 2 vials
Unit Price: Contact For Pricing
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Overview
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IKZF2 Biological Background
IKZF2, also known as Helios, is a transcription factor in the Ikaros family, primarily expressed in T cells and hematopoietic cells. It plays a crucial role in immune regulation by supporting regulatory T cells (Tregs), which maintain immune tolerance and prevent autoimmune diseases. Dysregulated IKZF2 is linked to hematological cancers like acute myeloid leukemia (AML), where it promotes leukemic stem cell survival and impairs myeloid differentiation, making it a key therapeutic target.
Transcription factors like IKZF2 are challenging to target with traditional small-molecule inhibitors, driving interest in targeted protein degradation technologies, such as PROTACs and molecular glues, which induce proteasomal degradation of IKZF2.
The SPRINTer IKZF2 Protein Turnover Biosensor Cell Line provides a powerful tool for studying IKZF2 degradation, advancing the development of innovative therapies for cancer and autoimmune diseases.
Product Highlights
- Tailored for studying IKZF2-targeted protein degradation using PROTACs and molecular glues
- Offers robust detection of protein turnover dynamics with exceptional sensitivity
- Real-time assessment of IKZF2 protein stability and degradation
- Designed for ease of use in compound characterization and screening studies
SPRINTer IKZF2 Protein Turnover Biosensor Assay Principle
Identify new molecular entities, such as PROTACs, that modulate IKZF2 protein levels in physiologically-relevant cell models using a homogenous assay format. The SPRINTer™ IKZF2 Protein Turnover Biosensor Assay enables sensitive quantification of PROTAC-mediated degradation of IKZF2.
This assay leverages stable biosensor cell lines that have been engineered using CRISPR/Cas9 gene editing to introduce Eurofins DiscoverX’s Enzyme Fragment Complementation (EFC) small β-galactosidase (β-gal) enzyme donor (ED) fragment into the endogenous IKZF2 gene locus. Expression of IKZF2 from its native promoter results in the production of an ED-tagged IKZF2 protein. The ED-tagged IKZF2 is then brought into close proximity to the cellular protein degradation machinery by a PROTAC.
The bi-functional small molecule PROTAC bridges the IKZF2 protein and a specific endogenous E3 ligase, which is responsible for the ubiquitin-mediated degradation of the target protein. By bringing the ED-tagged IKZF2 in proximity to the E3 ligase, the PROTAC induces ubiquitination and subsequent degradation of IKZF2. This results in the loss of the EFC signal.
The loss of the EFC signal occurs because the ED-tagged IKZF2 can no longer bind to the exogenous EFC large enzyme acceptor (EA) fragment, preventing the formation of a functional β-gal enzyme. Without this enzyme, the assay substrate cannot be hydrolyzed, resulting in the absence of a chemiluminescent signal. This EFC-based protein degradation technology enables quantification of drug-induced changes in IKZF2 protein levels, measuring the kinetics of PROTAC-induced degradation, and is suitable for high throughput screening to identify potential IKZF2-targeting drugs.
SPRINTer IKZF2 Protein Turnover Biosensor Assay Principle