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Applications: Study enzyme kinetics and screen small molecular inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: PI3 (phosphoinositide 3) kinase, or phosphatidylinositol 3 kinases, are a family of proteins that can be subdivided into four classes: I, II, III and IV. Class I are involved in converting PI (4, 5) P2 (phosphatidylinositol (4, 5)-biphosphate) into PI (3, 4, 5) P3 (phosphatidylinositol (3, 4, 5)-triphosphate) when activated by tyrosine kinase receptors and G-protein coupled receptors. p120γ is also known as PIK3CG (phosphatidylinositol-4,5-biphosphate 3-kinase catalytic subunit), PI3Kγ or p110γ and belongs to class IB. p120γ plays a role in chemotaxis, cytokine release and ROS (reactive oxygen species) generation and is thus an important player in the innate and adaptive immune systems. It has been linked to inflammatory diseases, such as RA (rheumatoid arthritis), atherosclerosis and other cardiovascular pathologies, lupus and cancer. The use of p120γ inhibitors combined with immune checkpoints inhibitors has potential in cancer therapy. Further studies into the modes of action and structure of p120γ will allow the development of more selective inhibitors and advance the treatment of inflammatory diseases and cancer linked to this protein.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.The PI3K lipid substrate is shipped separately on ice. Please store it at 4°C upon arrival (DO NOT FREEZE the PI3K lipid substrate).
Description: The Chemi-Verse™ PI3 Kinase (p120γ) Kinase Assay Kit is designed to measure PI3 (phosphoinositide 3) kinase (p120γ) kinase activity for screening and profiling applications using ADP-Glo™ as a detection reagent. The assay kit comes in a convenient 96-well format, with enough purified recombinant PI3 kinase (p120γ), kinase substrate, ATP, and kinase assay buffer for 100 enzyme reactions.
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: P48736
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Rathinaswamy M., et al., 2021, Sci Adv 7 (35): eabj4282.
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