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Applications: Study enzyme kinetics and screen small molecule 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. They are heterodimeric proteins with a regulatory and a catalytic subunit. The heterodimer between p110 (catalytic subunit) and p85 (regulatory subunit) belongs to class IA. P110 and p85 have three variants each. P110α is ubiquitously expressed, and p85α is the most abundant variant of p85. Class I PI3K participates in cell signaling, mostly via the activation of PKB (protein kinase B) and the PI3K/AKT/mTOR pathway. Dysfunction of these kinases impacts cell growth and differentiation, and mutations in p110α have been linked to cancer. At least three isoform-specific inhibitors are approved by FDA for the treatment of lymphoma and leukemia. Further studies will help identify more selective inhibitors with a good tolerance that can bypass the development of drug resistance.
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 p110α (E545K)/p85α Kinase Assay Kit is designed to measure the kinase activity of the complex PI3 (phosphoinositide 3) kinase consisting of mutant p110α (E545K) and p85α 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 human complex PI3 Kinase p110α (E545K)/p85α kinase, 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: p110α(E545K): P42336; p85α: P27986
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Vanhaesebroeck B., et al., 2021 Nature Reviews Drug Discovery 20: 741-769.
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