Chemi-Verse™ PI3 Kinase P110α (H1047R)/P85α Kinase Assay Kit

Catalog #
82103
$605 *
Size: 96 reactions
Qty
*US Pricing only. For international pricing, please contact your local distributor.
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Description

The Chemi-Verse™ PI3 Kinase P110α(H1047R)/P85α Kinase Assay Kit is designed to measure the kinase activity of complex PI3 (phosphoinositide 3) kinase consisting of mutant P110α (H1047R) 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(H1047R)/P85α kinase, kinase substrate, ATP, and kinase assay buffer for 100 enzyme reactions.

Synonyms
Serine/threonine protein kinase PIK3CA, p110α, p110-alpha, PI3K-alpha, PtdIns-3-kinase subunit p110-alpha, MCM, CCM4, CWS5, MCAP, PI3K, CLAPO, CLOVE, MCMTC, PIK3R1, PtdIns-3-kinase regulatory subunit alpha, AGM7, GRB1, p85, p85-ALPHA, PI3K, pi3k
Product Info
Storage and Usage
Citations
Assay Kit Format
Luminescent
Materials Required But Not Supplied
  • ADP-Glo™ Kinase Assay (Promega #V6930)
  • DTT (Dithiothreitol), 1M, optional
  • Microplate reader capable of reading luminescence
  • Adjustable micropipettor and sterile tips
  • 30°C incubator
Format
Catalog # Name Amount Storage
40641 PI3 kinase P110α (H1047R)/ P85α, FLAG-Tag* >1 µg -80°C
79334 5x Kinase Buffer 1 1.5 ml -20°C
79386 500 µM ATP 50 µl -20°C
40560 PI3K Lipid Substrate (Packaged separately, Do Not Freeze!) 500 µl 4°C
79696 White 96-well plate 1 Room Temp

*The concentration of the protein is lot-specific and will be indicated on the tube.

UniProt #
p110α (H1047R): P42336; p85α: P27986
Background

PI3 (phosphoinositide 3) kinases, 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.

References

Vanhaesebroeck B., et al., 2021, Nature Reviews Drug Discovery 20: 741-769.