PI3-Kinase Activity Fluorescence Polarization Assay

Product Number: K-1100

$454.00

$454.00
SKU: K-1100- Category: Tags: , , , ,

The PI3-Kinase Activity Fluorescence Polarization Assay determines PI3-K activity through quantification of its product, PI(3,4,5)P3 (PIP3).


Sample Type: in vitro determination of PI3-K activity in cancer tissues and cell lines and compound screening for drug discovery
Sample Volume: 2.5-5.0 µL enzyme / inhibitor
Assay Range: 0.0625 µM to 4.0 µM


Product Background
The PI3-Kinase Activity Fluorescence Polarization Assay measures PIP3. Briefly, once PI3-K reaction are complete, the PIP3 detector protein and the fluorescent probe are added. Polarization (mP) values decrease as probe, binding to the PIP3 detector, is displaced by the PIP3 produced by enzymatic activity.

Class I Phosphoinositide 3-kinases (PI3-K), are ubiquitously expressed lipid kinases which phosphorylate PI(4,5)P2 (PIP2) at the 3-hydroxyl of the inositol ring producing PIP3 has shown to be an important lipid second messenger with key roles in fundamental cellular responses such as proliferation and survival. Due to these interesting biological roles, PI3-K and PIP3 have become attractive targets for research and drug development in many diseases including inflammation and cancer.

Echelon has multiple formats available for Class III PI3-K. Please see the PI3-K Assay Comparison Guide below for more information.

Product Keywords: PI3-Kinase, PI3K, Phosphatidylinositol 3-kinases, PI 3-kinases, PI3Ks, K-1000

Bulk Discounts: Bulk discounts are available, please email echelon@echelon-inc.com for details

Notice to Purchaser: Echelon Biosciences products are sold for research and development purposes only and are not to be incorporated into products for resale without written permission from Echelon Biosciences. This kit and all non-radioactive, competitive assays for determining phosphoinositide-3-kinase (PI3-K) activity are covered by Echelon Biosciences Inc. U.S. Patent 7,067,269. The purchase of this product includes a limited, non-transferable immunity from suit under the foregoing patent claims for using only this amount of product for the purchaser’s own internal research. For inquiries email busdev@echelon-inc.com.

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Kits & Assays

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Activity, Inhibitor, Kinase, PI3K

Technical Data Sheet

PI3K Assay Comparison Guide

1. Drees, B. E., A. Weipert, et al. (2003). “Competitive fluorescence polarization assays for the detection of phosphoinositide kinase and phosphatase activity.” Comb Chem High Throughput Screen 6(4): 321-330.
2. Dehnhardt, C. M., Mansour Tarek S. (2009). “Lead Optimization of N-3-Substituted 7-Morpholinotriazolopyrimidines as Dual Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitors: Discovery of PKI-402.” J. Med. Chem.
3. Safina, B. S., S. Baker, et al. (2012). “Discovery of Novel PI3-Kinase d Specific Inhibitors for the Treatment of Rheumatoid Arthritis: Taming CYP3A4 Time-Dependent Inhibition.” Journal of Medicinal Chemistry 55(12): 5887–5900.
4. Heffron, T. P., R. A. Heald, et al. (2016). “The Rational Design of Selective Benzoxazepin Inhibitors of the δ-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).” Journal of Medicinal Chemistry.DOI: 10.1021/acs.jmedchem.5b01483
5. Yin, Y., et al. (2019). “Design, synthesis and biological evaluation of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates containing sulfonamido as potential PI3Kα inhibitors.” Bioorganic & Medicinal Chemistry 27(11): 2261-2267.

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