Product Background: Once PI 3-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.
Featured in Publications:
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
Class I PI3K Activity Assays: Echelon has multiple formats available. Please see the PI3-K Assay Comparison Chart for more information.
Class III PI3K Activity Assay (K-3000)
Lipid Mass ELISA's: PIP3 Mass ELISA (K-2500s) and PI(4,5)P2 Mass ELISA (K-4500)
Human PI3K Enzymes: alpha (p110α/p85α), beta (p110β/p85alphα), PI3Kααα E545K – Active Mutant (p110α/p85α)
Mouse PI3K Enzyme: PI3K (p110α/p85α)
Optimized PI3K enzyme buffer (K-KBZ)
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 email@example.com.
Product Keywords: PI3-Kinase, PI3K, Phosphatidylinositol 3-kinases, PI 3-kinases, PI3Ks, K-1000
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