BODIPY TMR PI(3,4,5)P3 (BODIPY TMR Phosphatidylinositol 3,4,5-trisphosphate) is a water soluble analog of PI(3,4,5)P3 (PIP3) labeled with the orange fluorophore, Bodipy^®-TMR, at the sn-1 position.

Phosphoinositides (PIPns) are minor components of cellular membranes but are integral signaling molecules for cellular communication. Phosphatidylinositol 3,4,5-trisphosphate (PIP3), formed from PI(4,5)P2 though phosphorylation by PI 3-kinase, activates numerous signaling pathways resulting in cell proliferation, growth, survival, glucose transport and protein synthesis. High PIP3 levels from disregulation of PI3-K have been demonstrated in cancer and inflammatory diseases. PIP3 is hydrolyzed by the phosphatases PTEN to PI(4,5)P2 and SHIP to PI(3,4)P2.

Publications

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1. Sweeney, G., et al. (2004). “Intracellular delivery of phosphatidylinositol (3,4,5)-trisphosphate causes incorporation of glucose transporter 4 into the plasma membrane of muscle and fat cells without increasing glucose uptake.” J Biol Chem 279(31): 32233-32242.2. Heffron, T. P., et al. (2016). “The Rational Design of Selective Benzoxazepin Inhibitors of the -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).” J Med Chem 59(3): 985-1002.3. 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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