SF1670 is an inhibitor of PTEN (IC50 = 2 μM). PTEN (Phosphatase and Tensin Homolog deleted on Chromosome 10) is a 3’ phosphoinositide phosphatase that converts PI(3,4,5)P3 to PI(4,5)P2 thus opposing PKB/Akt activation by PI 3-K. Pretreatment of neutrophils with SF1670 leads to enhanced fMLP-1 induced PI(3,4,5)P3 signaling effects such as Akt phosphorylation, NADPH oxidase-mediated superoxide formation, cell polarization, chemotactic migration, and phagocytosis. SF1670 also inhibits CD45 (IC50 = 200 nM).
Publications
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2) Yousefi, B., et al. (2017). “Balaglitazone reverses P-glycoprotein-mediated multidrug resistance via upregulation of PTEN in a PPARγ-dependent manner in leukemia cells.” Tumor Biology 39(10): 1010428317716501.
3) Alsina-Sanchís, E., et al. (2018). “ALK1 (Activin-Receptor Like Kinase 1) Loss Results in Vascular Hyperplasia in Mice and Humans Through PI3K (Phosphatidylinositol 3-Kinase) Activation.” Arteriosclerosis, thrombosis, and vascular biology 38(5): 1216-1229.
4) Mitchell, J., et al. (2018). “Colonic Inhibition of Phosphatase and Tensin Homolog Increases Colitogenic Bacteria, Causing Development of Colitis in Il10-/- Mice.” Inflammatory Bowel Diseases 24(8): 1718-1732.
