nsc117079

Description: NSC117079 is a novel and potent PHLPP1 (Pleckstrin homology domain and leucine-rich repeat protein phosphatase 1) inhibitor. PHLPP1 inhibits protein kinase B (AKT) survival signaling in neurons. Small molecule pan-PHLPP inhibitors (selective for PHLPP1 and PHLPP2) may offer a translatable method to induce AKT neuroprotection. NSC-117079 at 30 uM induces neutrophil adhesion to plated fibrinogen from 9.0+/-2.4% to 27.0+/-8.0% and enhanced neutrophil adhesion caused by 50 ng/mL GM-CSF from 22.9+/-6.0% to 47.6+/-10.9%. Neutrophil adhesion is followed by neutrophil transendothelial migration. Results suggest that PHLPP inhibitor NSC-117079 is effective in preventing Akt from dephosphorylation in neutrophils, and Akt phosphatase PHLPP serves to attenuate neutrophil adhesion but not migration.

References: J Pharmacol Exp Ther. 2013 Nov; 347(2):516-28.;