NSC117079

NSC117079 is a small molecule, selective inhibitor of PH domain leucine-rich repeat protein phosphatases (PHLPP1 and PHLPP2). Originally identified through chemical and virtual screening of the National Cancer Institute (NCI) Diversity Set, NSC117079 acts by blocking the PP2C phosphatase domain of PHLPP. This inhibition prevents the dephosphorylation of AKT, thereby enhancing AKT phosphorylation and promoting downstream cell survival, proliferation, and tissue repair pathways. NSC117079 is widely utilized as a pharmacological research tool to investigate PHLPP-dependent signaling in various therapeutic areas, including neuroprotection, inflammation, and osteoarthritis. In preclinical models of post-traumatic osteoarthritis (PTOA), intra-articular administration of NSC117079 has been shown to reduce cartilage degradation, decrease pathological sensory innervation (such as NaV1.8-positive fiber branching), and attenuate mechanical allodynia.

Other names

1-amino-9,10-dioxo-4-(3-sulfamoylanilino)anthracene-2-sulfonic acid1-amino-9,10-dioxo-4-(3-sulfamoylphenylamino)-9,10-dihydroanthracene-2-sulfonic acid