OSU-03012 is an analog of the COX-2 inhibitor Celecoxib (Celebrex®) which has anti-cancer activity. However, it does not inhibit COX-2 but rather is an inhibitor (IC50 = 5 mM) of phosphoinositide-dependant kinase-1 (PDK-1) thus preventing activation of Akt. OSU-03012 has been shown to have pro-apoptotic and anti-proliferative effects on of multiple cancer cell lines such as PC-3 (prostate), chronic lymphocytic leukemia, pancreatic, breast, glioblastoma, and myeloma with low micromolar IC50 values. |
