A novel celecoxib derivative, that acts as a potent inhibitor of 3-phosphoinositide-dependent kinase-1 (PDK1) activity (IC₅₀ = 5 µM for recombinant PDK1). It displays anti-cancer activity in a COX-2-independent manner via inhibition of the phosphatidyl inositol-3-kinase(PI3K)/Akt pathway. OSU03012 is a potent inhibitor of tumor cell growth with an average inhibitory concentration of 1.1 µM across a panel of 60 cancer cell lines.