ATP-competitive PDK-1 inhibitor (IC50 value 5 μM for both PDK-1/PDPK1) that inhibits the growth of thyroid, prostate and breast cancer xenografts in vivo. A Celecoxib (Axon 1919) derivative that inhibits PAK phosphorylation and cell proliferation with reduced Akt phosphorylation by PDK1, without inhibition of cycloogygenases. Moreover, overexpression of constitutively active forms of PDK-1 and Akt partially protected OSU-03012-induced apoptosis.

KEYWORDS: OSU 03012 | supplier | PDK-1 inhibitor | OSU03012 | CAS [742112-33-0] | Phosphatidylinositol | PDPK | PAK | Akt | apoptosis | prostate | breast | thyroid | cancer | proliferation | p70S6 | p21 | PKC