PDK-1 (3-phosphoinositide-dependent protein kinase 1) is a Ser/Thr protein kinase and a member of the protein A, G, and C (AGC) family. Through phosphorylation and subsequent activation of a number of other AGC kinase family members, such as protein kinase B, PDK-1, the key node in the PI3K pathway, plays a crucial role in insulin and growth-factor signaling.
The control of cell proliferation and migration is handled by PDK-1, which has also been linked to a number of cancers, including pancreatic and breast cancer. Activation of PDK-1 targets like Akt, S6K (p70 ribosomal S6 kinase), and SGK is caused by a number of cancer-causing mutations. As a result, PDK1 has attracted a lot of interest as a potential target for oncology drugs because it is a key activator of numerous pro-survival and oncogenic protein kinases.
|BX795 is a novel, potent and selective/specific PDK-1 (3-phosphoinositide-dependent kinase-1) inhibitor with potential antitumor activity.
|BX912 (BX-912) is a novel, potent and specific inhibitor of PDK-1 (phosphoinositide-dependent kinase 1) inhibitor with potential antitumor activity.
|GSK2334470 (GSK-2334470) is a novel, highly specific and potent inhibitor of PDK1 (3-phosphoinositide-dependent protein kinase) with potential antitumor activity.
|OSU-03012 (also called AR12), acelecoxib derivative without COX-2 inhibitory activity, is an orally bioavailable, specific, and potent inhibitor of recombinant PDK-1 (3-phosphoinositide-dependent kinase-1) with potential antitumor activity.