PDK1-IN-2 is a small molecule inhibitor of 3-phosphoinositol-dependent protein kinase-1 (PDK1). PDK1-IN-2 inhibits the binding of PDK1 to its substrate by competitively binding to the PIF pocket of PDK1, thereby inhibiting the kinase activity and downstream signaling of PDK1. PDK1-IN-2 can be used for cell survival and proliferation in cancer.
References:
[1]. Rettenmaier T J, et al. A small-molecule mimic of a peptide docking motif inhibits the protein kinase PDK1[J]. Proceedings of the National Academy of Sciences, 2014, 111(52): 18590-18595.