CRT0066101 is a very potent inhibitor of Protein Kinase D (PKD) isoforms with IC50 values for PKD-1, -2 and -3 = 1, 2.5 and 2 nM, respecitively. CRT0066101 has been shown to have anticancer activity. CRT0066101 potently inhibits proliferation of PANC-1 pancreatic cells, and blocks migration and invasion of U87MG glioblastoma cells. CRT0066101 has also been shown to decrease growth of primary tumors and metastasis of ER(-) breast cancers.