In Vitro: Protein kinase D inhibitor 1 (compound 17m) displays excellent PKD2 inhibition with almost no remaining kinase activity at 1 μM. Protein kinase D inhibitor 1 displays only weak antiproliferative activity, and does not significantly affect PANC-1 cell proliferation at a concentration of 5 μM. Protein kinase D inhibitor 1 (0-100 μM, 72 h) shows antitumor activity.