Protein kinase D inhibitor 1 (compound 17m) is a potent pan-PKD inhibitor. It exhibits inhibitory activity in the low nanomolar range, with IC50 values ranging between 17 and 35 nM. By inhibiting protein kinase D, this compound effectively suppresses cortactin phosphorylation, which is known to be PKD-dependent [1].

Protein kinase D inhibitor 1 (compound 17m) displays excellent PKD2 inhibition with almost no remaining kinase activity at 1 μM [1]. 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 [1]. Protein kinase D inhibitor 1 (0-100 μM, 72 h) shows antitumor activity [1]. Cell Viability Assay [1] Cell Line: LN-229, Capan-1, DND-41, HL-60, Z-138, NCI-H460, HCT-116, K-562 Concentration: 0-100 μM Incubation Time: 72 h Result: Inhibited of tumor cell growth of LN-229, Capan-1, DND-41, HL-60, Z-138, NCI-H460, HCT-116, and K-562, with IC 50 values of 80.6 ± 7, 40.7 ± 14.5, 42.7 ± 4.9, 17.9 ± 4.1, 35.3 ± 10.4, >95.8, >100, and >100, respectively.