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

PKD2:35 ± 5 nM, PKD3:17 ± 8 nM, PKD1:35 ± 10 nM

Protein kinase D inhibitor 1 (compound 17m) exhibits potent inhibition of PKD2 with almost no kinase activity at 1 μM [1]. Despite its significant PKD2 inhibition, it shows minimal antiproliferative effects on PANC-1 cells at 5 μM [1]. However, it reveals antitumor activity across a range of concentrations (0-100 μM) over 72 hours [1]. In a Cell Viability Assay on various cell lines including LN-229, Capan-1, DND-41, HL-60, Z-138, NCI-H460, HCT-116, and K-562, this compound effectively inhibited tumor cell growth. The IC50 values were 80.6 ± 7, 40.7 ± 14.5, 42.7 ± 4.9, 17.9 ± 4.1, and 35.3 ± 10.4 for the first five lines respectively, while exceeding 95.8 µM for NCI-H460, and greater than 100 µM for both HCT-116 and K-562 [1].