Protein kinase D inhibitor 1

Protein kinase D inhibitor 1 (compound 17m) is a pan-PKD inhibitor, with IC50 values ranging from 17 to 35 nM. Protein kinase D inhibitor 1 inhibits PKD-dependent cortactin phosphorylation[1].

Research Areas >> Cancer

Signaling Pathways >> Apoptosis >> PKD

PKD3:17 ± 8 nM (IC50)

PKD2:35 ± 5 nM (IC50)

PKD1:35 ± 10 nM (IC50)

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 IC50 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.

[1]. Gilles P, et al. Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine-based protein kinase D inhibitors. Eur J Med Chem. 2020 Nov 1;205:112638.