1781742-22-0

Protein kinase D (PKD) is a serine/threonine protein kinase that is activated by diacylglycerol, commonly downstream of PKC signaling. The three human PKD isoforms target a variety of proteins to alter cell proliferation, survival, invasion, and protein transport. CRT0066101 is an inhibitor of all three PKD isoforms (IC₅₀s = 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively).¹ It exhibits selectivity for PKD against a panel of >90 protein kinases, including PKCα, PKBα, MEK, ERK, c-Raf, c-Src, and c-Abl.¹ It can block cell proliferation, induce apoptosis, and reduce the viability of pancreatic cancer cells both in vitro and in vivo.¹

1. Harikumar, K.B., Kunnumakkara, A.B., Ochi, N., et al. A novel small-molecule inhibitor of protein kinase D blocks pancreatic cancer growth in vitro and in vivo Mol. Cancer Ther. 9(5),1136-1146(2010).