CRT0066101 dihydrochloride is a potent, specific, orally active pan-PKD (protein kinase D) inhibitor with biochemical IC50 of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively.
CRT0066101 dihydrochloride is a potent, specific, orally active pan-PKD (protein kinase D) inhibitor with biochemical IC50 of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively.
CRT0066101 shows selectivity against a panel of > 90 protein kinases including PKCα/PKBα/MEK/ERK/c-Raf/c-Src/c-Abl.
CRT0066101 reduces bromodeoxyuridine incorporation, increases apoptosis, blocks neurotensin-induced PKD1/2 activation and reduces neurotensin-induced, PKD-mediated Hsp27 phosphorylation, attenuated PKD1-mediated NF-kappaB activation in pancreatic cancer cells.
CRT0066101 potently blocks tumor growth in vivo.
