PKD (Protein kinase D) is an evolutionarily conserved protein kinase family with structural, enzymological, and regulatory properties different from the PKC family members. Signaling through PKD is induced by a remarkable number of stimuli, including G-protein-coupled receptor agonists and polypeptide growth factors.
PKD (Protein kinase D) family of serine/threonine protein kinases has three members: PKD1, PKD2, PKD3. PKD1, the most studied member of the family, is increasingly implicated in the regulation of a complex array of fundamental biological processes, including signal transduction, cell proliferation and differentiation, membrane trafficking, secretion, immune regulation, cardiac hypertrophy and contraction, angiogenesis, and cancer. PKD mediates such a diverse array of normal and abnormal biological functions via dynamic changes in its spatial and temporal localization, combined with its distinct substrate specificity.
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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; shows selectivity against a panel of > 90 protein kinases including PKCα/PKBα/MEK/ERK/c-Raf/c-Src/c-Abl; 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; potently blocks tumor growth in vivo.
kb-NB142-70 is a potent and selective PKD inhibitor with IC50 of 28.3 nM; displays 10-fold increase in the in vitro PKD1 inhibitory potency versus CID755673; inhibits PC-3, PANC-1, CFPAC-1 cellular growth with IC50 of 5-30 uM.
The first potent and selective cell-active pan-PKD inhibitor with IC50s of 182/280/227 nM for PKD1/2/3 respectively; exhibits selectivity for PKD1 versus AKT, PLK1, CAK, CAMKIIα and three PKC isoforms; blockes phorbol ester-induced endogenous PKD1 activation in LNCaP cells and inhibits prostate cancer cell proliferation, cell migration and invasion.
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