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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.



1883545-60-5 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.


521937-07-5 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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