Potent inhibitor of protein kinase D (PKD); inhibits all PKD isoforms (IC50
values are 1, 2 and 2.5 nM for PKD1, PKD3 and PKD2 respectively). Exhibits selectivity for PKD against a panel of >90 protein kinases, including PKCα
, MEK, ERK, c-Raf and c-Src. Reduces proliferation and cell viability of pancreatic cancer cells expressing moderate levels of endogenous PKD1/2. Orally bioavailable.
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All Tocris products are intended for laboratory research use only.
PKD1 mediates negative feedback of PI3K/Akt activation in response to G protein-coupled receptors.
Ni et al.
PLoS One, 2013;8:e73149
A novel small molecule inhibitor of protein kinase D blocks pancreatic cancer growth in vitro and in vivo.
Harikumar et al.
Mol.Cancer Ther., 2010;9:1136
The citations listed below are publications that use Tocris products. Selected citations for CRT 0066101 include:
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