Chemical Name: 2-[4-[[(2R)-2-aminobutyl]amino]-2-pyrimidinyl]-4-(1-methyl-1H-pyrazol-4-yl)phenol dihydrochloride
Biological ActivityPotent 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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Tocris products are intended for laboratory research use only, unless stated otherwise.
PKD1 mediates negative feedback of PI3K/Akt activation in response to G protein-coupled receptors.
Ni et al.
PLoS ONE, 2013;9: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
Citations for CRT 0066101
The citations listed below are publications that use Tocris products. Selected citations for CRT 0066101 include:
3 Citations: Showing 1 - 3
Protein kinase D at the Golgi controls NLRP3 inflammasome activation.
Authors: Zhang Et al.
J Exp Med 2017;214:2671
Protein kinase D and Gβγ subunits mediate agonist-evoked translocation of protease-activated receptor-2 from the Golgi apparatus to the plasma membrane.
Authors: Jensen Et al.
Protein kinase D1 drives pancreatic acinar cell reprogramming and progression to intraepithelial neoplasia.
Authors: Liou Et al.
Sci Rep 2015;6:6200
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The inhibitor was dissolved in DMSO and used at a concentration of 1µM (concentrations of 0.1µM and 0.5µM were also tested but we observed more potent inhibition with 1µM). BV2 microglia were treated with LPA (1µM) in the presence or absence of CRT. Using a time lapse microscope we analyzed the impact of PKD family inhibition on the LPA induced microglial migration.
Primary murine microglia were incubated for different time points with LPA (1µM) in the presence or absence of CRT (1µM). CRT significantly inhibited the expression of COX2 and promoted the expression of Arg1. DMSO can sometimes induce an expression (for different proteins) under control conditions. We observed this problem in BV2 cell line (but not in primary cells). In this case it is best to dilute the CRT in water.
The product was used per os on mice for an invivo study.