CRT 0066101
Chemical Name: 2-[4-[[(2R)-2-aminobutyl]amino]-2-pyrimidinyl]-4-(1-methyl-1H-pyrazol-4-yl)phenol dihydrochloride
Purity: ≥98%
Biological Activity
CRT 0066101 is a 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Insulin Receptor and GPCR Crosstalk Stimulates YAP via PI3K and PKD in Pancreatic Cancer Cells
F Hao, Q Xu, Y Zhao, JV Stevens, SH Young, J Sinnett-Sm, E Rozengurt
Mol. Cancer Res., 2017;0(0):. -
Protein kinase D1 (PKD1) phosphorylation on Ser(203) by type I p21-activated kinase (PAK) regulates PKD1 localization
JK Chang, Y Ni, L Han, J Sinnett-Sm, R Jacamo, O Rey, SH Young, E Rozengurt
J. Biol. Chem., 2017;0(0):. -
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
Product Datasheets
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Citations for CRT 0066101
The citations listed below are publications that use Tocris products. Selected citations for CRT 0066101 include:
7 Citations: Showing 1 - 7
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Protein kinase D promotes activity-dependent AMPA receptor endocytosis in hippocampal neurons.
Authors: Stephan A Et al.
Traffic 2021;22:454-470
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Evaluation of protein kinase D auto-phosphorylation as biomarker for NLRP3 inflammasome activation.
Authors: Ben Et al.
PLoS One 2021;16:e0248668
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Inhibiting Protein Kinase D Promotes Airway Epithelial Barrier Integrity in Mouse Models of Influenza A Virus Infection.
Authors: Steve N Et al.
Front Immunol 2021;11:580401
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The GEF-H1/PKD3 signaling pathway promotes the maintenance of triple-negative breast cancer stem cells.
Authors: Peter Et al.
Int J Cancer 2020;146:3423-3434
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Protein kinase D at the Golgi controls NLRP3 inflammasome activation.
Authors: Zhang Et al.
J Exp Med 2017;214:2671
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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.
J.Biol.Chem. 2016;291:11285
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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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