Catalog Number: 4975
Chemical Name: 2-[4-[[(2R)-2-aminobutyl]amino]-2-pyrimidinyl]-4-(1-methyl-1H-pyrazol-4-yl)phenol dihydrochloride
Biological Activity
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
  • M.Wt:
    411.33
  • Formula:
    C18H22N6O.2HCl
  • Solubility:
    Soluble to 100 mM in water and to 20 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    1883545-60-5
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. PKD1 mediates negative feedback of PI3K/Akt activation in response to G protein-coupled receptors.
    Ni et al.
    PLoS One, 2013;8:e73149
  2. 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:

The citations listed below are publications that use Tocris products. Selected citations for CRT 0066101 include:

2 Citations: Showing 1 - 2
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  1. 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
  2. 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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