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.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 411.33. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.43 mL||12.16 mL||24.31 mL|
|5 mM||0.49 mL||2.43 mL||4.86 mL|
|10 mM||0.24 mL||1.22 mL||2.43 mL|
|50 mM||0.05 mL||0.24 mL||0.49 mL|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
References are publications that support the products' biological activity.
Harikumar et al (2010) A novel small molecule inhibitor of protein kinase D blocks pancreatic cancer growth in vitro and in vivo. Mol.Cancer Ther. 9 1136 PMID: 20442301
Ni et al (2013) PKD1 mediates negative feedback of PI3K/Akt activation in response to G protein-coupled receptors. PLoS ONE 9 e73149 PMID: 24039875
If you know of a relevant reference for CRT 0066101, please let us know.
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2 Citations for CRT 0066101
Citations are publications that use Tocris products. Selected citations for CRT 0066101 include:
Jensen et al (2016) Protein kinase D and Gβγ subunits mediate agonist-evoked translocation of protease-activated receptor-2 from the Golgi apparatus to the plasma membrane. J.Biol.Chem. 291 11285 PMID: 27030010
Liou et al (2015) Protein kinase D1 drives pancreatic acinar cell reprogramming and progression to intraepithelial neoplasia. Sci Rep 6 6200 PMID: 25698580
Do you know of a great paper that uses CRT 0066101 from Tocris? If so please let us know.