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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|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|
References are publications that support the biological activity of the product.
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.
View Related Products by Product Action
Keywords: CRT 0066101, CRT 0066101 supplier, CRT0066101, potent, pan, protein, kinase, D, PKD, PKD1, PKD2, PKD3, inhibits, inhibitors, Protein, Kinase, 4975, Tocris Bioscience
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? Please let us know.
Reviews for CRT 0066101
Average Rating: 5 (Based on 1 Review.)
Have you used CRT 0066101?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
The product was used per os on mice for an invivo study.
the CRT0066101 PKD inhibitor can be dissolved in normal saline or DMSO easily (depends of the concentration)
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.