CRT 0066101

Catalog #: 4975
7 Citations Datasheet / COA / SDS

Catalog #	Availability	Size / Price	Qty
4975/10

CRT 0066101 | CAS No. 1883545-60-5 | Protein Kinase D Inhibitors

1 Image

Description: Potent protein kinase D (PKD) inhibitor

Chemical Name: 2-[4-[[(2R)-2-aminobutyl]amino]-2-pyrimidinyl]-4-(1-methyl-1H-pyrazol-4-yl)phenol dihydrochloride

Purity: ≥98%

View All Products for Protein Kinase D Inhibitors

Product Details

Citations (7)

Reviews

Biological Activity Technical Data Background Product Datasheets Calculators

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

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

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

COA view current batch

Or select another batch:

View Batch

SDS

Reconstitution Calculator

Molarity Calculator

Reconstitution Calculator

Molarity Calculator

Mass

Concentration

Volume

M. Wt* g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

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

Protein kinase D promotes activity-dependent AMPA receptor endocytosis in hippocampal neurons.
Authors: Stephan A Et al.
Traffic 2021;22:454-470
Evaluation of protein kinase D auto-phosphorylation as biomarker for NLRP3 inflammasome activation.
Authors: Ben Et al.
PLoS One 2021;16:e0248668
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
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
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.
J.Biol.Chem. 2016;291:11285
Protein kinase D1 drives pancreatic acinar cell reprogramming and progression to intraepithelial neoplasia.
Authors: Liou Et al.
Sci Rep 2015;6:6200

FAQs

No product specific FAQs exist for this product, however you may

View all Small Molecule FAQs

Reviews for CRT 0066101

There are currently no reviews for this product. Be the first to review CRT 0066101 and earn rewards!

Have you used CRT 0066101?

Submit a review and receive an Amazon gift card.

$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Tocris Bioscience is the leading supplier of novel and exclusive tools for life science research with over 30 years' experience in the industry. Tocris is a Bio-Techne brand.