CRT 0066101

Cat. No. 4975

CRT 0066101 C18H22N6O.2HCl [1883545-60-5]

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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 20 mM in water and to 10 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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

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.

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.

If you know of a relevant reference for CRT 0066101 please let us know.

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.

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Keywords: CRT 0066101, supplier, CRT0066101, potent, pan, protein, kinase, D, PKD, PKD1, PKD2, PKD3, inhibits, inhibitors, Tocris Bioscience, Protein Kinase D Inhibitor products

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