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Submit ReviewCRT 0066101
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% (HPLC)
Biological Activity for CRT 0066101
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 for CRT 0066101
| M. Wt | 411.33 |
| Formula | C18H22N6O.2HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1883545-60-5 |
| PubChem ID | 69074905 |
| InChI Key | CXYCRYGNFKDPRH-FMOMHUKBSA-N |
| Smiles | OC1=C(C3=NC(NC[C@@H](CC)N)=CC=N3)C=C(C2=CN(C)N=C2)C=C1.Cl.Cl |
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.
Solubility Data for CRT 0066101
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 41.13 | 100 | |
| DMSO | 8.23 | 20 |
Preparing Stock Solutions for CRT 0066101
The following data is based on the product molecular weight 411.33. Batch specific molecular weights may vary from batch to batch due to the degree 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 |
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Product Datasheets for CRT 0066101
References for CRT 0066101
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.
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Keywords: CRT 0066101, CRT 0066101 supplier, CRT0066101, potent, pan, protein, kinase, D, PKD, PKD1, PKD2, PKD3, inhibits, inhibitors, Protein, Kinase, 4975, Tocris Bioscience
7 Citations for CRT 0066101
Citations are publications that use Tocris products. Selected citations for CRT 0066101 include:
Liou et al (2015) Protein kinase D1 drives pancreatic acinar cell reprogramming and progression to intraepithelial neoplasia. Sci Rep 6 6200 PMID: 25698580
Steve N et al (2021) Inhibiting Protein Kinase D Promotes Airway Epithelial Barrier Integrity in Mouse Models of Influenza A Virus Infection. Front Immunol 11 580401 PMID: 33381112
Ben et al (2021) Evaluation of protein kinase D auto-phosphorylation as biomarker for NLRP3 inflammasome activation. PLoS One 16 e0248668 PMID: 34767572
Stephan A et al (2021) Protein kinase D promotes activity-dependent AMPA receptor endocytosis in hippocampal neurons. Traffic 22 454-470 PMID: 34564930
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
Peter et al (2020) The GEF-H1/PKD3 signaling pathway promotes the maintenance of triple-negative breast cancer stem cells. Int J Cancer 146 3423-3434 PMID: 31745977
Zhang et al (2017) Protein kinase D at the Golgi controls NLRP3 inflammasome activation. J Exp Med 214 2671 PMID: 28716882
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 4 Reviews.)
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Good and reliable PKD inhibitor.
By
Anonymous on 09/20/2019
Assay Type: In Vivo
Species: Mouse
Used in an in-vivo behavioral assay
Easy to dissolve in solution, works great in an in-vivo animal study. (Mechanical allodynia assay). Good and reliable PKD inhibitor
Lysophospatidic acid promotes microglia motility via the LPAR5-PKD axis..
By
lisha joshi on 06/10/2019
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: BV2 microglia cells
The inhibitor was dissolved in DMSO and used at a concentration of 1µM (concentrations of 0.1µM and 0.5µM were also tested but we observed more potent inhibition with 1µM). BV2 microglia were treated with LPA (1µM) in the presence or absence of CRT. Using a time lapse microscope we analyzed the impact of PKD family inhibition on the LPA induced microglial migration.
PKD family inhibition in LPA induced pro-inflammatory phenotype in microglia.
By
Joanna Plastira on 06/08/2019
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: Primary murine microglia cells
Primary murine microglia were incubated for different time points with LPA (1µM) in the presence or absence of CRT (1µM). CRT significantly inhibited the expression of COX2 and promoted the expression of Arg1. DMSO can sometimes induce an expression (for different proteins) under control conditions. We observed this problem in BV2 cell line (but not in primary cells). In this case it is best to dilute the CRT in water.
Very potent PKD inhibitor.
By
Anonymous on 11/06/2017
Assay Type: In Vivo
Species: Mouse
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)