CRT 0066101

Tocris Bioscience | Catalog # 4975

Potent protein kinase D (PKD) inhibitor
Tocris Bioscience

Key Product Details

Description

Potent protein kinase D (PKD) inhibitor
View all Protein Kinase D Inhibitors »

Product Description

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.

Product Specifications for CRT 0066101

Molecular Weight

411.33

Formula

C18H22N6O.2HCl

Storage

Store at -20°C

Purity

≥98% (HPLC)

Chemical Name

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

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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Background References

References are publications that support the biological activity of the product. See our Citations tab to view 51 publications citing the usage of this product.

Product Documents for CRT 0066101

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for CRT 0066101

For research use only

Customer Reviews for CRT 0066101 (4)

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  • Good and reliable PKD inhibitor
    Name: Anonymous
    Species: Mouse
    Assay Type: In Vivo
    Verified Customer | Posted 09/20/2019
    Easy to dissolve in solution, works great in an in-vivo animal study. (Mechanical allodynia assay). Good and reliable PKD inhibitor
    Used in an in-vivo behavioral assay
    CRT 0066101 4975
  • Lysophospatidic acid promotes microglia motility via the LPAR5-PKD axis.
    Name: lisha joshi
    Species: Mouse
    Assay Type: In Vitro
    Cell Line/Tissue: BV2 microglia cells
    Verified Customer | Posted 06/10/2019
    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.
    CRT 0066101 4975
  • PKD family inhibition in LPA induced pro-inflammatory phenotype in microglia
    Name: Joanna Plastira
    Species: Mouse
    Assay Type: In Vitro
    Cell Line/Tissue: Primary murine microglia cells
    Verified Customer | Posted 06/08/2019
    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.
    CRT 0066101 4975
  • Very potent PKD inhibitor
    Name: Anonymous
    Species: Mouse
    Assay Type: In Vivo
    Verified Customer | Posted 11/06/2017
    the CRT0066101 PKD inhibitor can be dissolved in normal saline or DMSO easily (depends of the concentration)
    The product was used per os on mice for an invivo study.

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