CRT 0066101

Catalog # Availability Size / Price Qty
CRT 0066101 | CAS No. 1883545-60-5 | Protein Kinase D Inhibitors
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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%

Product Details
Citations (3)
Reviews (4)

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

Soluble to 100 mM in water and to 20 mM in DMSO
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.

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Citations for CRT 0066101

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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
Application: Species: Mouse

Used in an in-vivo behavioral assay

PMID: 31142616 Reference

Lysophospatidic acid promotes microglia motility via the LPAR5-PKD axis.
By lisha joshi on 06/10/2019
Application: Species: Mouse

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
Application: Species: Mouse

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
Application: Species: Mouse

The product was used per os on mice for an invivo study.

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