CRT0066101

Catalog No.S8366

CRT0066101 Chemical Structure

Molecular Weight(MW): 411.33

CRT0066101 is a small molecule PKD family specific inhibitor which specifically blocks PKD1/2 activity and does not suppress PKCα/PKCβ/PKCε activity in multiple.

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Choose Selective Serine/threonin kinase Inhibitors

Biological Activity

Description CRT0066101 is a small molecule PKD family specific inhibitor which specifically blocks PKD1/2 activity and does not suppress PKCα/PKCβ/PKCε activity in multiple.
Targets
PKD1 [1]
(Cell-free assay)
PKD3 [1]
(Cell-free assay)
PKD2 [1]
(Cell-free assay)
1 nM 2 nM 2.5 nM
In vitro

CRT0066101 reduces BrdU incorporation, increases apoptosis, blocks neurotensin (NT)-induced PKD1/2 activation, reduces NT-induced PKD-mediated Hsp27 phosphorylation, attenuates PKD1-mediated NF-κB activation, and abrogates expression of NF-κB-dependent-dependent proliferative and pro-survival proteins. CRT0066101 significantly inhibits Panc-1 cell proliferation with an IC50 value of 1 μM. It also significantly reduces cell proliferation of Colo357, Panc-1, MiaPaCa-2, and AsPC-1 cells but has a modest effect in Capan-2 cells. Thus, CRT0066101 significantly blocks proliferation of PaCa cells that express moderate to high endogenous levels of PKD1/2. CRT0066101 (5 µM) blocks both the basal and NT-induced pS916-PKD1/2 (activated PKD1/2) in Panc-1 and Panc-28 cells, also abrogates NT-induced phosphorylation of Hsp27 (pS82-Hsp27), which is a physiological substrate of PKD1/2 in a dose-dependent manner[1].

Assay
Methods Test Index PMID
Western blot
Ppkd/PKC μ / pGSK3α / pGSK3β / β-catenin; 

PubMed: 26895471     


Western blot analysis of GSK3/β-catenin signaling following treatment with 0.1–10 μM of CRT0066101 in MCF-7-ADR cell lines. Blots are representative of five independent experiments. β-actin was used as the loading control. 

p-AKT / AKT / p-ERK / ERK; 

PubMed: 24634417     


Cells were exposed to CRT0066101 for 24 hours, and protein expression was determined by Western blot analysis. 

Cyclin D1 / Survivin / cIAP-1; 

PubMed: 20442301     


Panc-1 cells were either transfected with control (Panc-1) or PKD1 over-expressing (Panc-1-PKD1) vectors and 23 h post-transfection were treated with DMSO (−) or 5 µM CRT0066101 (+) for 1 h prior to preparation of whole cell lysates to analyze effects on 䲧疝Ỵ疞㧀疜膉痘 瘿뾠ՂᾰƌՂĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ՂĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒

26895471 24634417 20442301
In vivo CRT0066101 given orally (80 mg/kg/day) for 28 days significantly abrogates PaCa growth in Panc-1 subcutaneous xenograft model. Activated PKD1/2 expression in the treated tumor-explants is significantly inhibited with peak tumor concentration (12 µM) of CRT0066101 achieved within 2 h after oral administration. CRT0066101 given orally (80 mg/kg/day) for 21 days in Panc-1 orthotopic model potently blocks tumor growth in vivo. CRT0066101 significantly reduces Ki-67+ proliferation index (p< 0.01), increases TUNEL+ apoptotic cells (p<0.05), and abrogates expression of NF-κB-dependent proteins including cyclin D1, survivin, and cIAP-1. CRT0066101 blocks Panc-1 cell proliferation and growth in multiple xenograft models[1]

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: Panc-1 cells
  • Concentrations: 5 μM
  • Incubation Time: 1 h
  • Method:

    Panc-1 cells are either transfected with control (Panc-1) or PKD1 over-expressing (Panc-1-PKD1) vectors and 23 h post-transfection are treated with DMSO (−) or 5 µM CRT0066101 (+) for 1 h prior to preparation of nuclear extracts (NE) for measuring NF-κB activation by EMSA


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: CR-UK nu/nu mice
  • Formulation: 5% dextrose
  • Dosages: 80 mg/kg 
  • Administration: by oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro Water 82 mg/mL (199.35 mM)
DMSO 25 mg/mL warmed (60.77 mM)
Ethanol 2 mg/mL warmed (4.86 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 411.33
Formula

C18H22N6O.2HCl

CAS No. 1883545-60-5
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID