[CAS NO. 1883545-60-5]  CRT0066101 dihydrochloride

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PRODUCTS SPECIFICATIONS [1883545-60-5]

Catelog
SLK-S8366
Brand
Selleck
CAS
1883545-60-5

DESCRIPTION [1883545-60-5]

Overview

MDLMFCD30182249
Molecular Weight411.33
Molecular FormulaC18H22N6O.2HCl
SMILESOC1=CC=C(C2=CN(C)N=C2)C=C1C3=NC=CC(NC[C@H](N)CC)=N3.[H]Cl.[H]Cl

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.4311 mL12.1557 mL24.3114 mL
5 mM0.4862 mL2.4311 mL4.8623 mL
10 mM0.2431 mL1.2156 mL2.4311 mL
50 mM0.0486 mL0.2431 mL0.4862 mL

Description

CRT0066101 dihydrochloride is a small molecule 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 nM2 nM2.5 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.