AG-18 118409-57-7

.cp_wz table {border-top: 1px solid #ccc;border-left:1px solid #ccc; } .cp_wz table td{border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;} .cp_wz table th {border-right: 1px solid #ccc;border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;}


Molecular Weight:

186.17 AG-18 inhibits EGFR with IC50 of 35 μM.


Biological Activity


AG 18 inhibits EGFR and IR with Ki of 11 μM and 12 mM. AG 18 inhibits EGF-induced EGFR autophoshporylation with IC50 of 15 μM in A431 cells. AG 18 (10 μM) inhibits EGF-induced proliferation of GH3 cells. AG 18
(10 μM) causes significant inhibition of the cell proliferation induced
by 10 nM and 1 μM ghrelin. AG 18 (10 μM) blocks the ghrelin-stimulated
increase in ERK 1/2 phosphorylation in GH3 cells.


AG 18 inhibits the
volume-sensitive release of [3H]taurine in primary astrocyte cultures in
a dose-dependent manner. AG 18 activates Swelling-induced
volume-dependent D-[3H]aspartate release from primary astrocytic
cultures. AG 18 (300 μM) inhibits TPA-induced stimulation
of ICAM-1 expression in a dose dependent manner in A549 epithelial
cells. AG 18 (300 μM) also inhibits TPA stimulated NF-kappaB DNA-protein
binding and ICAM-1 promoter activity in A549 epithelial cells.


AG 18
(300 μM) inhibits TNF-alpha-induced NF-kappaB DNA-protein binding and
ICAM-1 promoter activity in a dose dependent manner in A549 epithelial
cells. IKK activity is stimulated by both TNF-alpha and TPA, and these
effects are inhibited by AG 18 (100 μM) in A549 epithelial cells. AG 18 (10 μM) decreases the potency of 5-HT 4-fold and reduces the
maximal contraction to 5-HT in the carotid artery. AG 18 (10 μM) shifts
KCl-induced contraction 2-fold and causes the maximum significantly
inhibition.






EGF-Receptor Autophosphorylation


WGA-purified EGF receptor from A431 cells (0.5 μg/assay) is activated
with EGF (800 nM) for 20 min at 4 ℃. The reaction is initiated by the
addition of Mg(Ac)2 (60 mM), Tris-Mes buffer, pH 7.6 (50 mM), and [32P]ATP
(20 pM, 5 μCi/assay). The reaction is conducted at either 4 ℃ or 15 ℃
and terminated by addition of sodium dodecyl sulfate (SDS) sample buffer
(10% glycerol, 50 mM Tris, pH 6.8, 5% β-mercaptoethanol, and 3% SDS).


The samples are run on a 8% SDS polyacrylamide gel (SDS-PAGE) (prepared
from 30% acrylamide and 0.8% bis-(acrylamide) and contained 0.375 M
Tris, pH 8.8, 0.1% SDS, 0.05% TEMED, and 0.46% ammonium persulfate). The
gel is dried and autoradiography is perfromed with Agfa Curix RP2 X-ray
film. The relevant radioactive bands are cut and counted in the
Cerenkov mode.


The fast phase of autophosphorylation continued for
another 10 min. The extent of phosphorylation completed in the first 10 s
at 15 ℃ comprises 1/3 of the total autophosphorylation signal and
probably reflects the phosphorylation of the first site on the receptor.
The 10-s interval is therefore chosen for use in subsequent
autophosphorylation experiments.






Method


GH3 cells are plated at 5 × 104 cells/well in media
containing 2% charcoal-stripped FCS and various concentrations of
ghrelin, desoctanoylated ghrelin and PMA or EGF for 72 hours with the
addition of 2 μCi/well [3H]thymidine for a further 6 hours. A
time-course of 24 hours, 48 hours and 72 hours is performed for ghrelin
stimulation and 72 hours is selected for further experiments.


Studies
are also performed to investigate the effect of rat ghrelin or
desoctanoyl ghrelin-induced proliferation and the effect of U0126,
GF109203X, AG 18, wortmannin and H-89 upon ghrelin-induced MAPK
stimulation. AG 18 at 10 μM is added 30 min before each treatment. Cells
are harvested before counting in the presence of scintillation fluid
using a Microbeta 1450 bcounter. Experiments are repeated at least three
times.

Contact us if you need more details on 118409-57-7. We are ready to answer your questions on packaging, logistics, certification or any other aspects about AG-18 118409-57-7、118409-57-7 AG-18. If these products fail to match your need, please contact us and we would like to provide relevant information.

Product Categories : Protein Tyrosine Kinase > EGFR Inhibitor