118409-57-7 (AG 18)
||2-(3,4-Dihydroxybenzylidene)malononitrile; AG 18; AG 18 (pharmaceutical); RG 50810; RG 50858; TX 825; Tyrphostin 23; Tyrphostin A 23; Tyrphostin AG 18; 2-(3,4-dihydroxybenzylidene)malononitrile
AG-18(RG-50810; Tyrphostin A23) inhibits EGFR with IC50 of 40 μM.
IC50 Value: 40 uM (inhibition of EGFR autophosphorylation)
AG-18 (Tyrphostin A23) are inhibitors of tyrosine kinases and function by binding to the active sites of the enzymes.
Protocol(Only for Reference)
||10 μM; 0.5 hour
||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.
||Selleck Chemicals LLC
Physical and Chemical Properties
|Appearance:Light yellow to yellow Solid
Mechanism and Indication
||Sponsor & Collaborators
||No Development Reported
Other Forms of 118409-57-7
Recommended Compounds in
Recommended Compounds in Same Indication
. Lyall RM, Zilberstein A, Gazit A, Tyrphostins inhibit epidermal growth factor (EGF)-receptor tyrosine kinase activity in living cells and EGF-stimulated cell proliferation. J Biol Chem. 1989 Aug 25;264(24):14503-9.
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. Ortiz-Zapater E, Soriano-Ortega E, Marcote MJ, Trafficking of the human transferrin receptor in plant cells: effects of tyrphostin A23 and brefeldin A. Plant J. 2006 Dec;48(5):757-70.
. Ogura T, Imanishi S, Shibamoto T. Activation of background membrane conductance by the tyrosine kinase inhibitor tyrphostin A23 and its inactive analog tyrphostin A1 in guinea pig ventricular myocytes. Jpn J Pharmacol. 2001 Nov;87(3):235-9.
. Salomonsson M, Arendshorst WJ. Effect of tyrosine kinase blockade on norepinephrine-induced cytosolic calcium response in rat afferent arterioles. Am J Physiol Renal Physiol. 2004 May;286(5):F866-74.