Description
AG 18 inhibits EGFR with IC50 of 35 μM.
Storage
2 years -20 centigrade Powder; 2 weeks 4 centigrade in DMSO; 6 months -80 centigrade in DMSO.
Molecular Formula
C10H6N2O2
Chemical Name
Propanedinitrile, 2-[(3,4-dihydroxyphenyl)methylene]-
Solubility
DMSO 37 mg/mL; Water <1 mg/mL; Ethanol 37 mg/mL
In vitro
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. [2]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.
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