3-(2-aminoetylo)-5-((4-etoksyfenylo)metyleno)-2,4-tiazolidinedion jest inhibitorem domeny dokującej kinazy regulowanej sygnałem zewnątrzkomórkowym (ERK). Inhibitory ERK zostały wykorzystane do badania urazowych uszkodzeń mózgu.
Działania biochem./fizjol.
3-(2-Aminoethyl)-5-((4-ethoxyphenyl)methylene)-2,4-thiazolidinedione is extracellular signal-regulated kinase (ERK) docking domain inhibitor. Inhibits ERK binding rather then ERK activity at the ATP domain. IC50 = 25 μM in HeLa, A549, and SUM-159 tumor cells. Currently, no specific inhibitors of the ERK proteins exist. Preferentially binds to ERK2 with a Kd of ~5 μM and prevents its interaction with protein substrates. Shown to block ERK-mediated phosphorylation of ribosomal S6 kinase-1 (RSK-1) and ternary complex factor Elk-1, but exhibits little effect on ERK1/2 phosphorylation by MEK1/2.
Extracellular signal-regulated kinase (ERK) docking domain inhibitor. Inhibits ERK binding rather then ERK activity at the ATP domain. IC50 = 25 μM in HeLa, A549, and SUM-159 tumor cells.
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