| Identification | Back Directory | [Name]
ERK Inhibitor | [CAS]
1049738-54-6 | [Synonyms]
ERK Inhibitor - CAS 1049738-54-6 - Calbiochem
(5Z)-3-(2-aminoethyl)-5-[(4-ethoxyphenyl)methylidene]-1,3-thiazolidine-2,4-dione:hydrochloride | [Molecular Formula]
C14H17ClN2O3S | [MDL Number]
MFCD09038681 | [MOL File]
1049738-54-6.mol | [Molecular Weight]
328.81 |
| Hazard Information | Back Directory | [Description]
ERK inhibitor is a cell-permeable inhibitor that binds ERK2 near its docking domain (KD = 5 μM). This prevents its interaction with protein substrates without inhibiting catalytic activity. ERK inhibitor blocks ERK-specific phosphorylation of ribosomal S6 kinase-1 and ternary complex factor Elk-1 but does not affect ERK1/2 phosphorylation by MEK1/2. Presumably through its effects on ERK, ERK inhibitor completely prevents proliferation of HeLa cells (IC50 = 15-20 μM), A549 lung carcinoma cells (IC50 = 25 μM), Sum-159 estrogen receptor-negative breast cancer cells and HT1080 fibrosarcoma cells. | [General Description]
A cell-permeable and reversible thiazolidinedione compound that displays anti-proliferative properties (IC50 ≤ 25 μM in HeLa, A549, and SUM-159 tumor cells). 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 in HeLa cells, while exhibiting little effect on ERK1/2 phosphorylation by MEK1/2. | [Biochem/physiol Actions]
Primary TargetERK | [storage]
Store at -20°C |
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