Other grades of this product :
| ERK Inhibitor Basic information |
| Product Name: | ERK Inhibitor | | Synonyms: | (5Z)-3-(2-aminoethyl)-5-[(4-ethoxyphenyl)methylidene]-1,3-thiazolidine-2,4-dione:hydrochloride;ERK Inhibitor - CAS 1049738-54-6 - Calbiochem | | CAS: | 1049738-54-6 | | MF: | C14H17ClN2O3S | | MW: | 328.81 | | EINECS: | | Product Categories: | | Mol File: | 1049738-54-6.mol |
| ERK Inhibitor Chemical Properties |
| storage temp. | +2C to +8C | | form | Light yellow solid |
| ERK Inhibitor Usage And Synthesis |
| 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 |
| ERK Inhibitor Preparation Products And Raw materials |
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