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HomeProduct name listERK Inhibitor

ERK Inhibitor

Synonym(s):3-(2-Aminoethyl)-5-((4-ethoxyphenyl)methylene)-2,4-thiazolidinedione, HCl;ERK Inhibitor - CAS 1049738-54-6 - Calbiochem

ERK Inhibitor Structural

What is ERK Inhibitor?

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.

What are the applications of Application

ERK Inhibitor is a cell-permeable thiazolidinedione compound that shows anti-proliferative properties

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

Properties of ERK Inhibitor

storage temp.  +2C to +8C
solubility  DMSO: 2 mg/ml
form  Light yellow solid
color  Off-white to yellow

Safety information for ERK Inhibitor

Computed Descriptors for ERK Inhibitor

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