Basic information Safety Supplier Related

ERK Inhibitor

Basic information Safety Supplier Related

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
  • 3-(2-aminoethyl)-5-[(4-ethoxyphenyl)methylene]-2,4-thiazolidinedione,monohydrochloride
  • ERK-IN-4
CAS:
1049738-54-6
MF:
C14H17ClN2O3S
MW:
328.81
Mol File:
1049738-54-6.mol
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ERK Inhibitor Chemical Properties

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

Shanghai Run-Biotech Co., Ltd.
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