ERK Inhibitor

ERK Inhibitor Structure
CAS No.
1049738-54-6
Chemical Name:
ERK Inhibitor
Synonyms
ERK-IN-4;ERK Inhibitor - CAS 1049738-54-6 - Calbiochem;3-(2-aminoethyl)-5-[(4-ethoxyphenyl)methylene]-2,4-thiazolidinedione,monohydrochloride;(5Z)-3-(2-aminoethyl)-5-[(4-ethoxyphenyl)methylidene]-1,3-thiazolidine-2,4-dione:hydrochloride
CBNumber:
CB13136749
Molecular Formula:
C14H17ClN2O3S
Molecular Weight:
328.81
MOL File:
1049738-54-6.mol
Modify Date:
2024/7/2 8:55:00

ERK Inhibitor Properties

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

ERK Inhibitor Chemical Properties,Uses,Production

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

Raw materials

Preparation Products

ERK Inhibitor Suppliers

(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 1049738-54-6