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ERK Inhibitor

Product Name
ERK Inhibitor
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
Formula Weight
328.81
MOL File
1049738-54-6.mol
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ERK Inhibitor Property

storage temp. 
+2C to +8C
solubility 
DMSO: 2 mg/ml
form 
Light yellow solid
color 
Off-white to yellow
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
328006-M
Product name
ERK Inhibitor
Purity
The ERK Inhibitor, also referenced under CAS 1049738-54-6, controls the biological activity of ERK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applica
Packaging
1 unit
Price
$133
Updated
2025/07/31
Cayman Chemical
Product number
15944
Product name
ERK Inhibitor
Purity
≥95%
Packaging
500μg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
15944
Product name
ERK Inhibitor
Purity
≥95%
Packaging
1mg
Price
$50
Updated
2024/03/01
Cayman Chemical
Product number
15944
Product name
ERK Inhibitor
Purity
≥95%
Packaging
5mg
Price
$117
Updated
2024/03/01
AK Scientific
Product number
9473CW
Product name
ErkInhibitor
Packaging
5mg
Price
$228
Updated
2021/12/16
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ERK Inhibitor Chemical Properties,Usage,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.

Uses

ERK-IN-4 is an ERK inhibitor binds preferentially to ERK2 with a Kd of 5 μM. ERK-IN-4 specificity inhibits ERK Rsk-1 and Elk-1 phosphorylation. ERK-IN-4 has little effect on ERK protein phosphorylation by its upstream activator MEK1/2[1].

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

IC 50

ERK2: 5 μM (Kd)

References

[1] Chad N Hancock, et al. Identification of novel extracellular signal-regulated kinase docking domain inhibitors. J Med Chem. 2005 Jul 14;48(14):4586-95. DOI:10.1021/jm0501174

ERK Inhibitor Preparation Products And Raw materials

Raw materials

Preparation Products

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ERK Inhibitor Suppliers

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1049738-54-6, ERK InhibitorRelated Search:


  • (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