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Merck
CN

328006-M

ERK Inhibitor

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 applications.

Synonym(s):

ERK Inhibitor, 3-(2-Aminoethyl)-5-((4-ethoxyphenyl)methylene)-2,4-thiazolidinedione, HCl

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About This Item

Empirical Formula (Hill Notation):
C14H16N2O3S · xHCl
CAS Number:
1049738-54-6
Molecular Weight:
292.35 (free base basis)
MDL number:
MFCD09038681
UNSPSC Code:
12352200
NACRES:
NA.77

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InChI key

PQVLWVGMXJPJLG-UHFFFAOYSA-N

SMILES string

S1C(=O)N(C(=O)C1=Cc2ccc(cc2)OCC)CCN.Cl

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

color

light yellow

solubility

DMSO: 10 mg/mL

Quality Level

100

Related Categories

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 Target
ERK
Target IC50: ≤ 25 µM for anti-proliferative properties in HeLa, A549, and SUM-159 tumor cells; KD of ~5 µM for ERK2

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Hancock, C. N., et al. 2005. J. Med. Chem.48, 4586.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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