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
• Empirical Formula (Hill Notation): C₁₄H₁₆N₂O₃S · xHCl
• CAS Number: 1049738-54-6
• Molecular Weight: 292.35 (free base basis)
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• 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
• storage temp.: 2-8°C

Description

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 K_D 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.

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 K_D 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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable