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.
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Synonym(s):
ERK Inhibitor, 3-(2-Aminoethyl)-5-((4-ethoxyphenyl)methylene)-2,4-thiazolidinedione, HCl
Empirical Formula (Hill Notation):
C14H16N2O3S · xHCl
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Quality Level
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
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.
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
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
WGK
WGK 1
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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