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Merck

A6355

Sigma-Aldrich

3-(2-Aminoethyl)-5-((4-ethoxyphenyl)methylene)-2,4-thiazolidinedione hydrochloride

powder, ≥98% (HPLC)

Synonym(e):

Erk Inhibitor

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About This Item

Empirische Formel (Hill-System):
C14H16N2O3S · HCl
CAS-Nummer:
Molekulargewicht:
328.81
MDL-Nummer:
UNSPSC-Code:
12352202
PubChem Substanz-ID:
NACRES:
NA.77

Assay

≥98% (HPLC)

Form

powder

Lagerbedingungen

desiccated
under inert gas

Farbe

off-white

Löslichkeit

DMSO: ≥4 mg/mL

Lagertemp.

2-8°C

SMILES String

Cl[H].CCOc1ccc(cc1)C=C2SC(=O)N(CCN)C2=O

InChI

1S/C14H16N2O3S.ClH/c1-2-19-11-5-3-10(4-6-11)9-12-13(17)16(8-7-15)14(18)20-12;/h3-6,9H,2,7-8,15H2,1H3;1H/b12-9+;

InChIKey

PQVLWVGMXJPJLG-NBYYMMLRSA-N

Anwendung

3-(2-Aminoethyl)-5-((4-ethoxyphenyl)methylene)-2,4-thiazolidinedione is an extracellular signal-regulated kinase (ERK) docking domain inhibitor. ERK inhibitors have been used to study traumatic brain injuries.

Biochem./physiol. Wirkung

3-(2-Aminoethyl)-5-((4-ethoxyphenyl)methylene)-2,4-thiazolidinedione is extracellular signal-regulated kinase (ERK) docking domain inhibitor. Inhibits ERK binding rather then ERK activity at the ATP domain. IC50 = 25 μM in HeLa, A549, and SUM-159 tumor cells. Currently, no specific inhibitors of the ERK proteins exist. 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, but exhibits little effect on ERK1/2 phosphorylation by MEK1/2.

Leistungsmerkmale und Vorteile

This compound is featured on the MAPKs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable


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The Journal of biological chemistry, 284(38), 25889-25899 (2009-06-09)
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Artikel

The mitogen-activated protein kinase (MAPK) family consists of both stress activated (SAPK) and mitogen-activated (MAPK) protein kinases. They form a network of signal transduction cascades that mediate cellular responses to a diverse range of stimuli, including growth factors, chemical or osmotic stress, irradiation, bacterial infection and proinflammatory cytokines.

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